GsMTx4

GsMTx4 is a spider venom peptide that selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology. GsMTx4 significantly attenuates bladder hyperactivity.

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GsMTx4(CAS 1209500-46-8)

CAT No: HB00094

CAS No: 1209500-46-8

Synonyms/Alias: GsMTx4;1209500-46-8;GsMTx-4;H-Gly-DL-Cys(1)-DL-Leu-DL-Glu-DL-Phe-DL-Trp-DL-Trp-DL-Lys-DL-Cys(2)-DL-Asn-DL-Pro-DL-Asn-DL-Asp-DL-Asp-DL-Lys-DL-Cys(3)-DL-Cys(1)-DL-Arg-DL-Pro-DL-Lys-DL-Leu-DL-Lys-DL-Cys(2)-DL-Ser-DL-Lys-DL-Leu-DL-Phe-DL-Lys-DL-Leu-DL-Cys(3)-DL-Asn-DL-Phe-DL-Ser-DL-Phe-NH2;CHEBI:194078;HB1161;AKOS024458413;C185H273N49O45S6;CID:90488987;

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M.F/FormulaC185H273N49O45S6
M.W/Mr.4096
SequenceOne Letter Code:GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF
Three Letter Code:H-Gly-DL-Cys(1)-DL-Leu-DL-Glu-DL-Phe-DL-Trp-DL-Trp-DL-Lys-DL-Cys(2)-DL-Asn-DL-Pro-DL-Asn-DL-Asp-DL-Asp-DL-Lys-DL-Cys(3)-DL-Cys(1)-DL-Arg-DL-Pro-DL-Lys-DL-Leu-DL-Lys-DL-Cys(2)-DL-Ser-DL-Lys-DL-Leu-DL-Phe-DL-Lys-DL-Leu-DL-Cys(3)-DL-Asn-DL-Phe-DL-Ser-DL-Phe-NH2
Labeling TargetTRP Channel
AppearanceWhite lyophilised solid
Purity>98%
ActivityBlocker
Source#Synthetic
Long-term Storage ConditionsSoluble in water
Shipping ConditionRoom temperature in continental US; may vary elsewhere.
InChIInChI=1S/C185H273N49O45S6/c1-98(2)72-121-160(255)203-114(54-27-33-65-188)156(251)229-141-96-284-283-95-140-178(273)225-134(84-147(195)239)184(279)234-71-39-60-144(234)182(277)224-131(83-146(194)238)170(265)222-133(86-151(245)246)172(267)223-132(85-150(243)244)171(266)206-116(56-29-35-67-190)158(253)230-142(97-285-282-94-139(177(272)221-130(82-145(193)237)169(264)218-127(79-105-46-19-12-20-47-105)166(261)226-136(91-236)174(269)211-120(152(196)247)76-102-40-13-9-14-41-102)231-163(258)124(75-101(7)8)214-153(248)112(52-25-31-63-186)204-164(259)125(77-103-42-15-10-16-43-103)217-162(257)123(74-100(5)6)213-154(249)113(53-26-32-64-187)207-173(268)135(90-235)227-179(141)274)180(275)232-138(176(271)210-119(58-37-69-199-185(197)198)183(278)233-70-38-59-143(233)181(276)209-117(155(250)212-121)57-30-36-68-191)93-281-280-92-137(202-148(240)87-192)175(270)215-122(73-99(3)4)161(256)208-118(61-62-149(241)242)159(254)216-126(78-104-44-17-11-18-45-104)165(260)219-129(81-107-89-201-111-51-24-22-49-109(107)111)168(263)220-128(80-106-88-200-110-50-23-21-48-108(106)110)167(262)205-115(157(252)228-140)55-28-34-66-189/h9-24,40-51,88-89,98-101,112-144,200-201,235-236H,25-39,52-87,90-97,186-192H2,1-8H3,(H2,193,237)(H2,194,238)(H2,195,239)(H2,196,247)(H,202,240)(H,203,255)(H,204,259)(H,205,262)(H,206,266)(H,207,268)(H,208,256)(H,209,276)(H,210,271)(H,211,269)(H,212,250)(H,213,249)(H,214,248)(H,215,270)(H,216,254)(H,217,257)(H,218,264)(H,219,260)(H,220,263)(H,221,272)(H,222,265)(H,223,267)(H,224,277)(H,225,273)(H,226,261)(H,227,274)(H,228,252)(H,229,251)(H,230,253)(H,231,258)(H,232,275)(H,241,242)(H,243,244)(H,245,246)(H4,197,198,199)
InChI KeyWVDNTWXIIKNMHY-UHFFFAOYSA-N
References

Grammastola spatulata mechanotoxin #4 (GsMTx4) is a 35 amino acid peptide that inhibits the gating of cation selective MSCs with similar affinity in either the l or d enantiomic forms, emphasizing its lack of stereospecificity when interacting with MSCs. Cationic MSCs may belong to the Transient Receptor Potential (TRP) and/or Piezo families known to be expressed in cardiomyocytes and vascular tissue. In vitro measures of MSC activity in cardiac tissue, single cells and patch assays, show GsMTx4 activity in the range of 0.1–5 μM. GsMTx4 is a gating modifier that inhibits MSCs by clamping the membrane tension of the outer monolayer where its penetration depth, and thus its surface area contribution, is tension dependent.

GsMTx4-D is a cardioprotectant against myocardial infarction during ischemia and reperfusion

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