Mambalgin-1

ASIC1a & 1b channel blocker

酸敏感離子通道ASIC1a & 1b通道阻斷劑

Mambalgin-1 was initially isolated by Sylvie Diochot and collaborators from the venom of the black mamba (Dendroaspis polylepis polylepis). is a potent and selective blocker of acid-sensing ion channels (ASIC). ASIC channels have been demonstrated to be implied in pain pathways and appear to be promising therapeutic targets.   rapidly and reversibly inhibits recombinant homomeric ASIC1a (IC₅₀=55 nM) and heteromeric ASIC1a+ASIC2a (IC₅₀=246 nM) or ASIC1a+ASIC2b channels (IC₅₀=61 nM) but also human channels hASIC1b (IC₅₀=192 nM) and  hASIC1a+hASIC1b (IC₅₀=72nM).

 belongs to the family of three-finger toxins and has no sequence/structural homology with either PcTx1 or APETx2.  differs from mambalgin-2 by one amino acid. Both have demonstrated a similar activity. has no effect on ASIC2a, ASIC3, ASIC1a+ASIC3 and ASIC1b+ASIC3 channels, as well as on TRPV1, P2X2, 5-HT3A, Nav1.8, Cav3.2 and Kv1.2 channels.

Fig 1: Dose-response curve of the effect of synthetic #MAM001 on ASIC1a current recorded in Xenopus oocytes. In this system, an IC₅₀ of 21 nM was determined.

技術(shù)資料

氨基酸序列：

LKC³YQHGKVVTC¹²HRDMKFC¹⁹YHNTGMPFRNLKLILQGC³⁷SSSC⁴¹SETENNKC⁴⁹C⁵⁰STDRC⁵⁵NK-OH

二硫鍵：Cys³-Cys¹⁹, Cys¹²-Cys³⁷, Cys⁴¹-Cys⁴⁹, Cys⁵⁰-Cys⁵⁵

長(zhǎng)度 (aa)： 57

分子式： C₂₇₂H₄₂₉N₈₅O₈₄S₁₀ 

分子量：6554.59 Da

外觀：White lyophilized solid

可溶性：water or saline buffer

CAS 號(hào)：not available

來(lái)源：Synthetic

純度：> 98%

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