312-93-6

• 常用中文名：地塞米松 21-磷酸
• 常用英文名：Dexamethasone Phosphate
• CAS号：312-93-6
• 分子式：C₂₂H₃₀FO₈P
• 分子量：472.44100
• 相关类别： 原料药 激素及调节内分泌功能类药 肾上腺皮质激素类药
• 发布时间：2018-08-12 07:49:32
• 更新时间：2024-01-02 20:37:17
• Dexamethasone phosphate (Dexamethasone 21-phosphate) 是一种无生物活性的化合物,可通过红细胞内酶进行去磷酸化。活性代谢物地塞米松随后通过细胞膜的简单被动扩散释放到循环中。Dexamethasone phosphate 包裹的红细胞具有用于类固醇依赖性溃疡性结肠炎研究的潜力。

名称

• 中文名: 地塞米松磷酸酯
• 英文名: dexamethasone phosphate
• 英文别名: Hexadrol phosphate; dexamethasone-21-phosphate; Dexamethasone 21-orthophosphate; Betnelan phosphate; Dexamethasone-21-dihydrogen-phosphate; Wymesone; Neodecadron; Oradexon phosphate; Dexamethasone phosphate; [2-[(8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] dihydrogen phosphate

物化性质

• 密度: 1.45g/cm3
• 沸点: 669.6ºC at 760mmHg
• 熔点: 154-157°C (lit.)
• 分子式: C₂₂H₃₀FO₈P
• 分子量: 472.44100
• 闪点: 358.7ºC
• 精确质量: 472.16600
• PSA: 151.17000
• LogP: 2.01270
• 外观性状: 白色至浅棕色固体
• 折射率: 1.594
• 储存条件: 通风低温干燥

生物活性

• 描述: Dexamethasone phosphate (Dexamethasone 21-phosphate) 是一种无生物活性的化合物,可通过红细胞内酶进行去磷酸化。活性代谢物地塞米松随后通过细胞膜的简单被动扩散释放到循环中。Dexamethasone phosphate 包裹的红细胞具有用于类固醇依赖性溃疡性结肠炎研究的潜力。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体
• 参考文献:

  [1]. Fabrizio Bossa, et al. Erythrocytes-mediated delivery of dexamethasone 21-phosphate in steroid-dependent ulcerative colitis: a randomized, double-blind Sham-controlled study. Inflamm Bowel Dis. 2013 Aug;19(9):1872-9.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TU4055000 CHEMICAL NAME : Pregna-1,4-diene-3,20-dione, 9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methyl-, 21-(dihydrogen phosphate) CAS REGISTRY NUMBER : 312-93-6 LAST UPDATED : 199706 DATA ITEMS CITED : 14 MOLECULAR FORMULA : C22-H30-F-O8-P MOLECULAR WEIGHT : 472.49 WISWESSER LINE NOTATION : L E5 B666 OV AHTTT&J A1 BF CQ E1 FV1OPQQO FQ G1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 36 mg/kg/90D-I TOXIC EFFECTS : Endocrine - changes in thymus weight Immunological Including Allergic - decrease in cellular immune response Immunological Including Allergic - decrease in humoral immune response TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 600 ug/kg SEX/DURATION : female 21-22 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - endocrine system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 200 ug/kg SEX/DURATION : female 19-20 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - respiratory system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 400 ug/kg SEX/DURATION : female 19-20 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - hepatobiliary system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 30 mg/kg SEX/DURATION : female 8-13 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 2 mg/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - other measures of fertility TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 600 ug/kg SEX/DURATION : female 17-19 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material) Reproductive - Specific Developmental Abnormalities - respiratory system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 600 ug/kg SEX/DURATION : female 17-19 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 1 mg/kg SEX/DURATION : female 11-14 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 1 mg/kg SEX/DURATION : female 14-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral DOSE : 1 mg/kg SEX/DURATION : female 22-25 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) MUTATION DATA TEST SYSTEM : Rodent - rat DOSE/DURATION : 3 mg/kg REFERENCE : JOENAK Journal of Endocrinology. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1939- Volume(issue)/page/year: 62,527,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3850 No. of Facilities: 130 (estimated) No. of Industries: 3 No. of Occupations: 10 No. of Employees: 5388 (estimated) No. of Female Employees: 2968 (estimated)

安全

• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 62
• 海关编码: 2937290090

合成路线

50-02-2 ~% 312-93-6

文献：Chemical and Pharmaceutical Bulletin, , vol. 22, # 7 p. 1439 - 1450

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