SRX-246 512784-93-9
- CAS No.
- 512784-93-9
- Chemical Name:
- SRX-246 512784-93-9
- Synonyms
- SRX246;SRX246,SRX-246;SRX-246 512784-93-9;[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)-
- CBNumber:
- CB94694901
- Molecular Formula:
- C42H49N5O5
- Molecular Weight:
- 703.88
- MDL Number:
- MFCD32689417
- MOL File:
- 512784-93-9.mol
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 |
form | Solid |
pka | 14.02±0.46(Predicted) |
color | White to off-white |
FDA UNII | 372X2P22UY |
SRX-246 512784-93-9 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0026445 | SRX246 99.69% | 512784-93-9 | 5mg | $350 | 2021-12-16 | Buy |
ChemScene | CS-0026445 | SRX246 99.69% | 512784-93-9 | 10mg | $550 | 2021-12-16 | Buy |
ChemScene | CS-0026445 | SRX246 99.69% | 512784-93-9 | 50mg | $1650 | 2021-12-16 | Buy |
ChemScene | CS-0026445 | SRX246 99.69% | 512784-93-9 | 100mg | $2250 | 2021-12-16 | Buy |
SRX-246 512784-93-9 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
SRX-246 512784-93-9 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 32354 | 58 |
TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 19929 | 58 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9729 | 58 |
Shanghai ruichang pharmaceutical technology co., LTD | 18621054990 | maychemicals@sina.com | China | 673 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11218 | 58 |
Kaifeng Mingren Pharmaceutical Co.,LTD | 0371-65741762 | sales@hasunny.com | China | 2380 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24980 | 58 |
Biosynth Biological Technology (Suzhou) Co Ltd | 51288865780 | sales@biosynth.com | China | 6051 | 58 |