SRX-246 512784-93-9 manufacturers
- SRX246
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- $1360.00
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2026-04-21
- CAS:512784-93-9
- Purity:
- Supply Ability: 10g
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| | SRX-246 512784-93-9 Basic information |
| Product Name: | SRX-246 512784-93-9 | | Synonyms: | SRX-246 512784-93-9;SRX246;[1,4'-Bipiperidine]-1'-butanamide, γ-oxo-α-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-3-oxazolidinyl]-4-[(1E)-2-phenylethenyl]-1-azetidinyl]-N-[(1R)-1-phenylethyl]-, (αR)-;SRX246,SRX-246 | | CAS: | 512784-93-9 | | MF: | C42H49N5O5 | | MW: | 703.87 | | EINECS: | | | Product Categories: | | | Mol File: | 512784-93-9.mol |  |
| | SRX-246 512784-93-9 Chemical Properties |
| Boiling point | 958.9±65.0 °C(Predicted) | | density | 1.281±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | pka | 14.02±0.46(Predicted) | | form | Solid | | color | White to off-white |
| | SRX-246 512784-93-9 Usage And Synthesis |
| Uses | 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]. | | 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: | Male Sprague-Dawley rats[1] | | Dosage: | 2 mg/kg (20 mg/kg for p.o.) | | Administration: | i.v. (Pharmacokinetic Analysis) | | Result: | Following i.v. administration, the plasma concentration declined steadily with a half-life (t1/2) of 6 hours. The Cmax and AUC0-∞ values are 953 ng/mL, 1141 ng h/mL, 6.02 hours. Following an oral administration, the Cmax, AUC0-∞ and t1/2 values 98.4 ng/mL, 624 ng h/mL and 2.38 hours, respectively. |
| | References | [1] Guillon CD, et al. Azetidinones as vasopressin V1a antagonists. Bioorg Med Chem. 2007 Mar 1;15(5):2054-80. DOI:10.1016/j.bmc.2006.12.031
[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. DOI:10.1002/jps.23495 |
| | SRX-246 512784-93-9 Preparation Products And Raw materials |
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