화학합성의 Calcium Channel Blocker Peptide Toxin (3)
본문
화학합성의 각종 Calcium Channel Blocker Peptide Toxin (3)
Calcium channel 연구에 유용한 유독 생물 유래의 합성 peptide toxin 입니다. 화학합성 peptide이기 때문에
endotoxin 오염의 걱정이 없습니다.
Protoxin I / ProTx-I
Blocker of voltage-gated sodium channels
Protoxin I (ProTx-I; β-theraphotoxin-Tp1a) is a toxin that was originally isolated from the venom of Thrixopelma pruriens
(Peruvian green velvet tarantula). This toxin reversibly inhibits the tetrodotoxin (TTX)-resistant channel Nav1.8 (IC50 =
27 nM) and Nav1.2, Nav1.5 and Nav1.7 with IC50 values between 50 and 100 nM. Furthermore, ProTx-I
shifts the voltage
dependence activity of T-type Cav3.1 channels (IC50= 50 nM) without affecting the voltage dependence of inactivation.
ProTx-I is a valuable tool to discriminate between Cav3.1 and Cav3.2.
Details
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AA sequence:
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Glu-Cys2-Arg-Tyr-Trp-Leu-Gly-Gly-Cys9-Ser-Ala-Gly-Gln-Thr-Cys15-Cys16-Lys-His-Leu-Val-Cys21-Ser-Arg-Arg-His-Gly-Trp-Cys28-Val-Trp-Asp-Gly-Thr-Phe-Ser
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(Disulfide bonds between Cys2-Cys16, Cys9-Cys21,
Cys15-Cys28)
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Length (aa):
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35
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Formula:
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C171H245N53O47S6
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Molecular Weight:
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3987.50 Da
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Appearance:
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White lyophilized solid
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Solubility:
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Water and saline buffer
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CAS number:
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Not available
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Source:
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Synthetic
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Purity rate:
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> 95 %
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References
1. Middelton R.E, et al. (2002) Two tarantula peptides inhibit activation of multiple sodium channels. Biochemestry.
2. Priest B.T., et al. (2007) ProTx-I and ProTx-II: gating modifiers of voltage-gated sodium channels. Toxicon. PubMed link
3. Ohkubo T, et al. (2010) Tarantula toxin ProTx-I differentiates between human T-type voltage-gated Ca2+ Channels Cav3.1
and Cav3.2. J Pharmacol Sci. PubMed link
ProTx-II
Nav1.7 selective inhibitor
ProTx-II (ProTx-2, Protoxin II) is a toxin that was originally isolated from Thrixopelma pruriens (Peruvian green velvet
tarantula). ProTx-II inhibits both tetrodotoxin-sensitive and tetrodotoxin-resistant voltage-gated sodium channels. ProTx-II
inhibits activation by shifting the voltage-dependence of channel activation to more positive potentials. ProTx-II blocks
Nav1.7 with an IC50 value of around 300 pM, Nav1.2,
Nav1.5 and Nav1.6 with IC50 values of 41 nM, 79 nM and 26 nM
respectively. It also acts on Cav3.1/CACNA1G and interacts more weakly with the related T-Type channel Cav3.2/CACNA1H
but potently inhibits the L-type calcium channel Cav1.2/CACNA1C. ProTx-II blocks action potential propagation in
nociceptors.
Details
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AA sequence:
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Tyr-Cys2-Gln-Lys-Trp-Met-Trp-Thr-Cys9-Asp-Ser-Glu-Arg-Lys-Cys15-Cys16-Glu-Gly-Met-Val- Cys21-Arg-Leu-Trp-Cys25-Lys-Lys-Lys-Leu-Trp-OH
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(Disulfide bonds between Cys2-Cys16, Cys9-Cys21 and
Cys15-Cys25)
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Length (aa):
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30
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Formula:
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C168H250N46O41S6
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Molecular Weight:
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3828.0 Da
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Appearance:
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White lyophilized solid
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Solubility:
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Water and saline buffer
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CAS number:
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484598-36-9
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Source:
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Synthetic
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Purity rate:
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> 95 %
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References
1. Klint JK., et al. (2012) Spider-venom peptides that target voltage-gated sodium channels: pharmacological tools and
potential therapeutic leads. Toxicon. PubMed link
2. Edgerton G. B., et al. (2008) Evidence for multiple effects of ProTxII on activation gating in Na(V)1.5,
Toxicon. PubMed link
3. William A., et al. (2007) ProTx-II, a selective inhibitor of Nav1.7 sodium channels, blocks action potential propagation in
nociceptors. Mol. Pharm. PubMed link
4. Priest B. T., et al. (2007) ProTx-I and ProTx-II: gating modifiers of voltage-gated sodium channels, Toxicon. PubMed link
5. Smith J. J., et al. (2005) Differential phospholipid binding by site 3 and site 4 toxins. Implications for structural variability
between voltage-sensitive sodium channel domains, J Biol Chem. PubMed link
6. Middleton R. E., et al. (2002) Two tarantula peptides inhibit activation of multiple sodium channels,
Biochemistry. PubMed link
Ordering informations
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Catalog No.
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Product Name
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Size
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07PTX001
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Protoxin I / ProTx-1
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0.1mg, 0.5mg & 1.0mg
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07PTX002
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ProTx-II
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0.1mg, 0.5mg & 1.0mg
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* 다른 사이즈나 bulk 공급도 가능하오니 별도로 문의하여 주십시오.
* 관련 제품
Maurocalcine / Huwentoxin I / ω CONOTOXIN SO-3 / ω-Conotoxin MVIIA
ω-agatoxin IVA / ω-CONOTOXIN GVIA/Omega conotoxin GVIA / ω-Conotoxin MVIIC/Omega conotoxin MVIIC / SNX482
▣ 관련 페이지 ; Smartox Biotechnology
- 이전글New peptide toxins from Smartox Biotechnology 14.03.15
- 다음글화학합성의 Potassium Channel Blocker Peptide Toxin(4) 13.12.05
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