102676-87-9

Name	Benzonitrile, 4-[(5R)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl]-
CAS	102676-87-9
Molecular Formula	C14H13N3
Molecular Weight	223.27
MOL File	102676-87-9.mol

Synonyms

(R)-Fadrozole (R)-CGS 16949A free base (R) Fadrozole,(R)Fadrozole (R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile Benzonitrile, 4-[(5R)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl]-

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Chemical Properties

Boiling point	481.7±38.0 °C(Predicted)
density	1.20±0.1 g/cm3(Predicted)
form	Solid
pka	7.16±0.40(Predicted)
color	Light yellow to yellow

Hazard Information

Uses

Dexfadrostat ((R)-Fadrozole) is a potent nonsteroidal inhibitor[1]. Dexfadrostat also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. Dexfadrostat reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.[1][2].

in vivo

Dexfadrostat ((R)-fadrozole; 0.24 and 1.2 mg/kg; daily; oral) and (S)-fadrozole similarly decreases plasma aldosterone levels, whereas urinary aldosterone excretion rate was reduced only by S-fadrozole^[2].
Dexfadrostat (0.24 and 1.2 mg/kg; daily; oral) effectively reverses preexistent left ventricular interstitial fibrosis by 50% (vs. 42% for canrenoate), S-fadrozole was devoid of an antifibrotic effect^[2].

Animal Model:	SHHF rats^[2]
Dosage:	0.24 and 1.2 mg/kg
Administration:	Daily; oral
Result:	Decreased plasma aldosterone levels and reversed preexistent left ventricular interstitial fibrosis.

References

[1] Furet P, et al. Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds. J Med Chem. 1993;36(10):1393-1400. DOI:10.1021/jm00062a012
[2] Minnaard-Huiban M, et al. Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats: discordant enantioselectivity versus reduction of plasma aldosterone. Endocrinology. 2008;149(1):28-31. DOI:10.1210/en.2007-0584

Supplier

Henan Alpha Chemical Co., Ltd.

Telephone0371-55013243 15324716602

Websitehttps://www.chemicalbook.com/supplier/24684125/

Nantong QuanYi Biotechnology Co., Ltd

Telephone0513-66337626 18051384581

Websitehttps://www.chemhifuture.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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