SRX246 |
| Katalog-Nr.GC38948 |
SRX246 ist ein potenter, zentralnervöser, hochselektiver und oral verfügbarer Vasopressin-1a (V1a)-Rezeptorantagonist (Ki=0,3 nM für den menschlichen V1a).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 512784-93-9
Sample solution is provided at 25 µL, 10mM.
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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 is under development for the treatment of stress-related disorders[1].
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: Male Sprague-Dawley rats[1]
[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.
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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