A synthetic progestin and PR agonist (EC50s = 3.4-10.5 nM in transactivation assays); selective for PR over ERα and ERβ

Dienogest – 25 mg

Brand:
Cayman
CAS:
65928-58-7
Storage:
-20
UN-No:
Non-Hazardous - /

Dienogest is a synthetic progestin and progesterone receptor (PR) agonist (EC50s = 3.4-10.5 nM in transactivation assays).{46786} It is selective for PR over estrogen receptor α (ERα) and ERβ, as well as glucocorticoid and mineralocorticoid receptors (EC50s = >3,000 nM for all), as well as sex hormone-binding globulin (SHBG) and cortisol-binding globulin (CBG; IC50s = 900-950 and 7,970 nM, respectively, in radioligand binding assays). It also inhibits dihydrotestosterone-induced transactivation of the androgen receptor (EC50s = 420.6-775 nM). Dienogest (0.1, 0.3, and 1 mg/kg per day for 21 days, p.o.) reduces lesion formation in a rat model of endometriosis.{46787} It reduces 17β-estradiol benzoate-dependent tumor growth in an MCF-7 ovariectomized mouse xenograft model when administered at doses of 0.1 and 1 mg/kg per day for 28 days.{46788} Formulations containing dienogest in combination with estradiol valerate have been used as contraceptives.  

 

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Description

A synthetic progestin and PR agonist (EC50s = 3.4-10.5 nM in transactivation assays); selective for PR over ERα and ERβ, as well as glucocorticoid, and mineralocorticoid receptors (EC50s = >3,000 nM for all), as well as SHBG and CBG (IC50s = 900-950 and 7,970 nM, respectively, in radioligand binding assays); inhibits dihydrotestosterone-induced transactivation of the androgen receptor (EC50s = 420.6-775 nM); reduces lesion formation in a rat model of endometriosis at 0.1, 0.3, and 1 mg/kg per day for 21 days orally; reduces 17β-estradiol benzoate-dependent tumor growth in an MCF-7 ovariectomized mouse xenograft model at 0.1 and 1 mg/kg per day for 28 days

Formal name: (17α)-17-hydroxy-3-oxo-19-norpregna-4,9-diene-21-nitrile

Synonyms:  STS 557

Molecular weight: 311.4

CAS: 65928-58-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Reproductive Biology

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