1. GPCR/G Protein
    Neuronal Signaling
    Metabolic Enzyme/Protease
  2. Neurokinin Receptor
    Cytochrome P450
  3. Casopitant mesylate

Casopitant mesylate (Synonyms: GW679769B)

Cat. No.: HY-14405A
Handling Instructions

Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).

For research use only. We do not sell to patients.

Casopitant mesylate Chemical Structure

Casopitant mesylate Chemical Structure

CAS No. : 414910-30-8

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Description

Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV)[1][2].

IC50 & Target[1]

NK1

 

CYP3A4

 

In Vivo

In a ferret-model of Cisplatin- induced emesis, Casopitant (GW679769) inhibits retching and vomiting and reduced nausea-like behaviours in a dose-dependent manner. The pharmacokinetics and brain penetration of casopitant are studied in the ferret-model of cisplatin-induced emesis. Following a single intraperitoneal dose, radioactive labeled Casopitant ([14C]Casopitant) is rapidly absorbed, with plasma and brain concentrations being approximately equal at two hours post-dosing. [14C]Casopitant is found in the brain as the parent compound and two major oxidative metabolites (M1 and M2), accounting for approximately 76%, 19%, and 3% of the radioactivity, respectively; suggesting that the pharmacologic activity of Casopitant in the ferret is largely attributable to the parent compound. Casopitant possesses a high affinity for brain NK1 receptors in the ferret[2].

Clinical Trial
Molecular Weight

712.72

Formula

C₃₁H₃₉F₇N₄O₅S

CAS No.

414910-30-8

SMILES

O=C(N1[[email protected]@H](C2=CC=C(F)C=C2C)C[[email protected]@H](N3CCN(C(C)=O)CC3)CC1)N([[email protected]@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)C.CS(=O)(O)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CasopitantGW679769BNeurokinin ReceptorCytochrome P450NK receptorCYPsChemotherapyNK1antiemeticssafetyCYP3A4substance-PPONVCINVbrainpermeableInhibitorinhibitorinhibit

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Casopitant mesylate
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