RG-12915

Modify Date: 2024-01-09 17:31:12

RG-12915 Structure
RG-12915 structure
Common Name RG-12915
CAS Number 136174-04-4 Molecular Weight 360.878
Density 1.3±0.1 g/cm3 Boiling Point 462.6±45.0 °C at 760 mmHg
Molecular Formula C20H25ClN2O2 Melting Point N/A
MSDS N/A Flash Point 233.6±28.7 °C

 Use of RG-12915


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

 Names

Name RG-12915
Synonym More Synonyms

 RG-12915 Biological Activity

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

IC50: 0.16 nM (5-HT3)[1]

In Vitro 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.
In Vivo 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].
References

[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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 462.6±45.0 °C at 760 mmHg
Molecular Formula C20H25ClN2O2
Molecular Weight 360.878
Flash Point 233.6±28.7 °C
Exact Mass 360.160461
LogP 4.03
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.631
Storage condition 2-8℃

 Synonyms

533O919MKO
4-Dibenzofurancarboxamide, N-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2-chloro-5a,6,7,8,9,9a-hexahydro-, (5aS,9aS)-
(5aS,9aS)-N-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-2-chloro-5a,6,7,8,9,9a-hexahydrodibenzo[b,d]furan-4-carboxamide
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