Smartox Biotechnology
 
작성일 : 13-06-24
[Smartox Biotechnology] 화학합성의 각종 ASIC Channel Blocker Peptide Toxin (1)
Psalmotoxin-1 (PcTx1, Pi-theraphotoxin-Pc1a) / APETx2
 
화학합성의 각종 ASIC Channel Blocker Peptide Toxin (1)
 
ASIC channel 연구에 유용한 유독 생물 유래의 합성 peptide toxin 입니다. 화학합성 peptide이기 때문에
endotoxin 오염의 걱정이 없습니다.
 
 
Psalmotoxin 1 - PcTx1
 
Psalmotoxin-1 (PcTx1, Pi-theraphotoxin-Pc1a) has been isolated from the venom of the Spider Psalmopoeus cambridgei
(Trinidad chevron tarantula). This toxin is known to block potently (IC50 = 1 nM) and selectively the H+-gated sodium
channel ASIC1a (acid-sensitive ion channel 1a). The blockage is rapid and reversible. The toxin can distinguish between
the two ASIC1 splice variants ASIC1a and ASIC1b. Psalmotoxin 1 loses its capacity to block ASIC1a as soon as this subunit is associated with another member of the family (ASIC2a or ASIC3). PcTx1 demonstrates an analgesic effect in acute
and neuropathic pain models.
 
Details
AA sequence:
 
Glu-Asp-Cys3-Ile-Pro-Lys-Trp-Lys-Gly-Cys10-Val-Asn-Arg-His-Gly-Asp-Cys17-Cys18-Glu-Gly-Leu-
Glu-Cys23-Trp-Lys-Arg-Arg-Arg-Ser-Phe-Glu-Val-Cys33-Val-Pro-Lys-Thr-Pro-Lys-Thr
 
 
(Disulfide bonds between Cys3-Cys18, Cys10-Cys23  & Cys17-Cys33 )
Length (aa):
 
40
Formula:
C200H312N62O57S6
Molecular Weight:
 
4690.82 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
CAS number:
Not available
Source:
 
Synthetic
Purity rate:
 
> 98%
 
References
1. Lazdunski, M., et al. (2000) Isolation of a tarantula toxin specific for a class of proton-gated Na+ channels, J Biol Chem.
2. Darbon, H., et al. (2003) Recombinant production and solution structure of PcTx1, the specific peptide inhibitor of
   ASIC1a proton-gated cation channels, Protein SciPubMed link
 
 
APETx2
 
APETx2 is a toxin that was originally isolated from Anthopleura elegantissima (Sea anemone). APETx2 selectively blocks
the H(+)-gated sodium channel ASIC3 (ACCN3). The blockage is rapid and reversible. This toxin does not block isoform
ASIC1a and isoform ASIC1b of ASIC1 (ACCN2), nor ASIC2 (ACCN1). It also inhibits the heteromeric ASIC2b-ASIC3
channel, and has less affinity for ASIC1b-ASIC3, ASIC1a-ASIC3, and no effect on the ASIC2a-ASIC3 channels. IC50 is
63 nM on ASIC3 channel. IC50 is 117 nM on ASIC2b-ASIC3 heteromeric channel. IC50 is 0.9 µM on ASIC1b-ASIC3
heteromeric channel. IC50 is 2 µM on ASIC1a-ASIC3 heteromeric channel.
 
Details
AA sequence:
 
H-Gly-Thr-Ala-Cys4-Ser-Cys6-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys20-Pro-
Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys30-Arg-Tyr-Phe-Leu-Gly-Thr-Cys37-Cys38-Thr-Pro-Ala-
Asp-OH
 
 
(Disulfide bonds between Cys4-Cys37, Cys6-Cys30   & Cys20-Cys38 )
Length (aa):
 
42
Formula:
C196H280N54O61S6
Molecular Weight:
 
4561.13 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
CAS number:
Not available
Source:
 
Synthetic
Purity rate:
 
> 95%
 
Smartox's citations
1. Peigneur S, et al. (2012) A natural point mutation changes both target selectivity and mechanism of action of sea
   anemone toxins. FASEB J. PubMed link
2. Blanchard MG, Rash LD, Kellenberger S. (2011) Inhibition of voltage-gated Na(+) currents in sensory neurons by the
   sea anemone toxin APETx2. Br J Pharmacol. PubMed link
3. Tsuchimochi H, Yamauchi K, McCord JL, Kaufman MP. (2011) Blockade of Acid Sensing Ion Channels Attenuates the
   Augmented Exercise Pressor Reflex in Rats with Chronic Femoral Artery Occlusion. J Physiol. PubMed link
 
Reference
1. Delaunay A., et al. (2012) Human ASIC3 channel dynamically adapts its activity to sense the extracellular pH in both
   acidic and alkaline directions. PNAS. PubMed link
2. Chagot B., et al. (2005) Solution structure of APETx2, a specific peptide inhibitor of ASIC3 proton-gated channels,
   Protein Sci. PubMed link
3. Diochot S., et al. (2004) A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in
   sensory neurons. EMBO J. PubMed link
 
 
Ordering informations
Catalog No.
Product Name
Size
 13PCT001
PcTx1
 0.1mg, 0.5mg & 1.0mg
07APE002
APETx2
 0.1mg, 0.5mg & 1.0mg
 
* 다른 사이즈나 bulk 공급도 가능하오니 별도로 문의하여 주십시오.
 
 
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