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Corlan

Names

[ CAS No. ]:
125-04-2

[ Name ]:
Corlan

[Synonym ]:
Pregn-4-ene-3,20-dione, 21-(3-carboxy-1-oxopropoxy)-11,17-dihydroxy-, monosodium salt, (11β)-
Sodium 4-{[(11β)-11,17-dihydroxy-3,20-dioxopregn-4-en-21-yl]oxy}-4-oxobutanoate
Solu-Glyc
Butanedioic acid, mono[(11β)-11,17-dihydroxy-3,20-dioxopregn-4-en-21-yl] ester, sodium salt (1:1)
Hydrocortisone hemisuccinate sodium salt
Natrium-4-{2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethoxy}-4-oxobutanoat
Intracort
Hydrocortisone sodium succinate
MFCD00069472
(11b)-21-(3-Carboxy-1-oxopropoxy)-11,17-dihydroxypregn-4-ene-3,20-dione Monosodium Salt
Saxizon
EINECS 204-725-5
Buccalsone
butanedioic acid, mono[(11β)-11,17-dihydroxy-3,20-dioxopregn-4-en-21-yl] ester, monosodium salt
Hydrocortisone 21-sodium succinate
Corlan
sodium 4-{2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethoxy}-4-oxobutanoate
Nordicort
4-{2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-diméthyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tétradécahydro-1H-cyclopenta[a]phénanthrén-17-yl]-2-oxoéthoxy}-4-oxobutanoate de sodium
Sodium 17-hydroxycorticosterone 21-succinate

Biological Activity

[Description]:

Hydrocortisone hemisuccinate sodium is an orally active physiological glucocorticoid. Hydrocortisone hemisuccinate sodium inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate sodium can be used for the research of ulcerative colitis (UC)[1].

[Related Catalog]:

Research Areas >> Metabolic Disease
Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor

[In Vitro]

Hydrocortisone hemisuccinate sodium inhibits IL-6 and IL-3 bioactivity, with IC50s of 6.7 and 21.4 μM, respectively, and shows no cytotoxic effects on IL-6-independent MH60 cells[3]. Hydrocortisone hemisuccinate sodium (0.12-60 μM; 72 h) inhibits phytohemagglutinin (PHA) response in peripheral lymphocytes (PBL) and T-lymphocytes cultures[3].

[In Vivo]

Hydrocortisone hemisuccinate sodium (30 mg/kg; p.o. twice daily for 5 d) reduces the weight loss and increases the food intake in mice[2]. Animal Model: Male Sprague-Dawley rats (200-220 g, 10-11 weeks) are induced colitis[2] Dosage: 30 mg/kg Administration: P.o. twice daily for 5 days Result: Significantly decreased the disease activity index (DAI) scores and myeloperoxidase (MPO) activity compared to the 2, 4, 6-trinitrobenzenesulfonic acid (TNBS) group. Increased the body weight.

[References]

[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.  

Chemical & Physical Properties

[ Boiling Point ]:
685.5ºC at 760mmHg

[ Molecular Formula ]:
C25H33NaO8

[ Molecular Weight ]:
484.51

[ Flash Point ]:
231.1ºC

[ Exact Mass ]:
484.207306

[ PSA ]:
141.03000

[ LogP ]:
0.86260

[ Appearance of Characters ]:
powder

[ Vapour Pressure ]:
9.36E-22mmHg at 25°C

[ Storage condition ]:
−20°C

[ Water Solubility ]:
H2O: 50 mg/mL

MSDS

Toxicological Information

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)

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
GM9015000

Articles

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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