Huwentoxin-IV (HWTX-IV), a tetrodotoxin-sensitive (TTX-s) Na+ channel blocker, isolated from the venom of the Chinese Bird spider Ornithoctonus huwena. A naturally modified HWTX-IV (mHWTX-IV), having a molecular mass 18 Da. lower than HWTX-IV, has also been isolated from the venom of the same spider. mHWTX-IV has been shown to have the same amino acid sequence as that of HWTX-IV, except that the N-terminal glutamic acid is replaced by pyroglutamic acid. mHWTX-IV inhibits tetrodotoxin-sensitive NaV channels of dorsal root ganglion neurons with an IC50 nearly equal to native HWTX-IV (IC50 value of 28 nM versus 26 nM). mHWTX-IV shows the same activation and inactivation kinetics seen for native HWTX-IV.nHuwentoxin-IV preferentially inhibits hNaV1.7. NaV1.7 plays a crucial role in pain transduction with familial gain of function mutations linked to several chronic pain disorders, while loss of NaV1.7 function results in congenital insensitivity to pain
产品描述
A Blocker of TTX-Sensitive NaV Channels
产品形式
Huwentoxin-IV (HWTX-IV), a tetrodotoxin-sensitive (TTX-s) Na+ channel blocker, isolated from the venom of the Chinese Bird spider Ornithoctonus huwena. A naturally modified HWTX-IV (mHWTX-IV), having a molecular mass 18 Da. lower than HWTX-IV, has also been isolated from the venom of the same spider. mHWTX-IV has been shown to have the same amino acid sequence as that of HWTX-IV, except that the N-terminal glutamic acid is replaced by pyroglutamic acid. mHWTX-IV inhibits tetrodotoxin-sensitive NaV channels of dorsal root ganglion neurons with an IC50 nearly equal to native HWTX-IV (IC50 value of 28 nM versus 26 nM). mHWTX-IV shows the same activation and inactivation kinetics seen for native HWTX-IV.nHuwentoxin-IV preferentially inhibits hNaV1.7. NaV1.7 plays a crucial role in pain transduction with familial gain of function mutations linked to several chronic pain disorders, while loss of NaV1.7 function results in congenital insensitivity to pain
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