氢化可的松琥珀酸钠

氢化可的松琥珀酸钠用途

Hydrocortisone hemisuccinate sodium 是一种有口服活性的生理性糖皮质激素。Hydrocortisone hemisuccinate sodium 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 sodium 可用于溃疡性结肠炎 (UC) 的研究。

氢化可的松琥珀酸钠名称

[ CAS 号 ]:
125-04-2

[ 中文名 ]:
氢化可的松琥珀酸钠

[ 英文名 ]:
Corlan

[中文别名 ]:

[英文别名 ]:

Solu-Glyc
Hydrocortisone hemisuccinate sodium salt
Intracort
Hydrocortisone sodium succinate
MFCD00069472
Saxizon
EINECS 204-725-5
Buccalsone
Hydrocortisone 21-sodium succinate
Corlan

氢化可的松琥珀酸钠生物活性

[ 描述 ]:

[ 相关类别 ]:

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

[体外研究]

半琥珀酸氢化可的松抑制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细胞没有细胞毒性作用[3]。半琥珀酸氢化可的松钠(0.12-60μM；72小时)抑制外周淋巴细胞(PBL)和T淋巴细胞培养物中的植物血凝素(PHA)反应[3]。

[体内研究]

半琥珀酸氢化可的松钠(30 mg/kg；每天两次,持续5天)可减少小鼠的体重减轻并增加食物摄入量[2]。动物模型：雄性Sprague-Dawley大鼠(200-220 g,10-11周)诱导结肠炎[2]剂量：30 mg/kg给药：每天两次,持续5天结果：与2,4,6-三硝基苯磺酸(TNBS)组相比,疾病活动指数(DAI)评分和髓过氧化物酶(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.

氢化可的松琥珀酸钠物理化学性质

[ 沸点 ]:
685.5ºC at 760mmHg

[ 分子式 ]:
C₂₅H₃₃NaO₈

[ 分子量 ]:
484.51

[ 闪点 ]:
231.1ºC

[ 精确质量 ]:
484.207306

[ PSA ]:
141.03000

[ LogP ]:
0.86260

[ 外观性状 ]:
powder

[ 蒸汽压 ]:
9.36E-22mmHg at 25°C

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
H2O: 50 mg/mL

氢化可的松琥珀酸钠MSDS

详细MSDS(安全技术说明书)

氢化可的松琥珀酸钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GM9015000

CHEMICAL NAME :: Cortisol, succinate, sodium salt

CAS REGISTRY NUMBER :: 125-04-2

LAST UPDATED :: 199612

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C25-H33-O8.Na

MOLECULAR WEIGHT :: 484.57

WISWESSER LINE NOTATION :: L E5 B666 OV MUTJ A1 CQ E1 FVYQOV2VO FQ &-NA- &43/36

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 2857 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - bronchiolar constriction Gastrointestinal - nausea or vomiting Blood - oxidant related (GPD deficient) anemia

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 154,210,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1320 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,625,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1050 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,625,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1400 mg/kg/14D-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 5,303,1980 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 1429 ug/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male Endocrine - androgenic

REFERENCE :: JCEMAZ Journal of Clinical Endocrinology and Metabolism. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.12- 1952- Volume(issue)/page/year: 57,671,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1800 mg/kg

SEX/DURATION :: female 9-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - urogenital system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 4,2969,1970

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1500 mg/kg

SEX/DURATION :: female 9-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 4,2969,1970

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1600 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 33,68C,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1200 mg/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 4,2957,1970

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

DOSE :: 120 mg/kg

SEX/DURATION :: female 10-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 16,175,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 30 mg/kg

SEX/DURATION :: female 28-30 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - immune and reticuloendothelial system

REFERENCE :: KRMJAC Kurume Medical Journal. (Kurume Univ. School of Medicine, Dept. of Physiology, 67, Asahi- machi, Kurume 830, Japan) V.1- 1954- Volume(issue)/page/year: 27,51,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 30 mg/kg

SEX/DURATION :: female 26-28 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - respiratory system

REFERENCE :: PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 48,547,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3657 No. of Facilities: 589 (estimated) No. of Industries: 3 No. of Occupations: 11 No. of Employees: 13629 (estimated) No. of Female Employees: 8741 (estimated)

氢化可的松琥珀酸钠安全信息

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

[ 危害码 (欧洲) ]:
Xi

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

[ WGK德国 ]:
3

[ RTECS号 ]:
GM9015000

氢化可的松琥珀酸钠文献

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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