sodium ascorbate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氢呋喃
• 英文名称: sodium ascorbate
• 英文别名: (+)-sodium L-ascorbate；vitamin C sodium salt；L-ascorbic acid sodium salt；vitamin C；sodium (R)-2-((S)-1,2-dihydroxyethyl)-4-hydroxy-5-oxo-2,5-dihydrofuran-3-olate；L-ascorbic acid sodium；L-sodium ascorbate；Na ascorbate；NaAsc；sodium (2R)-2-[(1S)-1,2-dihydroxyethyl]-4-hydroxy-5-oxo-2H-furan-3-olate；ascorbic acid sodium salt；ascorbate sodium；vitamin C sodium；Na-L-ascorbate；(+)-sodium 1-ascorbate；ascorbic acid sodium；sodium ascorbic acid；sodium vitamin C；VcNa；sodium (2R)-2-[(1S)-1,2-dihydroxyethyl]-4-hydroxy-5-oxo-2,5-dihydrofuran-3-olate；(2R)-2-[(1S)-1,2-dihydroxyethyl]-4-hydroxy-5-oxo-2H-furan-3-olate；sodium ascorbate powder；L-ascorbic sodium salt；sodium L-ascorbic acid；ascorbic sodium；sodium ascobate；ascorbic acid；sodium;(2R)-2-[(1S)-1,2-dihydroxyethyl]-3-hydroxy-5-oxo-2H-furan-4-olate
• 化学式: C₆H₇O₆*Na
• 分子量: 198.108
• InChiKey: PPASLZSBLFJQEF-RXSVEWSESA-M

计算性质

• 辛醇/水分配系数(LogP)：
  -5.6
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  110
• 氢给体数：
  3
• 氢受体数：
  6

ADMET

代谢

肾上腺皮质与抗坏血酸代谢密切相关...据报道，氢化可的松能够刺激从葡萄糖酸内酯合成抗坏血酸，但是去氧皮质酮或醛固酮在正常或肾上腺切除的大鼠中会导致抗坏血酸排泄增加...

... Adrenal cortex is closely associated with ascorbate metabolism ... Hydrocortisone was reported ... to stimulate synthesis of ascorbate from gluconolactone, but deoxycorticosterone or aldosterone caused ... increase in ascorbate excretion in normal or adrenalectomized rats...

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

暴露于烟酸抗坏血酸的肌肉组织在添加了不同浓度氯化钙的无钙离子但含有乙酰胆碱的浴液中反应比未处理的肌肉更为强烈。

Tissues exposed to Na ascorbate responded more vigorously than untreated muscles when graded concentrations of calcium chloride added to bathing solution minus Ca2+ ions but with acetylcholine.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

研究了维生素C钠（含或不含维生素K3）在体外使用培养的人肿瘤细胞系MCF-7（乳腺癌）、KB（口腔表皮癌）和AN3-CA（子宫内膜腺癌）的效应，浓度范围为0.198微克/毫升至1.98毫克/毫升。以不含维生素C钠和维生素的培养介质作为对照。在细胞生长至50%汇合时，将不同组合的维生素C钠和维生素K3加入培养物中进行1小时孵育。进行了DNA含量的测定。只有在高浓度（5 x 10^3摩尔/升）下，补充维生素C钠的培养基才具有生长抑制作用。联合给药在浓度低10至50倍的情况下显示出对细胞生长的协同抑制作用。这些结果适用于所有三种细胞类型...

The effects of sodium ascorbate with or without Vitamin K3 was studied in vitro using cultured human neoplastic cell lines MCF-7 (breast carcinoma), KB (oral epidermal carcinoma), and AN3-CA (endometrial adenocarcinoma) at concentrations of 0.198 ug/mL to 1.98 mg/mL. Culture media without sodium ascorbate and the vitamin were used as a control. At 50%confluence, different combinations of sodium ascorbate and Vitamin K3 were added to the cultures for a 1 hr incubation. DNA determinations were made. Sodium Ascorbate supplemented media had a growth inhibiting action only at high concentrations (5 x 10+3 mol/L). Combined administration demonstrated a synergisitic inhibition of cell growth at 10 to 50 times lower concentrations. These results are for all three cell types ...

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

将异抗坏血酸钠和/或亚硝酸钠给予雄性和雌性Wistar大鼠（每组5只大鼠）6个月。对照组仅喂基础饮食和水。处理组给予以下物质：0.075%，0.15%或0.3%的亚硝酸钠溶于水；1%，2%或4%的异抗坏血酸钠；或者两种化学品以低+低、中+中、高+高剂量组合。联合高剂量组的体重增加显著减少。联合高剂量组还显著降低了血清总蛋白，增加了血尿素氮（BUN）和相对肾脏重量。组织病理学检查显示，联合高剂量组的食道中至重度鳞状细胞增生，联合中剂量组轻度增生。性别之间没有差异。最小毒性剂量为0.15%亚硝酸钠+2%异抗坏血酸钠...

Sodium ascorbate and/or sodium nitrite /was administered/ for 6 months to male and female Wistar rats (5 rats/group). The control group was fed a basal diet and water only. Treated groups were administered the following: 0.075%, 0.15%, or 0.3% sodium nitrite dissolved in water; 1%, 2%, or 4% sodium ascorbate; or a combination with both chemicals at low + low, middle + middle, and high + high doses. Body weight gain was significantly decreased in the combined-high dose group. Significant decreases of serum total protein, increase of BUN (blood urea nitrogen) and relative kidney weight were also found in the combined-high dose group. Histopathological examination showed moderate or severe squamous cell hyperplasia of the forestomach in the combined-high dose group and slight hyperplasia in the combined-middle dose group. No differences were seen between the sexes. The minimum toxic dose was 0.15% sodium nitrite+2% sodium ascorbate ...

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 立即急救：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、球囊阀面罩设备或口袋面罩，按训练操作。如有必要，执行心肺复苏。立即用缓慢流动的水冲洗受污染的眼睛。不要催吐。如果患者呕吐，让患者向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。 /毒物A和B/

/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 if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the 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. /Poisons A and B/

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，如有需要，辅助通气。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……。预防癫痫发作，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）持续冲洗每只眼睛……。不要使用催吐剂。对于摄入，如果患者能吞咽、有强烈的干呕反射且不流口水，则用温水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释……。在去污后，用干燥的无菌敷料覆盖皮肤烧伤……。/毒药A和B/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. 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 ... . Anticipate seizures 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 ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

维生素C的还原形式，即抗坏血酸，具有强大的抗氧化作用，同时也参与细胞分化。抗坏血酸通过特定的钠/抗坏血酸共转运蛋白SVCT1和SVCT2被哺乳动物细胞摄取。尽管骨骼肌含有大约全身50%的维生素C，但SVCT转运蛋白在这种组织中的表达尚未被明确研究。...这项工作...使用小鸡作为模型系统分析了SVCT2在胚胎肌发生过程中的表达模式。...免疫组织化学分析显示，SVCT2在小鸡肌发生过程中的I型慢肌纤维以及包括人类在内的几种物种的出生后骨骼肌中优先表达...

Ascorbic acid, the reduced form of vitamin C, functions as a potent antioxidant as well as in cell differentiation. Ascorbate is taken up by mammalian cells through the specific sodium/ascorbate co-transporters SVCT1 and SVCT2. Although skeletal muscle contains about 50% of the whole-body vitamin C, the expression of SVCT transporters has not been clearly addressed in this tissue. ... This work ... analyzed the expression pattern of SVCT2 during embryonic myogenesis using the chick as model system. ... Immunohistochemical analyses showed that SVCT2 is preferentially expressed by type I slow-twitch muscle fibers throughout chick myogenesis as well as in post-natal skeletal muscles of several species, including human...

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

人类使用两种钠-抗坏血酸共转运蛋白（hSVCT1和hSVCT2）来转运饮食中必需的微量营养素抗坏血酸，即维生素C的还原活性形式。尽管人类肝脏在调节和维护维生素C稳态方面起着关键作用，但维生素C转运生理学以及hSVCT系统在这个器官中的调控尚未得到很好的定义。因此，这项研究使用了一个人类肝细胞系（HepG2），通过原代人类肝细胞确认了某些结果，并确定了抗坏血酸摄取的初始速率取决于Na(+)梯度、pH值，并且作为低微摩尔和高微摩尔浓度范围内浓度的函数是可饱和的。此外，hSVCT2蛋白和mRNA在HepG2细胞和原生人类肝脏中表达水平较高，克隆的hSVCT2启动子在HepG2细胞中具有更高的活性。使用短发夹RNA的结果表明，在HepG2细胞中，降低hSVCT2信息水平比降低hSVCT1信息水平更能减少整体抗坏血酸的摄取过程。PKC细胞内调节途径的激活导致抗坏血酸摄取的下调，这不是由hSVCT1或hSVCT2中单一预测的PKC特异性氨基酸磷酸化位点介导的。然而，PKC激活导致hSVCT1的内部化，而不是hSVCT2。检查其他细胞内调节途径对维生素C摄取的影响，确定了PKA、PTK和Ca(2+)/钙调蛋白也可能参与调节，但不是由一氧化氮依赖途径...

Humans use two sodium-ascorbate cotransporters (hSVCT1 and hSVCT2) for transporting the dietary essential micronutrient ascorbic acid, the reduced and active form of vitamin C. Although the human liver plays a pivotal role in regulating and maintaining vitamin C homeostasis, vitamin C transport physiology and regulation of the hSVCT systems in this organ have not been well defined. Thus, this research used a human hepatic cell line (HepG2), confirming certain results with primary human hepatocytes and determined the initial rate of ascorbic acid uptake to be Na(+) gradient, pH dependent, and saturable as a function of concentration over low and high micromolar ranges. Additionally, hSVCT2 protein and mRNA are expressed at higher levels in HepG2 cells and native human liver, and the cloned hSVCT2 promoter has more activity in HepG2 cells. Results using short interfering RNA suggest that in HepG2 cells, decreasing hSVCT2 message levels reduces the overall ascorbic acid uptake process more than decreasing hSVCT1 message levels. Activation of PKC intracellular regulatory pathways caused a downregulation in ascorbic acid uptake not mediated by a single predicted PKC-specific amino acid phosphorylation site in hSVCT1 or hSVCT2. However, PKC activation causes internalization of hSVCT1 but not hSVCT2. Examination of other intracellular regulatory pathways on ascorbic acid uptake determined that regulation also potentially occurs by PKA, PTK, and Ca(2+)/calmodulin, but not by nitric oxide-dependent pathways...

来源:Hazardous Substances Data Bank (HSDB)

反应信息

• 作为反应物：
  描述：

  sodium ascorbate 在 sodium hydroxide 作用下， 以 甲醇 为溶剂， 生成 维生素 C
  参考文献：
  名称：

  Method for production of stabilized sodium ascorbate powder

  摘要：

  维生素C组合物包含微量的碱金属化合物或碱土金属化合物，对颜色非常稳定，即使长时间储存也不会变黄。这种组合物可以通过添加微量添加剂轻松获得。

  公开号：

  US05120762A1
• 作为产物：
  描述：

  2-氨基-3-氯-1,4-萘醌 生成 sodium ascorbate
  参考文献：
  名称：

  NUCLEIC ACID-POLYMER CONJUGATES FOR BRIGHT FLUORESCENT TAGS

  摘要：

  一种组合物包括具有延伸链、侧链或支链的聚合物。将多个第一链的核酸链中的一个（或多个）连接到多个侧链中的每一个。将与第一链的核酸链互补的多个第二链的核酸链（一个或多个）与多个第一链的核酸链中的每一个形成复合物，以在多个侧链中的每一个形成双链的核酸链。至少一个荧光化合物与多个侧链中的每一个的双链的核酸链相关联。

  公开号：

  US20180142288A1
• 作为试剂：
  描述：

  pleuromutilin 在 N-甲基吗啉 、 sodium azide 、 四丁基溴化铵 、 copper(II) sulfate 、 sodium ascorbate 、 sodium hydroxide 作用下， 以 四氢呋喃 、 二氯甲烷 、 甲基叔丁基醚 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 11.0h， 生成 14-O-[2-((4-(3-aminophenyl-1H-1,2,3-triazol-1-yl)acetamide)-2-methylpropan-2-yl)thioacetyl]mutilin
  参考文献：
  名称：

  10.1016/j.bmcl.2024.129878

  摘要：

  DOI：

  10.1016/j.bmcl.2024.129878

文献信息

• [EN] QUINONE BASED NITRIC OXIDE DONATING COMPOUNDS<br/>[FR] COMPOSÉS DONNEURS D'OXYDE NITRIQUE À BASE DE QUINONE
  申请人：NICOX SA

  公开号：WO2013060673A1

  公开（公告）日：2013-05-02

  The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment of pathological conditions where a deficit of NO plays an important role in their pathogenesis.

  本发明涉及具有喹诚基结构的一氧化氮供体化合物，涉及其制备方法以及它们在治疗病理状况中的应用，其中一氧化氮缺乏在它们的发病机制中起重要作用。
• Synthesis of Novel N-Heterocyclic Compounds Containing 1,2,3-Triazole Ring System via Domino, “Click” and RDA Reactions
  作者：Márta Palkó、Mohamed El Haimer、Zsanett Kormányos、Ferenc Fülöp

  DOI：10.3390/molecules24040772

  日期：——

  synthesized with domino ring closure. A click reaction was performed to create the 1,2,3-triazole heterocyclic ring, followed by an RDA reaction resulting in dihydropyrimido[2,1-a]isoindole-2,6-diones. The absolute configuration, concluded by the norbornene structure that served as a chiral source, remained constant throughout the transformations. The structure of the synthesized compounds was examined by

  已经开发出一种简单、高产的合成路线来构成复杂的杂环，应用多米诺骨牌、点击和逆狄尔斯-阿尔德 (RDA) 反应序列。从 2-氨基甲酰胺开始，合成了一组具有多米诺环闭合的新异吲哚并[2,1-a]喹唑啉酮。进行点击反应以产生 1,2,3-三唑杂环，然后进行 RDA 反应，产生二氢嘧啶并 [2,1-a] 异吲哚-2,6-二酮。由作为手性来源的降冰片烯结构得出的绝对构型在整个转化过程中保持不变。通过 1H 和 13C 核磁共振 (NMR) 方法检查合成化合物的结构。
• [EN] NOVEL HEPCIDIN MIMETICS AND USES THEREOF<br/>[FR] NOUVEAUX MIMÉTIQUES D'HEPCIDINE ET LEURS UTILISATIONS
  申请人：BAYER HEALTHCARE LLC

  公开号：WO2018128828A1

  公开（公告）日：2018-07-12

  The present invention relates to novel peptides acting as hepcidin mimetics, as well as analogues and derivatives thereof. The invention further relates to compositions comprising the peptides of the present invention, and to the use of the peptides in the prophylaxis and treatment of hepcidin-associated disorders, including prophylaxis and treatment of iron overload diseases such as hemochromatosis, iron-loading anemias such as thalassemia, and diseases being associated with ineffective or augmented erythropoiesis, as well as further related conditions and disorders described herein.

  本发明涉及作为赫普西定类似物的新型肽，以及其类似物和衍生物。该发明还涉及包含本发明肽的组合物，以及在预防和治疗赫普西定相关疾病中使用这些肽，包括预防和治疗铁过载疾病如血色病、铁负荷性贫血如地中海贫血，以及与效率低下或增强的红细胞生成相关的疾病，以及本文所述的进一步相关病症和疾病。
• [EN] PYRIMIDINE JAK INHIBITORS FOR THE TREATMENT OF SKIN DISEASES<br/>[FR] INHIBITEURS DE JAK À BASE DE PYRIMIDINE POUR LE TRAITEMENT DE MALADIES DE LA PEAU
  申请人：THERAVANCE BIOPHARMA R&D IP LLC

  公开号：WO2020219640A1

  公开（公告）日：2020-10-29

  The invention provides compounds of formula (I): or pharmaceutically-acceptable salts thereof, that are inhibitors of Janus kinases. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat inflammatory and autoimmune skin diseases.

  该发明提供了式(I)的化合物或其药用可接受盐，这些化合物是Janus激酶的抑制剂。该发明还提供了包含这些化合物的药物组合物，以及使用这些化合物治疗炎症性和自身免疫性皮肤疾病的方法。
• [EN] PHENOTHIAZINE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS DE PHÉNOTHIAZINE ET LEURS UTILISATIONS
  申请人：CAMP4 THERAPEUTICS CORP

  公开号：WO2019195789A1

  公开（公告）日：2019-10-10

  The present invention provides phenothiazine compounds, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment of various diseases or conditions, for example ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA).

  本发明提供了吩噻嗪化合物，其制备方法，包含该化合物的药物组合物，以及在治疗各种疾病或症状中使用该化合物或组合物，例如核糖体紊乱和核糖体病，例如钻石-布莱克范贫血（DBA）。

表征谱图