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Phlo1a

Mu-theraphotoxin-Phlo1a, Mu-TRTX-Phlo1a

A Blocker of NaV1.7 Channels

Cat #: STP-350
Alternative Name Mu-theraphotoxin-Phlo1a, Mu-TRTX-Phlo1a
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Synthetic peptide
    MW: 4107 Da
    Purity: >98% (HPLC)
    Effective concentration 100 nM - 1 µM.
    Sequence ACRELLGGCSKDSDCCAHLECRKKWPYHCVWDWTI.
    Modifications Disulfide bonds between Cys2-Cys16, Cys9-Cys21, and Cys15-Cys29 (by homology). Ile35 – C-terminal amidation.
    Structure
    Molecular formula C178H262N52O49S6.
    Activity PhIo1a is a blocker of NaV1.7 channel1.
    References-Activity
    1. Chow, C.Y. et al. (2015) Toxins 7, 2494.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Any other aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Phlo1a inhibits the current of NaV1.7 channels expressed in Xenopus oocytes.
      Alomone Labs Phlo1a inhibits the current of NaV1.7 channels expressed in Xenopus oocytes.
      A. Time course of Phlo1a (#STP-350) inhibition of NaV1.7 channel current. Membrane potential was held at -100 mV, current was elicited by a 100 ms voltage step to -10 mV delivered every 10 sec, and inhibited by 0.2 µM and 1 µM Phlo1a (bars), applied for 5 min and 2.5 min, respectively. B. Superimposed traces of NaV1.7 channel current upon application of control, 0.2 µM and 1 µM Phlo1a (as indicated), taken from the recording shown in A.
    References - Scientific background
    1. Chow, C.Y. et al. (2015) Toxins 7, 2494.
    2. Klint J.K. et al. (2015) Br. J. Pharmacol. 172, 2445.
    Scientific background

    Phlo1a is a voltage-gated NaV1.7 channel blocker. It is a peptide toxin originally isolated from the venom of the Australian Phlogius sp. Tarantula. It inhibits the channel’s activation through interaction with one or more voltage-sensor domains. Phlo1a inhibits human NaV1.7 channels in a concentration-dependent manner with an IC50 value of 459 nM1.

    Phlo1a is 35-residue peptide that belongs to the NaSpTx family and is considered to be a valuable research tool and a lead molecule for the development of ion channel therapeutics. To date, twelve families of NaSpTx have been recognized. Phlo1a belongs to the NaSpTx2 family and contains three disulfide bonds. The majority of tarantula-venom peptides share a highly stable inhibitor cystine knot (ICK) fold that provides resistance to chemical and thermal degradation1.

    There are nine mammalian subtypes of voltage-gated sodium (NaV) channels: NaV1.1–NaV1.9. They are transmembrane proteins responsible for propagating action potentials in excitable cells, most notably nerves and muscle. These channels are considered to be important therapeutic targets for a wide variety of pathophysiological conditions such as chronic pain, cardiac arrhythmia, and epilepsy1,2.

    Target NaV1.7 channels
    Net Peptide Content: 100%
    Lyophilized Powder
    Last update: 11/04/2021

    Phlo1a (#STP-350) is a highly pure, synthetic, and biologically active peptide toxin.

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    For research purposes only, not for human use
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