SRX246_product_DataBase

Bioactivity

SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders[1].

Target

Ki: 0.3 nM (human vasopressin 1a receptor)

In Vivo

SRX246 (2 mg/kg; i.v.) treatment shows that the Cmax, AUC0-∞ and t1/2 values are 953 ng/mL, 1141 ng ▪h/mL, and 6.02 hours, respectively, in plasma pharmacokinetics. Following an oral administration (dose 20 mg/kg), The Cmax, AUC0-∞ and t1/2 values are 98.4 ng/mL, 624 ng ▪h/mL and 2.38 hours, respectively[1]. Animal Model:

Name

SRX246

CAS

512784-93-9

Formula

C42H49N5O5

Molar Mass

703.87

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]. Guillon CD, et al. Azetidinones as vasopressin V1a antagonists. Bioorg Med Chem. 2007 Mar 1;15(5):2054-80. [2]. Fabio KM, et al. Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist. J Pharm Sci. 2013 Jun;102(6):2033-2043.

PeptideDB

SRX246

CAS: 512784-93-9 F: C42H49N5O5 W: 703.87