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Aminoglutethimide

Aminoglutethimide
Aminoglutethimide structure
CAS No.
125-84-8
Chemical Name:
Aminoglutethimide
Synonyms
Elipten;Cytadren;Ba-16038;ORIMETEN;NSC-330915;AKOS NCG1-0032;AMINOGLUTETHAMIDE;AMINOGLUTETHIMIDE;TIMTEC-BB SBB000711;DL-AMINOGLUTETHIMIDE
CBNumber:
CB5131691
Molecular Formula:
C13H16N2O2
Formula Weight:
232.28
MOL File:
125-84-8.mol

Aminoglutethimide Properties

Melting point:
152-154 °C(lit.)
Boiling point:
374.44°C (rough estimate)
Density 
1.1099 (rough estimate)
refractive index 
1.6450 (estimate)
storage temp. 
2-8°C
solubility 
H2O: 0.2 mg/mL, slightly soluble
pka
11.60±0.40(Predicted)
form 
neat
color 
white
Water Solubility 
Soluble in water (2 mg/ml at 20°C), methanol (50 mg/ml), ethanol (7 mg/ml at 25°C), DMSO (20 mg/ml at 25°C), and chloroform.
Merck 
14,440
CAS DataBase Reference
125-84-8(CAS DataBase Reference)
EWG's Food Scores
1
FDA UNII
0O54ZQ14I9
NIST Chemistry Reference
Aminoglutethimide(125-84-8)
Proposition 65 List
Aminoglutethimide
EPA Substance Registry System
Aminoglutethimide (125-84-8)
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P280a-P304+P340-P405-P501a-P305+P351+P338-P261
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  26-36
RIDADR  3249
WGK Germany  3
RTECS  MA4026950
HazardClass  6.1(b)
PackingGroup  III
HS Code  2925190100

Aminoglutethimide price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 1025205 Aminoglutethimide United States Pharmacopeia (USP) Reference Standard 125-84-8 200mg $352.8 2019-12-02 Buy
Sigma-Aldrich A9657 DL-Aminoglutethimide 125-84-8 1g $845 2019-12-02 Buy
Alfa Aesar J62182 DL-Aminoglutethimide, 99% 125-84-8 1g $30.8 2019-12-02 Buy
Alfa Aesar J62182 DL-Aminoglutethimide, 99% 125-84-8 5g $81.4 2019-12-02 Buy
Cayman Chemical 20947 Aminoglutethimide ≥98% 125-84-8 5g $69 2018-11-19 Buy

Aminoglutethimide Chemical Properties,Uses,Production

Chemical Properties

White Solid

Uses

aromatase inhibitor, antineoplastic, testosterone suppressant

Uses

An aromatase inhibitor. Also blocks adrenal steroidogenesis

Definition

ChEBI: A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.

Indications

Aminoglutethimide (Cytadren) is a competitive inhibitor of desmolase, the enzyme that catalyzes the conversion of cholesterol to pregnenolone; it also inhibits 11-hydroxylase activity.This drug also reduces estrogen production by inhibiting the aromatase enzyme complex in peripheral (skin, muscle, fat) and steroid target tissues.

brand name

Cytadren (Novartis);C-16038-ba;Crytraden;Doredin;Mamomit;Ormeten.

World Health Organization (WHO)

Aminoglutethimide, a weak anticonvulsant, was introduced in 1960 for use in the treatment of epilepsy. However, its adrenocortical suppressant activity gave rise to serious adverse effects. The FDA decision in 1966 was taken in respect of a preparation indicated in epilepsy. In 1980 preparations containing aminoglutethimide were reintroduced in the USA exclusively for the treatment of Cushing's disease. In 1986 they were also registered in Saudi Arabia for use in Cushing's syndrome and for the treatment of breast cancer. In some other countries these preparations are additionally approved for carcinoma of the prostate.

General Description

Aminoglutethimide, 3-(4-aminophenyl)-3-ethyl-2,6-piperidinedione, is mainly usedto treat Cushing syndrome, a condition of adrenal steroidexcess, a use in which the P450scc inhibition of thiscompound is exploited rather than its aromatase inhibition.Aminoglutethimide is a weak inhibitor of aromataseand has been used successfully in the treatment of estrogen-dependent breast cancer. Because of the developmentof more selective aromatase inhibitors, the use ofaminoglutethimide for its ability to inhibit aromatase is notsupported.

Clinical Use

Aminoglutethimide is suitable for use in Cushing’s syndrome that results from adrenal carcinoma and in congenital adrenal hyperplasia, in which it protects the patient from excessive secretion of endogenous androgens. The drug is not curative, and relapse occurs when treatment is terminated. Since aminoglutethimide therapy is frequently associated with mineralocorticoid deficiency, mineralocorticoid supplements may be needed. Aminoglutethimide and metyrapone are frequently used in combination at lower doses of both drugs as an adjunct to radiation or surgical therapy.

Side effects

Such a medical adrenalectomy is an efficacious treatment for metastatic breast and prostate cancer, since it diminishes the levels of circulating sex hormones. Glucocorticoids are administered concomitantly to suppress enhanced corticotrophin release. Cortisol is preferable to dexamethasone in this situation because aminoglutethimide markedly enhances the hepatic microsomal metabolism of dexamethasone. Hepatic enzyme induction may be responsible for the development of tolerance to the side effects of aminoglutethimide, such as ataxia, lethargy, dizziness, and rashes.

Metabolic pathway

Following administration of a single oral dose of 14C- aminoglutethimide to rats, guinea pigs, rabbits, and man, more than 89% of the dose is excreted in urine and feces within 72h, and dogs eliminate only 51% in this time. Extensive metabolism occurs in all species, with N-acetylaminoglutethimide being the major metabolite except for dogs and man. In the latter two species, the unchanged drug is the main product excreted. As shown in the pathways, it appears that aminoglutethimide is metabolized by several pathways in man and, of the ten metabolites, only two are present in any quantity, namely N-acetylaminoglutethimide and N-hydroxyaminoglutethimide, the latter increasing during the course of treatment.

Aminoglutethimide Preparation Products And Raw materials

Raw materials

Preparation Products


Aminoglutethimide Suppliers

Global( 110)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21829 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30050 58
SHANDONG ZHI SHANG CHEMICAL CO.LTD
+86 18953170293
+86 0531-67809011 sales@sdzschem.com CHINA 2995 58
Hubei xin bonus chemical co. LTD
86-13657291602
027-59338440 linda@hubeijusheng.com CHINA 23047 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales03@yibaibiotech.com CHINA 420 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 35436 58
CONIER CHEM AND PHARMA LIMITED
86-18523575427
sales@conier.com CHINA 47486 58
Shaanxi Dideu Medichem Co. Ltd
+86-15319487004
+86-29-88380327 1015@dideu.com CHINA 3429 58
Amadis Chemical Company Limited
0086-571-89925085
0086-571-89925065 sales@amadischem.com China 132151 58

View Lastest Price from Aminoglutethimide manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2020-04-29 Aminoglutethimide
125-84-8
US $0.00-0.00 / 公斤 1KG 99.0%+ 800 tons Shaanxi Dideu Medichem Co. Ltd
2020-04-29 Aminoglutethimide
125-84-8
US $0.00-0.00 / 公斤 1KG 99.0%+ 800 tons Shaanxi Dideu Medichem Co. Ltd
2019-08-28 Aminoglutethimide
125-84-8
US $0.00-0.00 / KG 1g 99.0% 50kg/month Beijing Yibai Biotechnology Co., Ltd

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