二十二酸 | 112-85-6

• 物质功能分类: 化学试剂 - 有机试剂 - 脂肪酸
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 中文名称: 二十二酸
• 中文别名: 山俞酸；山萮酸；二十二酸(山嵛酸)C22:0；扁油酸；蘿酸；山俞酸(二十二酸)；山嵛酸；二十二碳酸；二十二烷酸
• 英文名称: n-docosanoic acid
• 英文别名: Docosanoic acid；behenic acid
• CAS: 112-85-6
• 化学式: C₂₂H₄₄O₂
• mdl: MFCD00002807
• 分子量: 340.59
• InChiKey: UKMSUNONTOPOIO-UHFFFAOYSA-N

物化性质

• 熔点：
  72-80 °C(lit.)
• 沸点：
  306°C 60mm
• 密度：
  d4100 0.8221
• 闪点：
  306°C/60mm
• 溶解度：
  在氯仿的溶解度为50mg/mL，澄清
• LogP：
  4.121-9.91 at 25℃
• 物理描述：
  OtherSolid, Liquid; PelletsLargeCrystals
• 颜色/状态：
  Waxy solid
• 蒸汽压力：
  7.15X10-8 mm Hg at 25 °C (est)
• 折光率：
  Index of refraction: 1.4270 at 100 °C/D
• 碰撞截面：
  191.18 Ų [M-H]- [CCS Type: DT, Method: single field calibrated with Agilent tune mix (Agilent)]
• 保留指数：
  2567;2564;2569;2564
• 稳定性/保质期：
  1. 避免与氧化剂、还原剂、碱接触。 2. 存在于烤烟烟叶和白肋烟烟叶中。

计算性质

• 辛醇/水分配系数(LogP)：
  9.6
• 重原子数：
  24
• 可旋转键数：
  20
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.954
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

ADMET

毒理性

• 毒性总结

癸酸对大鼠的经口LD50值大于2,000 mg/kg。目前没有关于刺激性和敏感性的数据。在一项使用经合组织（OECD）联合重复剂量和生殖/发育毒性测试[OECD TG 422]的口服研究中，癸酸以0、100、300、1,000 mg/kg/天的剂量给予大鼠，至少连续42天。没有发生死亡，并且在任何参数中都没有观察到与物质相关的毒性效应。因此，重复剂量毒性和生殖/发育毒性的NOAEL（无观察到有害效应的剂量）被认为是1,000 mg/kg/天。该化学物质在细菌突变试验[OECD TG 471, 472]和体外染色体畸变试验[OECD TG 473]中均为阴性。... 癸酸对藻类（小球藻）、水生无脊椎动物（大型溞）或鱼类（青鳉）的急性毒性值大于其水溶性（0.016 mg/L）。在为期21天的大型溞繁殖试验中，NOEC（无观察到效应的浓度）也大于其水溶性。在使用分散剂进行的极高水平测试中，按照OECD测试指南[TG201, 202, 203, 204, 或 211]进行的任何测试中都没有观察到显著效果。有信息显示，某些碳链较短的脂肪酸在饱和浓度下对某些水生生物（淡水的端足类动物；海水条件下的剑尾鱼）没有造成死亡。根据这些数据和额外的信息，可以合理地假设癸酸在其水溶性（0.016 mg/L）以下的浓度对水生生物是无毒的。由于获得的NOEC值高于物质的水溶性，因此没有计算PNEC（预测无效应浓度）。

Oral LD50 value of docosanoic acid for rats is greater than 2,000 mg/kg. There are no available data for irritation and sensitization. In an oral study using the OECD combined repeated dose and reproductive/developmental toxicity test [OECD TG 422], docosanoic acid was administered to rats at doses of 0, 100, 300, 1,000 mg/kg/day for at least 42 days . No deaths occurred and also no substance related toxic effects were observed in any parameters. Therefore, the NOAEL is considered to be 1,000 mg/kg/day for both repeated dose toxicity and reproductive/developmental toxicity. The chemical was negative in both a bacterial mutation test [OECD TG 471, 472] and a chromosomal aberration test in vitro [OECD TG 473]. ... Acute toxicity values of docosanoic acid on alga (Selenastrum capricornutum), aquatic invertebrate (Daphnia magna) or fish (Oryzias latipes) are greater than its water solubility (0.016 mg/L). The NOEC in a 21-day reproduction test with Daphnia magna is also greater than its water solubility. No significant effects are observed in any tests conducted at extremely high concentrations by using dispersant under OECD test guidelines [TG201, 202, 203, 204, or 211]. There is information that some fatty acids with shorter carbon chain caused no mortality at saturated concentration in certain aquatic organisms (gammarus in freshwater; Medaka in seawater condition). Considering from these data and additional information, it is reasonable to assume that docosanoic acid is not toxic to aquatic organisms at the concentration less than its water solubility (0.016 mg/L). A PNEC is not calculated since NOEC values obtained are above the water solubility of the substance.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

behenic 酸在洗涤的猪血小板上的血小板聚集作用通过添加钙离子得到了增强。亚油酸在等摩尔浓度下与behenic 酸共同添加时，完全抑制了behenic 酸的效果。

THE BLOOD PLATELET AGGREGATING EFFECT OF BEHENIC ACID ON WASHED PIG BLOOD PLATELETS WAS ENHANCED BY THE ADDITION OF CALCIUM IONS. LINOLENIC ACID COMPLETELY INHIBITED THE EFFECT OF BEHENIC ACID WHEN BOTH WERE ADDED IN EQUIMOLAR CONCENTRATIONS.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 紧急急救：确保已经进行了充分的中和。如果患者停止呼吸，请开始人工呼吸，最好使用需求阀复苏器、袋阀面罩装置或口袋面罩，按训练进行操作。根据需要进行心肺复苏。立即用缓慢流动的水冲洗受污染的眼睛。不要催吐。如果发生呕吐，让患者前倾或将其置于左侧（如果可能的话，头部向下），以保持呼吸道畅通，防止吸入。保持患者安静，维持正常体温。寻求医疗帮助。 /有机酸及相关化合物/

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand-valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Organic acids and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 基本治疗：建立专利气道（如有需要，使用口咽或鼻咽气道）。如有必要，进行吸痰。观察呼吸不足的迹象，如有必要，辅助呼吸。通过非循环呼吸面罩以10至15升/分钟的速度给予氧气。监测肺水肿，如有必要，进行治疗……。监测休克，如有必要，进行治疗……。对于眼睛污染，立即用水冲洗眼睛。在运输过程中，用0.9%的生理盐水（NS）连续冲洗每只眼睛……。不要使用催吐剂。对于摄入，如果患者能吞咽、有强烈的呕吐反射且不流口水，则用水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释。活性炭无效……。不要尝试中和，因为可能会发生放热反应。在去污后，用干燥、无菌的敷料覆盖皮肤烧伤……。/有机酸及其相关化合物/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist respirations if necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool. Activated charcoal is not effective ... . Do not attempt to neutralize because of exothermic reaction. Cover skin burns with dry, sterile dressings after decontamination ... . /Organic acids and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 高级治疗：对于无意识、严重肺水肿或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。在上呼吸道阻塞的最初迹象出现时，可能需要尽早进行插管。使用气囊面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿……。对于严重的支气管痉挛，考虑给予β受体激动剂，如沙丁胺醇……。监测心率和必要时治疗心律失常……。开始静脉输注5%葡萄糖水（D5W）/SRP: "保持开放"，最小流量/。如果出现低血容量的迹象，使用0.9%盐水（NS）或乳酸钠林格液（LR）。对于伴有低血容量迹象的低血压，谨慎给予液体。如果病人在正常血容量时低血压，考虑使用血管加压药。注意观察液体过载的迹象……。使用丙美卡因盐酸协助眼部冲洗……。/有机酸及相关化合物/

/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Early intubation, at the first sign of upper airway obstruction, may be necessary. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Consider vasopressors if patient is hypotensive with a normal fluid volume. Watch for signs of fluid overload ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Organic acids and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• TSCA：
  Yes
• 安全说明：
  S24/25,S26,S36/37/39
• 危险类别码：
  R36/37/38
• WGK Germany：
  -
• 海关编码：
  2915900090
• 危险品运输编号：
  NONH for all modes of transport
• 危险类别：
  6.1
• 包装等级：
  II
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335
• 储存条件：
  1. 储存于阴凉、干燥、通风良好的库房，远离火种和热源，避免阳光直射。包装需密封，防止受潮。应与氧化剂、还原剂及强碱分开存放，严禁混储。 2. 配备相应品种和数量的消防器材，并在储区准备泄漏应急处理设备和合适的收容材料。

SDS

Name:	Docosanoic Acid Tech. 85% Material Safety Data Sheet
Synonym:	Behenic Acid
CAS:	112-85-6

Section 1 - Chemical Product MSDS Name:Docosanoic Acid Tech. 85% Material Safety Data Sheet
Synonym:Behenic Acid

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Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS

CAS#	Chemical Name	content	EINECS#
112-85-6	Docosanoic Acid	85%	204-010-8

Hazard Symbols: None Listed.
Risk Phrases: None Listed.

---

Section 3 - HAZARDS IDENTIFICATION
EMERGENCY OVERVIEW
The toxicological properties of this material have not been fully investigated.
Potential Health Effects
Eye:
May cause eye irritation.
Skin:
May cause skin irritation.
Ingestion:
May cause irritation of the digestive tract. The toxicological properties of this substance have not been fully investigated.
Inhalation:
May cause respiratory tract irritation. The toxicological properties of this substance have not been fully investigated.
Chronic:
No information found.

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Section 4 - FIRST AID MEASURES
Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid.
Skin:
Get medical aid. Flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes. Wash clothing before reuse.
Ingestion:
Never give anything by mouth to an unconscious person. Get medical aid. Do NOT induce vomiting. If conscious and alert, rinse mouth and drink 2-4 cupfuls of milk or water.
Inhalation:
Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical aid.
Notes to Physician:

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Section 5 - FIRE FIGHTING MEASURES
General Information:
As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion.
Extinguishing Media:
Use agent most appropriate to extinguish fire. Use water spray, dry chemical, carbon dioxide, or appropriate foam.

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Section 6 - ACCIDENTAL RELEASE MEASURES
General Information: Use proper personal protective equipment as indicated in Section 8.
Spills/Leaks:
Clean up spills immediately, observing precautions in the Protective Equipment section. Sweep up, then place into a suitable container for disposal. Avoid generating dusty conditions. Provide ventilation.

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Section 7 - HANDLING and STORAGE
Handling:
Wash thoroughly after handling. Remove contaminated clothing and wash before reuse. Use with adequate ventilation. Minimize dust generation and accumulation. Avoid contact with eyes, skin, and clothing. Keep container tightly closed. Avoid ingestion and inhalation.
Storage:
Store in a tightly closed container. Store in a cool, dry, well-ventilated area away from incompatible substances.

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Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION
Engineering Controls:
Facilities storing or utilizing this material should be equipped with an eyewash facility and a safety shower. Use adequate ventilation to keep airborne concentrations low.
Exposure Limits CAS# 112-85-6: Personal Protective Equipment Eyes: Wear appropriate protective eyeglasses or chemical safety goggles as described by OSHA's eye and face protection regulations in 29 CFR 1910.133 or European Standard EN166.
Skin:
Wear appropriate protective gloves to prevent skin exposure.
Clothing:
Wear appropriate protective clothing to prevent skin exposure.
Respirators:
A respiratory protection program that meets OSHA's 29 CFR 1910.134 and ANSI Z88.2 requirements or European Standard EN 149 must be followed whenever workplace conditions warrant respirator use.

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Section 9 - PHYSICAL AND CHEMICAL PROPERTIES

Physical State: Powder
Color: white
Odor: None reported.
pH: Not available.
Vapor Pressure: Not available.
Viscosity: Not available.
Boiling Point: 306 deg C @ 60.00mmHg
Freezing/Melting Point: 80.00 - 82.00 deg C
Autoignition Temperature: Not applicable.
Flash Point: Not applicable.
Explosion Limits, lower: Not available.
Explosion Limits, upper: Not available.
Decomposition Temperature:
Solubility in water:
Specific Gravity/Density:
Molecular Formula: C22H44O2
Molecular Weight: 340.58

---

Section 10 - STABILITY AND REACTIVITY
Chemical Stability:
Stable under normal temperatures and pressures.
Conditions to Avoid:
Incompatible materials, dust generation, excess heat, strong oxidants.
Incompatibilities with Other Materials:
Oxidizing agents.
Hazardous Decomposition Products:
Carbon monoxide, irritating and toxic fumes and gases, carbon dioxide.
Hazardous Polymerization: Has not been reported.

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Section 11 - TOXICOLOGICAL INFORMATION
RTECS#:
CAS# 112-85-6 unlisted.
LD50/LC50:
Not available.
Carcinogenicity:
Docosanoic Acid - Not listed by ACGIH, IARC, or NTP.

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Section 12 - ECOLOGICAL INFORMATION

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Section 13 - DISPOSAL CONSIDERATIONS
Dispose of in a manner consistent with federal, state, and local regulations.

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Section 14 - TRANSPORT INFORMATION

IATA
No information available.
IMO
No information available.
RID/ADR
No information available.

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Section 15 - REGULATORY INFORMATION

European/International Regulations
European Labeling in Accordance with EC Directives
Hazard Symbols: Not available.
Risk Phrases:
Safety Phrases:
S 24/25 Avoid contact with skin and eyes.
S 28A After contact with skin, wash immediately with
plenty of water.
S 37 Wear suitable gloves.
S 45 In case of accident or if you feel unwell, seek
medical advice immediately (show the label where
possible).
WGK (Water Danger/Protection)
CAS# 112-85-6: 0
Canada
CAS# 112-85-6 is listed on Canada's DSL List.
CAS# 112-85-6 is not listed on Canada's Ingredient Disclosure List.
US FEDERAL
TSCA
CAS# 112-85-6 is listed on the TSCA inventory.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

理化性质

无色针状结晶或蜡状固体，不溶于水，难溶于甲醇。以甘油酯形式存在于硬化菜油和硬化鱼油中，在花生油、菜籽油及芥籽油中亦有少量存在。

山嵛酸

山嵛酸又称为二十二酸，是通过将芥酸分子中的双键进行氢化得到的一种饱和的直链二十二碳酸。其独特的性质在众多行业中均有广泛应用，如制造山萮醇、山萮酸酯及山萮酸酰胺等产品。此外，其衍生物在塑料工业、金属制造工业、食品工业、医药工业和化妆品工业中亦有广泛应用。

作为医药杀真菌剂、农业杀虫剂以及化妆品添加剂，山嵛酸还可用作纺织整理柔软剂。其银盐可制成热显影性感光材料“干银纸”，铵盐则具有防腐作用，能防止藻类附着于舰艇上。

制备方法

二十二酸可通过多种方式制备，最常用的方法是从乳木果油和棕榈仁油中提取。其主要步骤分为两个部分：首先，通过精炼和加氢处理去除杂质；然后，利用蒸馏或萃取等方法提纯原料。第二步主要是采用真空蒸馏和结晶技术进一步纯化已提取的二十二酸。

生物活性

Docosanoic acid 是一种较难被人体吸收的饱和脂肪酸，能够提高人类体内的胆固醇水平。

靶点

• Human Endogenous Metabolite（人类内源性代谢产物）

用途

• 用作有机合成原料。
• 制造山嵛醇、山嵛酸酯及山嵛酸酰胺等产品，在纺织、石油、洗涤剂和化妆品等行业有广泛的应用。
• 用于制造类似产品的衍生物，包括增塑剂和稳定剂。

反应信息

• 作为反应物：
  描述：

  二十二酸 在 sodium tetrahydroborate 、 碘 作用下， 以 四氢呋喃 为溶剂， 以87.6%的产率得到二十二烷-1-醇
  参考文献：
  名称：

  [EN] A PROCESS FOR THE PREPARATION OF DOCOSANOL
  [FR] PROCÉDÉ DE PRÉPARATION DE DOCOSANOL

  摘要：

  本发明提供了一种制备十二烷醇（I）的方法。该方法包括将顺式-13-十二烯酸（V）还原以获得十二酸（III），进而将其进一步还原以获得十二烷醇（I）。

  公开号：

  WO2018220504A1
• 作为产物：
  描述：

  十六醛 在 palladium on activated charcoal 正丁基锂 、 氢气 作用下， 以 甲醇 为溶剂， 反应 6.75h， 生成 二十二酸
  参考文献：
  名称：

  Deshmukh; Veeresh, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1996, vol. 35, # 12, p. 1239 - 1241

  摘要：

  DOI：
• 作为试剂：
  描述：

  1H-1,2,4-三唑 、 iron(II) perchlorate hexahydrate 、 sodium docusate 在 二十二酸 、 维生素 C 作用下， 以 正辛烷 、 乙醇 、 水 为溶剂， 反应 4.0h， 生成
  参考文献：
  名称：

  Thin films of spin-crossover coordination polymers with large thermal hysteresis loops prepared by nanoparticle spin coating

  摘要：

  自旋交替纳米颗粒在衬底上形成均匀的薄膜，这些薄膜表现出具有大热滞回环的突然自旋转变。

  DOI：

  10.1039/c4cc04123b

文献信息

• [EN] AGENTS AND METHODS FOR TREATING DYSPROLIFERATIVE DISEASES<br/>[FR] AGENTS ET MÉTHODES POUR TRAITER DES MALADIES DYSPROLIFÉRATIVES
  申请人：MEMORIAL SLOAN KETTERING CANCER CENTER

  公开号：WO2019161345A1

  公开（公告）日：2019-08-22

  Compounds are described with the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and n are defined as anywhere herein, which are useful for the treatment of cancer and other dysproliferative diseases.

  化合物的一般公式为（I），其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R10、R11、R12和n的定义如本文的任何地方所述，这些化合物对于治疗癌症和其他增生异常疾病是有用的。
• Method of producing aliphatic nitrile
  申请人：Terasaka Michio

  公开号：US20050059836A1

  公开（公告）日：2005-03-17

  The present invention relates to a method of producing an aliphatic nitrile by reacting an aliphatic carboxylic acid, by reacting an aliphatic dicarboxylic acid or their alkyl esters (the alkyl group with 1 to 5 carbon atoms) with ammonia in the presence of a catalyst of titanium oxide supported on solid silica. In addition, the present invention relates to a method of producing an aliphatic amine, including hydrogenating the aliphatic nitrile by using a hydrogenating catalyst and a catalyst for producing an aliphatic nitrile.

  本发明涉及一种通过在固体二氧化硅上支撑的钛氧化物催化剂存在下，通过将脂肪族羧酸与氨反应，或者通过将脂肪族二羧酸或其烷基酯（烷基基团含有1至5个碳原子）与氨在催化剂存在下反应来生产脂肪族腈的方法。此外，本发明涉及一种生产脂肪族胺的方法，包括使用氢化催化剂和用于生产脂肪族腈的催化剂对脂肪族腈进行氢化。
• Bna Conjugates and Methods of Use
  申请人：James Kenneth D.

  公开号：US20080207505A1

  公开（公告）日：2008-08-28

  Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, decreasing arterial blood pressure and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the hBNP compound are also disclosed, having an amino acid sequence that is other than the native sequence.

  本发明公开了改性利钠肽化合物及其共轭物。具体而言，提供了至少连接有一个修饰基团的hBNP的共轭形式。这些改性利钠肽化合物共轭物保留了刺激cGMP产生、结合NPR-A受体、降低动脉血压以及在某些实施例中相对于未经改性的对应利钠肽化合物具有改善的循环半衰期的活性。这些化合物和共轭物的口服、静脉注射、肠内、皮下、肺部和静脉形式可作为治疗和/或治疗心脏病症，特别是充血性心力衰竭的治疗。还公开了包含具有各种长度和构型的寡聚结构的修饰基团。此外，还公开了hBNP化合物的类似物，其氨基酸序列与天然序列不同。
• Pharmaceutical compositions of drug-oligomer conjugates and methods of treating diseases therewith
  申请人：——

  公开号：US20030069170A1

  公开（公告）日：2003-04-10

  Pharmaceutical compositions that include a drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating diseases in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.

  描述了包括药物-寡聚物共轭物、脂肪酸成分和胆盐成分的药物组合物。药物以共价键连接到寡聚物基团上。脂肪酸成分和胆盐成分以1:5至5:1的重量比存在。还提供了利用这种药物组合物治疗需要此类治疗的受试者的方法，以及提供这种药物组合物的方法。
• Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
  申请人：——

  公开号：US20030229009A1

  公开（公告）日：2003-12-11

  Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.

  描述了合成前胰岛素多肽的方法，包括将包括胰岛素多肽和一个或多个肽段的前胰岛素多肽与一个寡聚体接触，这些肽段通过肽键结合，可以被切割以产生胰岛素多肽，条件足以将寡聚体与前胰岛素多肽的胰岛素多肽部分结合并提供前胰岛素多肽-寡聚体共轭物，并从前胰岛素多肽-寡聚体共轭物中切割一个或多个肽段，以提供胰岛素多肽-寡聚体共轭物。还提供了合成前胰岛素多肽-寡聚体共轭物的方法，以及前胰岛素多肽-寡聚体共轭物。还提供了合成C肽多肽-寡聚体共轭物和其他前多肽-寡聚体共轭物的方法。

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