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Casopitant mesylate

Catalog No. T10688 CAS 414910-30-8

Synonyms: GW679769B

Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.

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Casopitant mesylate, CAS 414910-30-8

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,330.00
50 mg	8-10 weeks	$ 1,740.00
100 mg	8-10 weeks	$ 2,780.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description

Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.

In vivo

In a ferret-model of Cisplatin-induced emesis, Casopitant inhibits retching and vomiting and reduced nausea-like behaviours in a dose-dependent manner. 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. Casopitant possesses a high affinity for brain NK1 receptors in the ferret [2].

Synonyms	GW679769B
Molecular Weight	712.72
Formula	C31H39F7N4O5S
CAS No.	414910-30-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Ruhlmann C, et al. Casopitant: a novel NK(1)-receptor antagonist in the prevention of chemotherapy-induced nausea and vomiting. Ther Clin Risk Manag. 2009 Apr;5(2):375-84. 2. Minthorn E, et al. Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret. Drug Metab Dispos. 2008 Sep;36(9):1846-52.

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Keywords

Casopitant mesylate 414910-30-8 GPCR/G Protein Metabolism Neuroscience P450 Neurokinin receptor Casopitant Mesylate GW679769B inhibitor inhibit

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