Casopitant mesylate salt form · mesylate · Parent Casopitant · Synonyms: GW679769B

Casopitant mesylate is a potent, selective, brain permeable and orally active neurokinin 1 receptor antagonist.

For research use only. Not for human or veterinary use.

Target Neurokinin Receptor Cytochrome P450

Research area Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Casopitant mesylate structure

CAS No.: 414910-30-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 870.00	BP-00091A-25mg	In stock	Get quote
50 mg	USD 1,430.00	BP-00091A-50mg	In stock	Get quote
100 mg	USD 2,150.00	BP-00091A-100mg	In stock	Get quote

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Description

Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist.

Biological activity

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).

Identifiers

SMILES: O=C(N1[C@@H](C2=CC=C(F)C=C2C)C[C@@H](N3CCN(C(C)=O)CC3)CC1)N([C@@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)C.CS(=O)(O)=O
InChIKey: YRFKYVWDPCOSTE-REWBLLDVSA-N

Specifications

MW (average): 712.7190
Formula: C₃₁H₃₉F₇N₄O₅S
CAS No.: 414910-30-8
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 33.33 mg/mL

Documents

References

[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.

Same target

Search Neurokinin Receptor

Same research area

Search Neurological Disease