Guangxitoxin 1E

Guangxitoxin-1E is a specific inhibitor of the Kv current of β-cells, can enhance the glucose-dependent intracellular calcium elevations and increases the glucose-dependent insulin secretion. It is considered as a useful tool for the investigation of type 2 diabetes.

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Guangxitoxin 1E(CAS 1233152-82-3)

CAT No: R0935

CAS No: 1233152-82-3

Synonyms/Alias: Guangxitoxin 1E;1233152-82-3;AKOS027470252;DA-63966;PD079860;

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M.F/FormulaC178H248N44O45S7
M.W/Mr.3949
SequenceOne Letter Code:EGECGGFWWKCGSGKPACCPKYVCSPKWGLCNFPMP
Three Letter Code:H-DL-Glu-Gly-DL-Glu-DL-Cys(1)-Gly-Gly-DL-Phe-DL-Trp-DL-Trp-DL-Lys-DL-Cys(2)-Gly-DL-Ser-Gly-DL-Lys-DL-Pro-DL-Ala-DL-Cys(3)-DL-Cys(1)-DL-Pro-DL-Lys-DL-Tyr-DL-Val-DL-Cys(2)-DL-Ser-DL-Pro-DL-Lys-DL-Trp-Gly-DL-Leu-DL-Cys(3)-DL-Asn-DL-Phe-DL-Pro-DL-Met-DL-Pro-OH
Labeling TargetKv2.1 / Kv2.2 channel
AppearanceWhite lyophilized solid
Purity>98%
ActivityInhibitor
Source#Synthetic
Long-term Storage ConditionsSoluble in water
Solubility-20 °C
InChIInChI=1S/C178H248N44O45S7/c1-95(2)70-118-159(247)214-131(165(253)208-124(77-139(184)226)163(251)209-125(73-99-34-11-8-12-35-99)175(263)219-65-28-49-137(219)171(259)203-117(59-69-268-6)174(262)222-68-31-50-138(222)178(266)267)92-272-271-91-130-167(255)216-133-94-274-270-90-128(213-158(246)115(56-58-147(235)236)195-142(229)83-189-150(238)108(183)55-57-146(233)234)153(241)190-81-140(227)188-82-141(228)198-119(71-98-32-9-7-10-33-98)160(248)206-123(76-103-80-187-111-41-18-15-38-107(103)111)162(250)207-122(75-102-79-186-110-40-17-14-37-106(102)110)161(249)200-112(42-19-23-60-179)157(245)212-129(154(242)193-86-145(232)199-126(87-223)152(240)192-84-143(230)196-116(45-22-26-63-182)173(261)218-64-27-46-134(218)168(256)194-97(5)149(237)211-130)89-269-273-93-132(215-172(260)148(96(3)4)217-164(252)120(72-100-51-53-104(225)54-52-100)204-155(243)113(43-20-24-61-180)201-170(258)136-48-30-67-221(136)177(133)265)166(254)210-127(88-224)176(264)220-66-29-47-135(220)169(257)202-114(44-21-25-62-181)156(244)205-121(151(239)191-85-144(231)197-118)74-101-78-185-109-39-16-13-36-105(101)109/h7-18,32-41,51-54,78-80,95-97,108,112-138,148,185-187,223-225H,19-31,42-50,55-77,81-94,179-183H2,1-6H3,(H2,184,226)(H,188,227)(H,189,238)(H,190,241)(H,191,239)(H,192,240)(H,193,242)(H,194,256)(H,195,229)(H,196,230)(H,197,231)(H,198,228)(H,199,232)(H,200,249)(H,201,258)(H,202,257)(H,203,259)(H,204,243)(H,205,244)(H,206,248)(H,207,250)(H,208,253)(H,209,251)(H,210,254)(H,211,237)(H,212,245)(H,213,246)(H,214,247)(H,215,260)(H,216,255)(H,217,252)(H,233,234)(H,235,236)(H,266,267)
InChI KeySZVUKNYCMKWHNH-UHFFFAOYSA-N
References

In addition to being more potent than hanatoxin or stromatoxin, this peptide, Guangxitoxin-1E (GxTX-1E) had higher specificity for Kv2 channels, inhibiting Kv4.3 channels with an 8-fold lower potency and without significant effect on Kv1 or Kv3 family channels. The high selectivity of GxTX-1E for Kv2 makes it an attractive tool for studying the function of Kv2 channels in various types of neurons.

Kv2 Channel Regulation of Action Potential Repolarization and Firing Patterns in Superior Cervical Ganglion Neurons and Hippocampal CA1 Pyramidal Neurons

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