SRX246

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].

Product Specifications

CAS Number

[512784-93-9]

UNSPSC

12352005

Target

Vasopressin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/srx-246.html

Purity

99.76

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1CCC(N2CCCCC2)CC1)C[C@H](C(N[C@@H](C3=CC=CC=C3)C)=O)N4[C@@H]([C@H](N5[C@@H](C6=CC=CC=C6)COC5=O)C4=O)/C=C/C7=CC=CC=C7

Molecular Formula

C42H49N5O5

Molecular Weight

703.87

References & Citations

[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.