RAD140 Cas No.1182367-47-0

1182367-47-0 Biological Activity

Description

RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). IC50 value: 7 nM (Ki, fot androgen receptor) [1]Target: androgen receptor in vitro: RAD140 demonstrates excellent affinity for the androgen receptor (Ki = 7 nM) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM). [1] RAD140 is a novel SARM with high affinity and specificity for AR, is orally available, and exhibits potent anabolic effects in rodents and nonhuman primates.[2]in vivo: The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats and monkeys. [1] RAD140 is also neuroprotective using the rat kainate lesion model. RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.

Related Catalog

Signaling Pathways >> Others >> Androgen Receptor

Research Areas >> Endocrinology

References

[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.

1182367-47-0 Chemical & Physical Properties

Melting point 

179-183°C

Boiling point

687.7±65.0 °C at 760 mmHg

Density

1.4±0.1 g/cm3

Molecular Formula

C20H16ClN5O2

Molecular Weight

393.826

Flash Point

369.7±34.3 °C

PSA

118.76000

LogP

3.02

Exact Mass

393.099243

Vapour Pressure

0.0±2.3 mmHg at 25°C

Index of Refraction

1.652