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RG-12915
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RG-12915图片
CAS NO:136174-04-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
RG-12915是一种选择性的5-HT3拮抗剂,IC50值为0.16nM。
Cas No.136174-04-4
Canonical SMILESO=C(C1=C2OC(CCCC3)C3C2=CC(Cl)=C1)NC4CN5CCC4CC5
分子式C20H25ClN2O2
分子量360.88
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.

RG 12915 is a potent and selective displacer of binding of 5-hydroxytryptamine (5-HT3) binding sites (IC50 value = 0.16 nM), whereas failing to displace binding of ligands for the alpha-1, alpha-2 and beta adrenergic, 5-HT1 or 5-HT2 or cholinergic-muscarinic sites with IC50 values less than 1 μM.

RG 12915 has a lower ED50 value (0.004 mg/kg) for attenuating cisplatin-induced emetic episodes in the ferret. RG 12915 (1 mg/kg, p.o.) is highly protective against cisplatin-induced emesis in the dog. RG 12915 has no significant gastroprokinetic activity in the same species[1].

[1]. Fitzpatrick LR, et al. RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in the ferret and dog. J Pharmacol Exp Ther. 1990 Aug;254(2):450-5.