氢可琥珀酸酯

氢可琥珀酸酯用途

Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate),一种糖皮质激素, 是口服活性的甾体抗炎剂 (SAID)。Hydrocortisone hemisuccinate 抑制 IL-6 和 IL-3 的生物活性,IC50 值分别为 6.7 和 21.4 μM。Hydrocortisone hemisuccinate 可用于溃疡性结肠炎 (UC) 的研究。

氢可琥珀酸酯名称

[ CAS 号 ]:
2203-97-6

[ 中文名 ]:
氢化可的松琥珀酸酯

[ 英文名 ]:
Hydrocortisone hemisuccinate

[中文别名 ]:

氢可琥珀酸酯

[英文别名 ]:

Hydrocortisone 21-he
MFCD00046256
saxizon
cortisol,hydrogensuccinate
cortisolsuccinate
hydrocortisone hemisuccinate ester
CORTISOL HEMISUCCINATE
Hydrocortisone hydrogen succinate
Hydrocortisone hemisuccinate
EINECS 218-612-3

氢可琥珀酸酯生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 内分泌

信号通路 >> 免疫及炎症 >> 白细胞介素相关

研究领域 >> 炎症/免疫

研究领域 >> 代谢疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体

[ 靶点 ]

IL-6:6.7 μM (IC50)

IL-3:21.4 μM (IC50)

[体外研究]

氢化可的松半琥珀酸盐抑制IL-6和IL-3的生物活性,IC50分别为6.7和21.4μM,对IL-6非依赖性MH60细胞无细胞毒性作用[3]。半琥珀酸氢化可的松(0.12-60μM；72小时)抑制外周血淋巴细胞(PBL)和T淋巴细胞培养中的植物血凝素(PHA)反应[3]。

[体内研究]

半琥珀酸氢化可的松(30mg/kg；p.o.每日两次,持续5d)可减轻小鼠体重并增加食物摄入量[2]。动物模型：雄性Sprague-Dawley大鼠(200-220g,10-11周)诱导结肠炎[2]剂量：30mg/kg给药：P.o.每日2次,连续5d结果：与2,4,6-三硝基苯磺酸(TNBS)组相比,DAI评分和MPO活性显著降低。增加了体重。

[参考文献]

[1]. Kang BS, et, al. Inhibitory effects of anti-inflammatory drugs on interleukin-6 bioactivity. Biol Pharm Bull. 2001 Jun;24(6):701-3.

[2]. You YC, et, al. In vitro and in vivo application of pH-sensitive colon-targeting polysaccharide hydrogel used for ulcerative colitis therapy. Carbohydr Polym. 2015 Oct 5;130:243-53.

[3]. Langhoff E, et, al. The immunosuppressive potency in vitro of physiological and synthetic steroids on lymphocyte cultures. Int J Immunopharmacol. 1987;9(4):469-73.

氢可琥珀酸酯物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
685.5±55.0 °C at 760 mmHg

[ 分子式 ]:
C₂₅H₃₄O₈

[ 分子量 ]:
462.533

[ 闪点 ]:
231.1±25.0 °C

[ 精确质量 ]:
462.225372

[ PSA ]:
138.20000

[ LogP ]:
2.13

[ 蒸汽压 ]:
0.0±4.8 mmHg at 25°C

[ 折射率 ]:
1.587

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
Practically insoluble in water, freely soluble in acetone and in anhydrous ethanol. It dissolves in dilute solutions of alkali carbonates and alkali hydroxides.

氢可琥珀酸酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TU5010147

CHEMICAL NAME :: Preg-4-ene-3,20-dione, 21-(3-carboxy-1-oxopropoxy)-11,17-dihydroxy-, (11-beta)-

CAS REGISTRY NUMBER :: 2203-97-6

LAST UPDATED :: 199504

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C25-H34-O8

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4200 mg/kg/10W-C

TOXIC EFFECTS :: Immunological Including Allergic - decrease in humoral immune response

REFERENCE :: BECTA6 Bulletin of Environmental Contamination and Toxicology. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1966- Volume(issue)/page/year: 41,523,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4704 No. of Facilities: 114 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 16945 (estimated) No. of Female Employees: 15681 (estimated)

氢可琥珀酸酯安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
TU5010147

氢可琥珀酸酯合成路线

详细合成路线

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氢可琥珀酸酯文献

Daily endogenous cortisol production and hydrocortisone pharmacokinetics in adult horses and neonatal foals.

Am. J. Vet. Res. 73(1) , 68-75, (2012)

To compare daily endogenous cortisol production rate and the pharmacokinetics of an i.v. bolus of hydrocortisone between neonatal foals and adult horses.10 healthy full-term 2- to 4-day-old foals and ...

The compatibility of a low concentration of hydrocortisone sodium succinate with selected drugs during a simulated Y-site administration.

Crit. Care Resusc. 15(1) , 63-6, (2013)

Bolus dose concentrations of hydrocortisone (50mg/mL) are reported to be incompatible with midazolam and ciprofloxacin in Y-site mixing studies. We evaluated the physical and chemical compatibility of...

Glucocorticoids decrease serum adiponectin level and WAT adiponectin mRNA expression in rats.

Steroids 75(12) , 853-8, (2010)

Accumulating evidence suggests that adiponectin plays an important role in the genesis of obesity and insulin resistance. Although it has been shown that glucocortocoids (GC) inhibit adiponectin expre...

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