SRX246 - a vasopressin 1a (V1a) receptor antagonist. CAS# 512784-93-9


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M19493-C Contact sales@xcessbio.com for quotation $100

Description

SRX246, CAS No. 512784-93-9, 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.

Product information

CAS Number: 512784-93-9

Molecular Weight: 703.87

Formula: C42H49N5O5

Chemical Name: (2R)-4-{[1,4'-bipiperidin]-1'-yl}-4-oxo-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]-N-[(1R)-1-phenylethyl]butanamide

Smiles: C[C@@H](NC(=O)[C@@H](CC(=O)N1CCC(CC1)N1CCCCC1)N1[C@H](/C=C/C2C=CC=CC=2)[C@@H](C1=O)N1[C@H](COC1=O)C1C=CC=CC=1)C1C=CC=CC=1

InChiKey: FJUKOXWSIGULLE-JVOQCOEYSA-N

InChi: InChI=1S/C42H49N5O5/c1-30(32-16-8-3-9-17-32)43-40(49)36(28-38(48)45-26-22-34(23-27-45)44-24-12-5-13-25-44)46-35(21-20-31-14-6-2-7-15-31)39(41(46)50)47-37(29-52-42(47)51)33-18-10-4-11-19-33/h2-4,6-11,14-21,30,34-37,39H,5,12-13,22-29H2,1H3,(H,43,49)/b21-20+/t30-,35-,36-,37-,39+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.

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