TRPV1-Tat (trifluoroacetate salt)

TRPV1-Tat is a peptide antagonist of transient receptor potential vanilloid 1 (TRPV1). It consists of amino acids 736-745 from the A-kinase anchor protein (AKAP)-binding domain of TRPV1 and the cell-penetrating peptide sequence from HIV Tat. TRPV1-Tat (200 µM) inhibits currents induced by heat or phorbol 12-myristate 13-acetate (PMA, Cay-10008014) in whole-cell patch-clamp assays using primary mouse dorsal root ganglia. It increases the hind paw mechanical pain threshold in rats when administered at the doses 10 or 30 µM.Formal Name: (S)-N1-((6S,9S,12S,15S,18S,24S,27S,30S,33S,36R,39S,42S,45S,49S,53S,56S)-39-((1H-indol-3-yl)methyl)-1,60-diamino-12,15-bis(4-aminobutyl)-33-benzyl-56-formyl-9,18,30,42-tetrakis(3-guanidinopropyl)-49,53-bis(hydroxyamino)-24,45-bis(4-hydroxybenzyl)-1-imino-27-isopropyl-36-(mercaptomethyl)-7,10,13,16,19,22,25,28,31,34,37,40,43,46,47,50,51,54-octadecaoxo-2,8,11,14,17,20,23,26,29,32,35,38,41,44,55-pentadecaazahexacontan-6-yl)-2-((S)-5-guanidino-2-((S)-5-guanidino-2-((S)-5-guanidino-2-(hydroxyamino)pentanamido)pentanamido)pentanamido)pentanediamide, trifluoroacetate salt. Synonyms: 736-745-Tat, Transient Receptor Potential Vanilloid 1-Tat. Molecular Formula: C127H206N50O29S . XCF3COOH. Formula Weight: 2929.4. Purity: >98%. Formulation: (Request formulation change), A solid. Peptide Sequence: KDDYRWCFRVYGRKKRRQRRR-OH. Solubility: DMF: 1 mg/ml, PBS (pH 7.2): 5 mg/ml. SMILES: OC(C(F)(F)F)=O.O=C(N[C@@H](CC(O)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC2=CNC3=C2C=CC=C3)C(N[C@@H](CS[H])C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C(C)C)C(N[C@@H](CC4=CC=C(O)C=C4)C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN[H])C(N[C@@H](CCCCN[H])C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC5=CC=CC=C5)=O)=O)=O)=O)=O)=O)[C@H](CCCCN[H])N[H]. InChi Code: InChI=1S/C127H206N50O29S.C2HF3O2/c1-67(2)99(177-111(197)85(35-20-56-155-126(145)146)167-112(198)89(58-68-22-4-3-5-23-68)172-117(203)94(66-207)176-114(200)91(61-71-64-157-76-26-7-6-24-74(71)76)173-109(195)84(34-19-55-154-125(143)144)166-113(199)90(60-70-39-43-73(179)44-40-70)171-116(202)93(63-98(184)185)174-115(201)92(62-97(182)183)170-100(186)75(131)25-8-11-47-128)118(204)175-88(59-69-37-41-72(178)42-38-69)101(187)158-65-96(181)159-77(29-14-50-149-120(133)134)102(188)160-78(27-9-12-48-129)103(189)161-79(28-10-13-49-130)104(190)162-80(30-15-51-150-121(135)136)105(191)163-82(32-17-53-152-123(139)140)107(193)168-86(45-46-95(132)180)110(196)165-81(31-16-52-151-122(137)138)106(192)164-83(33-18-54-153-124(141)142)108(194)169-87(119(205)206)36-21-57-156-127(147)148,3-2(4,5)1(6)7/h3-7,22-24,26,37-44,64,67,75,77-94,99,157,178-179,207H,8-21,25,27-36,45-63,65-66,128-131H2,1-2H3,(H2,132,180)(H,158,187)(H,159,181)(H,160,188)(H,161,189)(H,162,190)(H,163,191)(H,164,192)(H,165,196)(H,166,199)(H,167,198)(H,168,193)(H,169,194)(H,170,186)(H,171,202)(H,172,203)(H,173,195)(H,174,201)(H,175,204)(H,176,200)(H,177,197)(H,182,183)(H,184,185)(H,205,206)(H4,133,134,149)(H4,135,136,150)(H4,137,138,151)(H4,139,140,152)(H4,141,142,153)(H4,143,144,154)(H4,145,146,155)(H4,147,148,156),(H,6,7)/t75-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,99-,/m0./s1. InChi Key: HEGOLKOOICSRRY-NRBGWQPWSA-N.