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Casopitant mesylate

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Specification

Cat. No.

SMD707

Related Diseases

Depression

Product Name

Casopitant mesylate

Size

1.0mg; 10.0mg

Price

Inquiry

Availability

2 Weeks

Description

Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK1 receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema.

CAS Number

414910-30-8 (mesylate)

Chemical Formula

C31H39F7N4O5S

Molecular Weight

712.72

Elemental Analysis

C, 52.24; H, 5.52; F, 18.66; N, 7.86; O, 11.22; S, 4.50

Synonym

GW679769; GW 679769; GW-679769; Casopitant mesylate. Trade names: Rezonic (US); Zunrisa (EU).

IUPAC/Chemical Name

(2R,4S)-4-(4-Acetyl-1-piperazinyl)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methyl-1-piperidinecarboxamide

InChi Key

YRFKYVWDPCOSTE-REWBLLDVSA-N

InChi Code

InChI=1S/C30H35F7N4O2.CH4O3S/c1-18-13-24(31)5-6-26(18)27-17-25(40-11-9-39(10-12-40)20(3)42)7-8-41(27)28(43)38(4)19(2)21-14-22(29(32,33)34)16-23(15-21)30(35,36)37;1-5(2,3)4/h5-6,13-16,19,25,27H,7-12,17H2,1-4H3;1H3,(H,2,3,4)/t19-,25+,27-;/m1./s1

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

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 Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>5 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).

HS Tariff Code

2934.99.03.00

All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.