SNX-482 (ammonium salt)

SNX-482 is a peptide originally isolated from H. gigas venom that acts as a class E/R-type voltage-sensitive calcium channel blocker (IC50 = 30 nM in 192C cells expressing human class E channels). It is selective for class E/R-type over class A and class B calcium channels (IC50s = >280 and ~800 nM, respectively), as well as the voltage-gated potassium channels Kv1.1, Kv1.2, and Kv1.4 (IC50s = >140 nM for all). SNX-482 inhibits class E/R-type calcium currents in isolated rat posterior pituitary (IC50 = 4 nM), however, it has no effect on class E/R-type calcium currents in isolated rat granule cells, retinal ganglion cells, or hippocampal pyramidal cells at concentrations up to 200 nM. Intrathecal administration of SNX-482 (0.5 µg/animal) inhibits formalin-induced neurokinin-1 (NK1) receptor internalization and cfos expression in the ipsilateral dorsal horn and reduces formalin-induced paw flinching in rats.Formal Name: glycyl-L-valyl-L-alpha-aspartyl-L-lysyl-L-alanylglycyl-L-cysteinyl-L-arginyl-L-tyrosyl-L-methionyl-L-phenylalanylglycylglycyl-L-cysteinyl-L-seryl-L-valyl-L-asparaginyl-L-alpha-aspartyl-L-alpha-aspartyl-L-cysteinyl-L-cysteinyl-L-prolyl-L-arginyl-L-leucylglycyl-L-cysteinyl-L-histidyl-L-seryl-L-leucyl-L-phenylalanyl-L-seryl-L-tyrosyl-L-cysteinyl-L-alanyl-L-tryptophyl-L-alpha-aspartyl-L-leucyl-L-threonyl-L-phenylalanyl-L-seryl-L-aspartic acid, cyclic (7->21),(14->26),(20->33)-tris(disulfide), ammonium salt. Molecular Formula: C192H274N52O60S7 . XNH4. Formula Weight: 4495.0. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Water: soluble. SMILES: O=C(N[C@@H](C(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H](CCCCN[H])C(N[C@H](C(NCC(N[C@@H](CSSC[C@H](N1)C(N2CCC[C@H]2C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(NCC3=O)=O)CC(C)C)=O)=O)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC4=CC=C(O)C=C4)C(N[C@@H](CCSC)C(N[C@H](C(NCC(NCC(N[C@@H](CSSC[C@H](N3)C(N[C@@H](CC5=CNC=N5)C(N[C@@H](CO)C(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CC6=CC=C(O)C=C6)C7=O)=O)=O)CC8=CC=CC=C8)=O)CC(C)C)=O)=O)=O)C(N[C@@H](CO)C(N[C@@H](C(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CSSC[C@H](N7)C(N[C@H](C(N[C@@H](CC9=CNC%10=C9C=CC=C%10)C(N[C@@H](CC(O)=O)C(N[C@H](C(N[C@]([C@H](O)C)([H])C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(O)=O)=O)=O)CC%11=CC=CC=C%11)=O)=O)CC(C)C)=O)=O)=O)C)=O)C1=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC%12=CC=CC=C%12)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)CN[H].[NH4+]. InChi Code: InChI=1S/C192H274N52O60S7.H3N/c1-91(2)57-114-157(270)207-79-146(257)213-135-85-306-307-86-136-183(296)237-133(83-248)179(292)242-153(95(9)10)187(300)231-124(67-141(195)252)170(283)228-126(69-148(260)261)173(286)229-127(70-149(262)263)174(287)239-138(184(297)240-139(189(302)244-55-30-42-140(244)185(298)217-112(161(274)219-114)41-29-54-202-192(198)199)89-311-308-84-134(212-145(256)78-205-155(268)96(11)209-159(272)110(39-26-27-52-193)214-171(284)128(71-150(264)265)232-186(299)152(94(7)8)241-142(253)73-194)181(294)215-111(40-28-53-201-191(196)197)160(273)223-119(63-102-43-47-106(250)48-44-102)164(277)216-113(51-56-305-14)162(275)222-117(60-99-31-18-15-19-32-99)158(271)206-76-143(254)204-77-144(255)211-136)88-310-309-87-137(238-167(280)120(64-103-45-49-107(251)50-46-103)225-177(290)131(81-246)234-165(278)118(61-100-33-20-16-21-34-100)224-163(276)115(58-92(3)4)221-176(289)130(80-245)236-169(282)123(226-182(135)295)66-105-75-200-90-208-105)180(293)210-97(12)156(269)218-122(65-104-74-203-109-38-25-24-37-108(104)109)168(281)227-125(68-147(258)259)172(285)220-116(59-93(5)6)175(288)243-154(98(13)249)188(301)230-121(62-101-35-22-17-23-36-101)166(279)235-132(82-247)178(291)233-129(190(303)304)72-151(266)267,/h15-25,31-38,43-50,74-75,90-98,110-140,152-154,203,245-251H,26-30,39-42,51-73,76-89,193-194H2,1-14H3,(H2,195,252)(H,200,208)(H,204,254)(H,205,268)(H,206,271)(H,207,270)(H,209,272)(H,210,293)(H,211,255)(H,212,256)(H,213,257)(H,214,284)(H,215,294)(H,216,277)(H,217,298)(H,218,269)(H,219,274)(H,220,285)(H,221,289)(H,222,275)(H,223,273)(H,224,276)(H,225,290)(H,226,295)(H,227,281)(H,228,283)(H,229,286)(H,230,301)(H,231,300)(H,232,299)(H,233,291)(H,234,278)(H,235,279)(H,236,282)(H,237,296)(H,238,280)(H,239,287)(H,240,297)(H,241,253)(H,242,292)(H,243,288)(H,258,259)(H,260,261)(H,262,263)(H,264,265)(H,266,267)(H,303,304)(H4,196,197,201)(H4,198,199,202),1H3/p+1/t96-,97-,98+,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,152-,153-,154-,/m0./s1. InChi Key: ZSKZRLXWVVFXHM-TXGYVFHPSA-O. Origin: Synthetic.