1. GPCR/G Protein
  2. Vasopressin Receptor
  3. SRX246

SRX246 

Cat. No.: HY-105685 Purity: 99.69%
Handling Instructions

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.

For research use only. We do not sell to patients.

SRX246 Chemical Structure

SRX246 Chemical Structure

CAS No. : 512784-93-9

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10 mM * 1 mL in DMSO USD 542 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
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100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

Ki: 0.3 nM (human vasopressin 1a receptor)[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.
Clinical Trial
Molecular Weight

703.87

Formula

C₄₂H₄₉N₅O₅

CAS No.

512784-93-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

SRX246SRX 246SRX-246Vasopressin ReceptorCNSpenetrationmooddisordersblood-brainbarrieroralvasopressinselectivePTSDHuntington’sdiseaseInhibitorinhibitorinhibit

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