ACV 1

• CAT Number: P000208
• CAS Number: 740980-24-9
• Molecular Formula: C71H103N23O25S4
• Molecular Weight: 1806.98
• Purity: ≥95%
• Target: Nicotinic Receptor
• Storage: Store at -20C
• InChI: InChI=1S/C71H103N23O25S4/c1-3-32(2)55-68(117)89-44(56(74)105)27-120-122-30-47-65(114)88-43(26-95)62(111)87-42(23-54(103)104)70(119)94-18-6-8-48(94)66(115)81-36(7-4-16-78-71(75)76)57(106)90-46(29-123-121-28-45(63(112)91-47)80-51(98)24-72)64(113)84-39(21-50(73)97)60(109)83-38(19-33-10-12-35(96)13-11-33)59(108)85-40(22-53(101)102)61(110)86-41(20-34-25-77-31-79-34)69(118)93-17-5-9-49(93)67(116)82-37(58(107)92-55)14-15-52(99)100/h10-13,25,31-32,36-49,55,95-96H,3-9,14-24,26-30,72H2,1-2H3,(H2,73,97)(H2,74,105)(H,77,79)(H,80,98)(H,81,115)(H,82,116)(H,83,109)(H,84,113)(H,85,108)(H,86,110)(H,87,111)(H,88,114)(H,89,117)(H,90,106)(H,91,112)(H,92,107)(H,99,100)(H,101,102)(H,103,104)(H4,75,76,78)
• InChIKey: KJQOYUHYAZGPIZ-PIJHVLQJSA-N
• SMILES: CCC(C)C1C(=O)NC(CSSCC2C(=O)NC(C(=O)NC(C(=O)N3CCCC3C(=O)NC(C(=O)NC(CSSCC(C(=O)N2)NC(=O)CN)C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N4CCCC4C(=O)NC(C(=O)N1)CCC(=O)O)CC5=CNC=N5)CC(=O)O)CC6=CC=C(C=C6)O)CC(=O)N)CCCNC(=N)N)CC(=O)O)CO)C(=O)N

ACV 1 (CAS 740980-24-9) is a neuronal nicotinic receptor antagonist that displays selectivity for the α9α10 subtype (IC50 values are 19, 140, 980, 4200 and 7300 nM for α9α10, α6/α3β2β3, α6/α3β4, α3β4 and α3β2 subtypes respectively). It alleviates neuropathic pain in three rat models of human neuropathic pain and accelerates functional recovery of injured neurons.

Reference

1.Sandall, D. W., et al. "A novel α-conotoxin identified by gene sequencing is active in suppressing the vascular response to selective stimulation of sensory nerves in vivo." Biochemistry 42.22 (2003): 6904-6911.
2.Nevin, Simon T., et al. "Are α9α10 nicotinic acetylcholine receptors a pain target for α-conotoxins?." Molecular pharmacology 72.6 (2007): 1406-1410.
3.Halai, Reena, et al. "Scanning mutagenesis of α-conotoxin Vc1. 1 reveals residues crucial for activity at the α9α10 nicotinic acetylcholine receptor." Journal of Biological Chemistry 284.30 (2009): 20275-20284.
4.Vincler, Michelle, et al. "Molecular mechanism for analgesia involving specific antagonism of α9α10 nicotinic acetylcholine receptors." Proceedings of the National Academy of Sciences 103.47 (2006): 17880-17884.