Vosilasarm_product_DataBase

Bioactivity

Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors[1].

Target

Ki: 7 nM (Androgen receptor)

Invitro

Vosilasarm (0-300 nM; pretreated for 1 hour) increases neuron viability against Aβ in a concentration-dependent manner[2]. Vosilasarm (100 nM; 1 hour) protects cultured neurons against apoptotic insults. Vosilasarm shows protective profiles of significantly protecting against neuronal death induced by Aβ and AAII, but not H2O2[2]. Vosilasarm (100 nM; 15 minutes) induces a significant increase in levels of phosphorylated but not total ERK in neuronal cultures[2].

In Vivo

The stability of Vosilasarm is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and Vosilasarm also has good bioavailability in rats (F = 27-63%) and monkeys (65-75%)[1]. In castrated immature rats, Vosilasarm (0.03-0.3 mg/kg; for 11 days) stimulates the levator ani bulbocavernosus muscle weight and prostate weight[1]. A high dose of Vosilasarm (10 mg/kg, p.o.) actually antagonizes the effect of testosterone propionate (TP) at 1 mg/kg on the seminal vesicles but adds to the effect of TP on the levator ani muscle. The effective dose for achieving antagonism by Vosilasarm is 0.3-1 mg/kg (p.o.) for 1 mg/kg TP (s.c.). In the young castrate male rat model, Vosilasarm appears to be a potent and complete androgen agonist on the levator ani, but a weaker, partial antagonist on the seminal vesicle and possibly the prostate[1]. Vosilasarm is neuroprotective in vivo using the rat kainate lesion model. In experiments with gonadectomized, adult male rats, Vosilasarm is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as demonstrated by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate[2].

Name

Vosilasarm

CAS

1182367-47-0

Formula

C20H16ClN5O2

Molar Mass

393.83

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Miller CP, et al. Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Med Chem Lett. 2010 Dec 2;2(2):124-129. [2]. Jayaraman A, et al. Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. Endocrinology. 2014 Apr;155(4):1398-1406.

PeptideDB

Vosilasarm

CAS: 1182367-47-0 F: C20H16ClN5O2 W: 393.83