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编 号:F374610
分子式:C42H49N5O5
分子量:703.87
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
SRX246 (2 mg/kg;iv) 处理显示 Cmax、AUC0-∞ 和 t1/2 值为 953 ng/mL、1141 ng ?h/mL 和 6.02 小时,分别用于血浆药代动力学。口服给药后 (剂量 20 mg/kg),Cmax、AUC0-∞ 和 t1/2 值分别为 98.4 ng/mL、624 ng ?h/mL 和 2.38 小时。Animal Model:Male Sprague-Dawley rats
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.
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