Casopitant mesylate
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.
| Supplier | Ace Therapeutics |
|---|---|
| Product # | SMD707 |
| CAS # | 414910-30-8 (mesylate) |
| Pricing | Customizable size, Inquiry |
| Synonym | GW679769; GW 679769; GW-679769; Casopitant mesylate. Trade names: Rezonic (US); Zunrisa (EU). |
| Product Category | Lab-use Small Molecule Drugs |
| 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 |
| 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 |
| Availability | 2 Weeks |