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OPC 21268 Sale

(Synonyms: N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺,OPC-21268) 目录号 : GC10622

A nonpeptide antagonist of vasopressin V1 receptors

OPC 21268 Chemical Structure

Cas No.:131631-89-5

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Rats[1]Male Sprague-Dawley rats, 300 to 400 g, are injected with Fuscoside (OPC-21268) (0.1, 0.3, 1 mg/kg). Fuscoside (OPC-21268) is given 2 min before the injection of AVP at 30 mU/kg i.v., angiotensin II at 0.3 μg/kg i.v., and noradrenaline at 3 μg/kg i.v.[1].

References:

[1]. Yamamura Y, et al. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science. 1991 Apr 26;252(5005):572-4.
[2]. Bemana I, et al. Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats. Neurosurgery. 1999 Jan;44(1):148-54.

产品描述

Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.

The concentration of Fuscoside (OPC-21268) that displaces 50% of specific AVP binding (IC50) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (Ki) of Fuscoside (OPC-21268) for V1 receptors (0.14 μM)[1].

Fuscoside (OPC-21268) competitively and specifically antagonizes pressor responses to AVP in vivo. Oral administration of Fuscoside (OPC-21268) (10 mg/kg) inhibits the vasoconstriction induced by exogenous AVP in a dose- and time-dependent manner and the effect lasts for more than 8 hours at 30 mg/kg[1]. Fuscoside (OPC-21268) predominantly exerts a protective effect in areas where the maximum amount of blood-brain barrier breakdown occurs, and it is effective in the treatment of cold-induced vasogenic brain edema. Fuscoside (OPC-21268) treatment at the dosages of 200 and 300 mg/kg significantly reduces brain water content in both hemispheres. Swelling of the traumatized hemispheres is also significantly reduced at 200 and 300 mg/kg dosages[2].

References:
[1]. Yamamura Y, et al. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science. 1991 Apr 26;252(5005):572-4.
[2]. Bemana I, et al. Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats. Neurosurgery. 1999 Jan;44(1):148-54.

Chemical Properties

Cas No. 131631-89-5 SDF
别名 N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺,OPC-21268
化学名 N-(3-(4-(4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidine-1-carbonyl)phenoxy)propyl)acetamide
Canonical SMILES O=C1N(C2=CC=CC=C2CC1)C3CCN(C(C(C=C4)=CC=C4OCCCNC(C)=O)=O)CC3
分子式 C26H31N3O4 分子量 449.54
溶解度 <44.95mg/ml in DMSO; <11.24mg/ml in ethanol 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.2245 mL 11.1225 mL 22.245 mL
5 mM 0.4449 mL 2.2245 mL 4.449 mL
10 mM 0.2224 mL 1.1122 mL 2.2245 mL
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