APETx2

APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.

Product information

CAS Number: 713544-47-9

Molecular Weight: 4561.04

Formula: C196H280N54O61S6

Chemical Name: 2-(2-{[1-(2-{[34-(4-aminobutyl)-52-{2-[2-(2-aminoacetamido)-3-hydroxybutanamido]propanamido}-19,69-dibenzyl-28-(butan-2-yl)-13,75,96-tris(3-carbamimidamidopropyl)-40-(carbamoylmethyl)-99-(carboxymethyl)-60,87,102-tris(1-hydroxyethyl)-4,37,49,81-tetrakis(hydroxymethyl)-16,25,72,90-tetrakis[(4-hydroxyphenyl)methyl]-22-[(1H-indol-3-yl)methyl]-66-(2-methylpropyl)-3,6,12,15,18,21,24,27,30,33,36,39,42,45,48,51,59,62,65,68,71,74,77,80,83,86,89,92,95,98,101,104,110,117-tetratriacontaoxo-54,55,112,113,119,120-hexathia-2,5,11,14,17,20,23,26,29,32,35,38,41,44,47,50,58,61,64,67,70,73,76,79,82,85,88,91,94,97,100,103,109,116-tetratriacontaazapentacyclo[55.53.7.4⁴⁶,⁷⁸.0⁷,¹¹.0¹⁰⁵,¹⁰⁹]121n-115-yl]formamido}-3-hydroxybutanoyl)pyrrolidin-2-yl]formamido}propanamido)butanedioic acid

Smiles: CC(C)CC1NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC2=CC=C(O)C=C2)NC(=O)C(CCCNC(N)=N)NC(=O)C2CSSCC3NC(=O)C(CO)NC(=O)C(CSSCC(NC(=O)C(NC(=O)CNC1=O)C(C)O)C(=O)NC(CSSCC(NC(=O)C(CO)NC(=O)C1CCCN1C(=O)C(CCCNC(N)=N)NC(=O)C(CC1=CC=C(O)C=C1)NC(=O)C(CC1=CC=CC=C1)NC(=O)C(CC1=CNC4=CC=CC=C14)NC(=O)C(CC1=CC=C(O)C=C1)NC(=O)C(NC(=O)CNC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC(N)=O)NC(=O)CNC3=O)C(C)CC)C(=O)N1CCCC1C(=O)NC(C(C)O)C(=O)NC(CC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC1=CC=C(O)C=C1)C(=O)NC(C(C)O)C(=O)NCC(=O)NC(CO)C(=O)N2)C(=O)NC(C(C)O)C(=O)N1CCCC1C(=O)NC(C)C(=O)NC(CC(O)=O)C(O)=O)NC(=O)C(C)NC(=O)C(NC(=O)CN)C(C)O

InChiKey: HEHYILNFEUDIQC-UHFFFAOYSA-N

InChi: InChI=1S/C196H280N54O61S6/c1-12-94(4)152-186(303)230-125(71-107-48-56-112(263)57-49-107)169(286)229-126(72-108-77-209-114-34-20-19-33-113(108)114)170(287)228-122(67-103-31-17-14-18-32-103)167(284)227-123(69-105-44-52-110(261)53-45-105)165(282)223-118(38-25-61-208-196(204)205)190(307)248-62-26-40-141(248)183(300)235-133(86-254)177(294)241-139-92-317-316-91-138(181(298)247-157(101(11)259)192(309)250-64-28-39-140(250)182(299)215-95(5)158(275)232-129(193(310)311)75-151(273)274)239-180(297)137-90-315-313-88-135(236-159(276)96(6)216-187(304)154(98(8)256)242-144(265)76-198)179(296)234-132(85-253)176(293)237-134(163(280)213-79-146(267)218-127(73-143(199)264)171(288)233-131(84-252)175(292)221-115(35-21-22-58-197)160(277)211-81-148(269)243-152)87-312-314-89-136(178(295)222-117(37-24-60-207-195(202)203)164(281)225-124(70-106-46-54-111(262)55-47-106)168(285)226-121(66-102-29-15-13-16-30-102)166(283)224-119(65-93(2)3)162(279)212-82-149(270)244-155(99(9)257)188(305)240-137)238-174(291)130(83-251)219-147(268)80-214-185(302)153(97(7)255)245-173(290)120(68-104-42-50-109(260)51-43-104)217-145(266)78-210-161(278)116(36-23-59-206-194(200)201)220-172(289)128(74-150(271)272)231-189(306)156(100(10)258)246-184(301)142-41-27-63-249(142)191(139)308/h13-20,29-34,42-57,77,93-101,115-142,152-157,209,251-263H,12,21-28,35-41,58-76,78-92,197-198H2,1-11H3,(H2,199,264)(H,210,278)(H,211,277)(H,212,279)(H,213,280)(H,214,302)(H,215,299)(H,216,304)(H,217,266)(H,218,267)(H,219,268)(H,220,289)(H,221,292)(H,222,295)(H,223,282)(H,224,283)(H,225,281)(H,226,285)(H,227,284)(H,228,287)(H,229,286)(H,230,303)(H,231,306)(H,232,275)(H,233,288)(H,234,296)(H,235,300)(H,236,276)(H,237,293)(H,238,291)(H,239,297)(H,240,305)(H,241,294)(H,242,265)(H,243,269)(H,244,270)(H,245,290)(H,246,301)(H,247,298)(H,271,272)(H,273,274)(H,310,311)(H4,200,201,206)(H4,202,203,207)(H4,204,205,208)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

APETx2 (i.t. or i.m. application, 0.022 to 2.2 µM) resulted in a potent and complete reversal of established mechanical hypersensitivity in the complete Freund's adjuvant (CFA) inflammatory pain model.

Products are for research use only. Not for human use.