Description
RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
Product information
CAS Number: 136174-04-4
Molecular Weight: 360.88
Formula: C20H25ClN2O2
Chemical Name: N-{1-azabicyclo[2.2.2]octan-3-yl}-4-chloro-8-oxatricyclo[7.4.0.0²,⁷]trideca-2,4,6-triene-6-carboxamide
Smiles: O=C(NC1CN2CCC1CC2)C1C=C(Cl)C=C2C3CCCCC3OC2=1
InChiKey: LDYMIBZOCSHLBG-UHFFFAOYSA-N
InChi: InChI=1S/C20H25ClN2O2/c21-13-9-15-14-3-1-2-4-18(14)25-19(15)16(10-13)20(24)22-17-11-23-7-5-12(17)6-8-23/h9-10,12,14,17-18H,1-8,11H2,(H,22,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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