Netupitant

• CAT Number: A000038
• CAS Number: 290297-26-6
• Molecular Formula: C30H32F6N4O
• Molecular Weight: 578.59
• Purity: ≥95%
• Synonyms: CID6451149, CID 6451149, CID-6451149
• Target: Neuronal Signaling
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• InChI: 1S/C30H32F6N4O/c1-19-8-6-7-9-23(19)24-17-26(40-12-10-38(4)11-13-40)37-18-25(24)39(5)27(41)28(2,3)20-14-21(29(31,32)33)16-22(15-20)30(34,35)36/h6-9,14-18H,10-13H2,1-5H3
• InChIKey: WAXQNWCZJDTGBU-UHFFFAOYSA-N
• SMILES: CC1=CC=CC=C1C2=CC(=NC=C2N(C)C(=O)C(C)(C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4CCN(CC4)C

Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). 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 NK-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. Check for active clinical trials or closed clinical trials using this agent. O n 10/10 2014 FDA approved netupitant for the treatment of nausea and vomiting in patients undergoing cancer chemotherapy.

Reference

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