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RG-12915

Catalog No. T12716 CAS 136174-04-4

RG-12915 is a selective antagonist of 5-HT3(IC50 value of 0.16 nM).

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RG-12915, CAS 136174-04-4

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Purity: 98%

Biological Description

Chemical Properties

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Description	RG-12915 is a selective antagonist of 5-HT3(IC50 value of 0.16 nM).
Targets&IC50	5-HT3:0.16 nM
In vitro	RG 12915 is a displacer of binding of 5-hydroxytryptamine (5-HT3) binding sites with IC50 value of 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 (IC50 values less than 1 μM).
In vivo	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. RG 12915 has a lower ED50 value for attenuating cisplatin-induced emetic episodes in the ferret[1].

Molecular Weight	360.88
Formula	C20H25ClN2O2
CAS No.	136174-04-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RG-12915 136174-04-4 GPCR/G Protein Neuroscience 5-HT Receptor RG 12915 RG12915 Inhibitor inhibitor inhibit

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