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bestASONe | 356-12-7

中文名称
——
中文别名
——
英文名称
bestASONe
英文别名
StraderM;vanos;Topsyn;[2-(12,19-difluoro-11-hydroxy-6,6,9,13-tetramethyl-16-oxo-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-8-yl)-2-oxoethyl] acetate
bestASONe化学式
CAS
356-12-7
化学式
C26H32F2O7
mdl
——
分子量
494.533
InChiKey
WJOHZNCJWYWUJD-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

物化性质

  • 熔点:
    309 °C
  • 比旋光度:
    D +83° (chloroform)
  • 沸点:
    235°C (rough estimate)
  • 密度:
    1.2001 (estimate)
  • 溶解度:
    二甲基亚砜:≥19mg/mL

计算性质

  • 辛醇/水分配系数(LogP):
    3.2
  • 重原子数:
    35
  • 可旋转键数:
    4
  • 环数:
    5.0
  • sp3杂化的碳原子比例:
    0.73
  • 拓扑面积:
    99.1
  • 氢给体数:
    1
  • 氢受体数:
    9

ADMET

毒理性
  • 在妊娠和哺乳期间的影响
◉ 母乳喂养期间使用概述:轻松在母乳喂养期间尚未进行研究。由于只有大量使用最强效的皮质类固醇才可能在母亲体内产生系统性影响,因此短期使用外用皮质类固醇不太可能通过进入母乳而对哺乳婴儿构成风险。然而,最好还是使用最弱效的药物,并尽可能在最小的皮肤区域使用。特别是要确保婴儿的皮肤不直接接触涂抹了药物的区域。只有在乳头或乳晕上使用低效皮质类固醇,因为婴儿可能会直接从皮肤上摄取药物;应避免在乳头上使用轻松。应使用溶性乳膏或凝胶产品涂抹乳房,因为软膏可能会使婴儿通过舔舐接触到高平的矿物石蜡。如果外用皮质类固醇应用于乳房或乳头区域,应在哺乳前彻底擦除。 ◉ 对哺乳婴儿的影响:将相对高矿皮质激素活性的皮质类固醇异氟泼尼松醋酸酯)涂在母亲的乳头上,导致她两个月大的哺乳婴儿出现QT间期延长、库欣综合症外貌、严重高血压、生长减缓和电解质异常。这位母亲从婴儿出生起就因为乳头疼痛而使用该乳膏。 ◉ 对泌乳和母乳的影响:截至修订日期,未找到相关的已发布信息。
◉ Summary of Use during Lactation:Fluocinonide has not been studied during breastfeeding. Since only extensive application of the most potent corticosteroids may cause systemic effects in the mother, it is unlikely that short-term application of topical corticosteroids would pose a risk to the breastfed infant by passage into breastmilk. However, it would be prudent to use the least potent drug on the smallest area of skin possible. It is particularly important to ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated. Only the lower potency corticosteroids should be used on the nipple or areola where the infant could directly ingest the drugs from the skin; fluocinonide should be avoided on the nipple. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking. Any topical corticosteroid should be wiped off thoroughly prior to nursing if it is being applied to the breast or nipple area. ◉ Effects in Breastfed Infants:Topical application of a corticosteroid with relatively high mineralocorticoid activity (isofluprednone acetate) to the mother's nipples resulted in prolonged QT interval, cushingoid appearance, severe hypertension, decreased growth and electrolyte abnormalities in her 2-month-old breastfed infant. The mother had used the cream since birth for painful nipples. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
来源:Drugs and Lactation Database (LactMed)

安全信息

  • 危险等级:
    6.1(a)
  • 危险品标志:
    T+
  • 安全说明:
    S22,S25,S28,S36/37/39,S45
  • 危险类别码:
    R28
  • WGK Germany:
    3
  • 海关编码:
    2937210000
  • 危险品运输编号:
    UN 2811 6.1/PG 2
  • 包装等级:
    I
  • 危险类别:
    6.1(a)
  • 储存条件:
    | 室温 |

SDS

SDS:0bca9e969e3d280d5277a65ee7f816a3
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Section 1. Chemical Product and Company Identification
Fluocinonide
Common Name/
Trade Name
Fluocinonide

Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at
least 15 minutes. Get medical attention.
Skin Contact In case of contact, immediately flush skin with plenty of water. Cover the irritated skin with an emollient. Remove
contaminated clothing and shoes. Wash clothing before reuse. Thoroughly clean shoes before reuse. Get
medical attention.
Serious Skin Contact Wash with a disinfectant soap and cover the contaminated skin with an anti-bacterial cream. Seek immediate
medical attention.
Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get
medical attention.
Serious Inhalation Evacuate the victim to a safe area as soon as possible. Loosen tight clothing such as a collar, tie, belt or
waistband. Seek medical attention.
Ingestion If swallowed, do not induce vomiting unless directed to do so by medical personnel. Never give anything by
mouth to an unconscious person. Loosen tight clothing such as a collar, tie, belt or waistband. Get medical
attention immediately.
Serious Ingestion Not available.

Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Flash Points Not available.
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), halogenated compounds.
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances Non-flammable in presence of shocks.
Explosion Hazards in Presence Slightly explosive in presence of open flames and sparks.
of Various Substances Non-explosive in presence of shocks.
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Special Remarks on When heated to decomposition it emits toxic fumes. As with most organic solids, fire is possible at elevated
Fire Hazards temperatures
Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presences of an ignition source is a potential dust
Hazards explosion hazard.

Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container.
Large Spill Poisonous solid.
Stop leak if without risk. Do not get water inside container. Do not touch spilled material. Use water spray to
reduce vapors. Prevent entry into sewers, basements or confined areas; dike if needed. Eliminate all ignition
Fluocinonide

Section 7. Handling and Storage
Precautions Keep locked up.. Keep away from heat. Keep away from sources of ignition. Do not ingest. Do not breathe
dust. Wear suitable protective clothing. In case of insufficient ventilation, wear suitable respiratory equipment. If
ingested, seek medical advice immediately and show the container or the label. Avoid contact with skin and eyes.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area.

Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to
airborne contaminants below the exposure limit.
Personal Protection Splash goggles. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent.
Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used
a Large Spill to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist
BEFORE handling this product.
Exposure Limits Not available.

Section 9. Physical and Chemical Properties
Physical state and appearance Solid. (Powdered solid.) Odor Not available.
Taste Not available.
Molecular Weight 494.54 g/mole
Color White.
pH (1% soln/water) Not applicable.
Not available.
Boiling Point
Melting Point 300°C (572°F)
Not available.
Critical Temperature
Specific Gravity Not available.
Vapor Pressure Not applicable.
Vapor Density Not available.
Volatility Not available.
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Ionicity (in Water) Not available.
Dispersion Properties Not available.
Solubility Insoluble in cold water, hot water.
Soluble in ethanol

Section 10. Stability and Reactivity Data
Stability The product is stable.
Not available.
Instability Temperature
Conditions of Instability Excess heat, dust generation
Incompatibility with various Not available.
substances
Corrosivity Non-corrosive in presence of glass.
Fluocinonide
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization Will not occur.

Section 11. Toxicological Information
Routes of Entry Absorbed through skin. Dermal contact. Inhalation. Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): 14 mg/kg [Rat].
Chronic Effects on Humans Not available.
Other Toxic Effects on Very hazardous in case of ingestion.
Humans Hazardous in case of skin contact (irritant, permeator), of inhalation.
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on May cause adverse reproductive effects.
Chronic Effects on Humans May affect genetic material (mutagenic)
Special Remarks on other Potential Health Effects:
Toxic Effects on Humans Skin: Skin contact may cause skin irritation witn burning, itching, dryness, Folliculitis, Hypertrichosis, acneform
eruptions, Hypopigmentation, Perioral dermatitis. May also cause allergic contact dermatitis, skin atrophy (loss of
skin collegan), maceration of the skin, secondary infection, Striae, Miliaria. Topical corticosteroids can be
absorbed through the skin in sufficient amounts to produce systemic effects (see ingestion)
Eyes: May cause eye irritaiton, corneal ulcers and visual disturbances
Inhalation: May be harmful if inhaled. It may be irritating to the mucous membranes and upper respiratory tract.
Ingestion: May be fatal if swallowed. It may affect blood (changes is leukocyte count, changes in bone marrow),
and metabolism (weight loss), cardiovascular system (hypertension, cardiac failure). It may also cause edema
Note: Systemic absorption of topical corticosteroids has produced reversible hypothalmic-pituitary-adrenal (HPA)
axid supression, manifestations of Cushing's syndrome, hyperglycemia, and glucosuria in some individuals.

Section 12. Ecological Information
Ecotoxicity Not available.
BOD5 and COD Not available.
Possibly hazardous short term degradation products are not likely. However, long term degradation products may
Products of Biodegradation
arise.
The products of degradation are as toxic as the product itself.
Toxicity of the Products
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation

Section 13. Disposal Considerations
Waste Disposal Waste must be disposed of in accordance with federal, state and local environmental
control regulations.
Fluocinonide

Section 14. Transport Information
DOT Classification CLASS 6.1: Poisonous material.
Identification : Toxic solid, organic, n.o.s. (Fluocinonide) UNNA: 2811 PG: II
Not available.
Special Provisions for
Transport
DOT (Pictograms)

Section 15. Other Regulatory Information and Pictograms
No products were found.
Federal and State
Regulations
California
Proposition 65
Warnings
Other Regulations OSHA: Hazardous by definition of Hazard Communication Standard (29 CFR 1910.1200).
EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances.
WHMIS (Canada) Not controlled under WHMIS (Canada).
Other Classifications
DSCL (EEC) R28- Very toxic if swallowed. S22- Do not breathe dust.
R63- Possible risk of harm to the S25- Avoid contact with eyes.
unborn child. S36/37/39- Wear suitable protective clothing,
gloves and eye/face protection.
S45- In case of accident or if you feel unwell,
seek medical advice immediately (show the
label where possible).
Health Hazard
HMIS (U.S.A.) 2 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
2 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
Fluocinonide
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.


SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

醋酸氟轻松简介

醋酸氟轻松又名轻松醋酸酯化学名称为6α,9α-二-11β,21-二羟基-16α,17α-[(1-甲基亚乙基)双氧]孕甾-1,4-二烯-3,20-二酮-21-醋酸酯。作为临床常用的强效外用抗炎糖皮质激素药物,广泛应用于各种皮炎、湿疹、牛皮癣、红斑狼疮、扁平苔藓及骨性关节炎等疾病的治疗。

作用与用途

本品为含的糖皮质激素,局部外用时可使真皮毛细血管收缩。通过抑制DNA合成影响细胞代谢,从而抑制表皮细胞的增殖或再生;亦能抑制结缔组织内纤维细胞的新生成和色素细胞的生成。还能稳定细胞内溶酶体膜,防止组胺释放引起的组织损伤,易于从皮肤吸收。具有抗炎、止痒、抗增生及免疫抑制作用。

外用后的吸收与代谢

外用后可经完整皮肤吸收,吸收程度受制剂基质、病肤的病理情况以及是否封包用药等因素影响。吸收后与血浆蛋白结合,并主要在肝脏代谢,通过肾脏排泄。

适用范围

适用于接触性皮炎、过敏性皮炎、脂溢性皮炎、神经性皮炎、日光性皮炎、湿疹、屑病、扁平苔癣及皮肤瘙痒症等。

用法与用量

局部外用:使用0.025%软膏或乳膏均匀涂抹于患处,每日2~3次。一周总量不超过12.5mg。封包治疗仅适用于慢性肥厚或掌跖部位的皮损。

不良反应

长期或大面积应用,尤其是采用封闭疗法时可能因吸收而引起全身不良反应,包括库欣综合征、高血糖症和糖尿病等。此外,还可能导致皮肤萎缩、毛细血管扩张、痤疮样皮炎、口周皮炎、毛囊炎及诱发或加重感染性皮肤病。

注意事项
  1. 对本品过敏者以及结核性、病毒性、真菌性和细菌性皮肤疾病患者禁用。
  2. 孕妇和哺乳期妇女应慎用,婴儿也应慎用。
  3. 皮肤并发细菌感染者需并用抗菌药物。
  4. 不宜用于大面积破损皮肤或长期大面积使用,以免吸收中毒。
  5. 长期每日多次涂抹可导致耐药性,建议适当间歇用药。
化学性质

白色或类白色的结晶性粉末。熔点为308-311℃。易溶于丙酮,略溶于乙醇,不溶于,无臭,无味。

用途

主要用于治疗过敏性皮炎、湿疹等疾病。

文献信息

  • CORTICOSTEROID CONJUGATES AND USES THEREOF
    申请人:Teicher Martin H.
    公开号:US20100056488A1
    公开(公告)日:2010-03-04
    The invention features corticosteroids conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage, the resulting conjugate is a peripherally acting steroid with reduced activity in the central nervous system. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a corticosteroid conjugate.
  • Oligomer-Corticosteroid Conjugates
    申请人:Zhang Wen
    公开号:US20100286107A1
    公开(公告)日:2010-11-11
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
  • OLIGOMER-CORTICOSTEROID CONJUGATES
    申请人:NAKTAR THERAPEUTICS
    公开号:US20140309398A1
    公开(公告)日:2014-10-16
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits different properties compared to the properties of the corticosteroid not attached to the water-soluble oligomer.
  • US8796248B2
    申请人:——
    公开号:US8796248B2
    公开(公告)日:2014-08-05
  • [EN] OLIGOMER-CORTICOSTEROID CONJUGATES<br/>[FR] CONJUGUÉS D'OLIGOMÈRES ET CORTICOSTÉROÏDES
    申请人:NEKTAR THERAPEUTICS AL CORP
    公开号:WO2009045539A2
    公开(公告)日:2009-04-09
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
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