화학합성의 Sodium Channel Blocker Peptide Toxin(1)
본문
화학 합성의 각종 Sodium Channel Blocker Peptide Toxin (1)
Sodium channel 연구에 유용한 유독 생물 유래의 합성 peptide toxin 입니다. 화학합성 peptide이기 때문에
endotoxin 오염의 걱정이 없습니다.
Protoxin I (ProTx-1)
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 TTX sensitive Nav channels such 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.
Details
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AA sequence: |
|
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 |
|
Disulfide bridges: |
|
Cys2-Cys16, Cys9-Cys21, Cys15-Cys28 |
|
Length (aa): |
|
35 |
|
Formula: |
|
C171H245N53O47S6 |
|
Molecular Weight: |
|
3987.50 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
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Water or saline buffer |
|
CAS number: |
|
Not available |
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Source: |
|
Synthetic |
|
Purity rate: |
|
> 95 % |
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.
GsAF-I
GsAF-I (also termed β-theraphotoxin-Gr1b) was originally isolated from the venom of Grammostola rosea spider. This
peptide toxin is reported to block the following voltage-gated sodium channels: Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6 and Nav1.7 with respective IC50 values of 0.4, 0.6, 1.3, 0.3, 1.2 and 0.04 μM. In addition, the toxin blocks the hERG1
isoform with an IC50 value of 4.8 μM.
Details
|
AA sequence: |
|
Tyr-Cys2-Gln-Lys-Trp-Leu-Trp-Thr-Cys9-Asp-Ser-Glu-Arg-Lys-Cys15-Cys16-Glu-Asp-Met-Val-
Cys21-Arg-Leu-Trp-Cys25-Lys-Lys-Arg-Leu-NH2 |
|
|
|
(Disulfide bonds between Cys2-Cys16, Cys9-Cys21, and Cys15-Cys25) |
|
Length (aa): |
|
29 |
|
Formula: |
|
C160H245N47O41S7 |
|
Molecular Weight: |
|
3707.48 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
|
Aqueous buffer |
|
CAS number: |
|
Not available |
|
Source: |
|
Synthetic |
References
1. Elisa Redaelli, et al. (2010) Target Promiscuity and Heterogeneous Effects of Tarantula Venom Peptides Affecting Na+
GsAF-II
GsAF-II (also termed Kappa-theraphotoxin-Gr2c) was originally isolated from the venom of Grammostola rosea spider. This
peptide toxin has antinociceptive and antiarrhythmic effects in mammals. The peptide is reported to block the following
voltage-gated sodium channels: Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6 and Nav1.7 with IC50 values of, respectively,
5.7, 12, 24, 4, 6.6 and 1.3 μM. This peptide also blocks hERG1 with an IC50 value of 4.7 μM.
Details
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AA sequence: |
|
Tyr-Cys2-Gln-Lys-Trp-Met-Trp-Thr-Cys9-Asp-Glu-Glu-Arg-Lys-Cys15-Cys16-Glu-Gly-Leu-Val-
Cys21-Arg-Leu-Trp-Cys25-Lys-Lys-Lys-Ile-Glu-Trp-OH |
|
|
|
(Disulfide bonds between Cys2-Cys16, Cys9-Cys21, and Cys15-Cys25) |
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Length (aa): |
|
31 |
|
Formula: |
|
C176H261N47O45S7 |
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Molecular Weight: |
|
3979.78 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
|
Aqueous buffer |
|
CAS number: |
|
Not available |
|
Source: |
|
Synthetic |
References
1. Elisa Redaelli, et al. (2010) Target Promiscuity and Heterogeneous Effects of Tarantula Venom Peptides Affecting Na+
and K+ Ion Channels. JBC. PubMed link
Jingzhaotoxin III
Jingzhaotoxin-III (ß-TRTX-Cj1α) has been isolated initially from the Chinese Tarantula spider Chilobrachys Jingzhao venom.
Jingzhaotoxin-III selectively inhibits the voltage-dependent sodium channel Nav1.5 channel with an IC50 value close to
350 nM. It is inactive on Nav1.2, Nav1.4, Nav1.6 and Nav1.7 and should therefore be considered as an interesting
research tool to discriminate between sodium channel subtypes. The toxin binds onto receptor site 4 presumably located on DIIS3-S4 linker of Nav1.5 and supposedly blocks Nav1.5 through a different mechanism than ProTx-II and Huwentoxin IV. ß-TRTX-Cj1α is composed of 36 amino acid residues including 6 cysteines cross-linked according to a C1-C4, C2-C5
and C3-C6 pattern.
Details
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AA sequence: |
|
Asp-Gly-Glu-Cys4-Gly-Gly-Phe-Trp-Trp-Lys-Cys11-Gly-Arg-Gly-Lys-Pro-Pro-Cys18-Cys19-Lys-Gly-Tyr-Ala-Cys24-Ser-Lys-Thr-Trp-Gly-Trp-Cys31-Ala-Val-Glu-Ala-Pro |
|
|
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(Disulfide bonds between Cys4-Cys19, Cys11-Cys24, and Cys18-Cys31) |
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Length (aa): |
|
36 |
|
Formula: |
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C174H241N47O46S6 |
|
Molecular Weight: |
|
3919.53 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
|
Aqueous buffer |
|
CAS number: |
|
Not available |
|
Source: |
|
Synthetic |
References
1. Yucheng Xiao, et al. (2004) Jingzhaotoxin-III, a Novel Spider Toxin Inhibiting Activation of Voltage-gated Sodium
Channel in Rat Cardiac Myocytes. JBC. PubMed link
2. Mingqiang Rong, et al. (2011) Molecular basis of the tarantula toxin jingzhaotoxin-III (Beta -TRTX-Cj1 alpha) interacting
with voltage sensors in sodium channel subtype Nav1.5. FASEB J. PubMed link
Biotinyl-Protoxin II (ProTx II)
Protoxin II (ProTx II) is a toxin that was originally isolated from Thrixopelma pruriens (Peruvian green velvet tarantula).
Protoxin II inhibits voltage-gated calcium and sodium channels (site 4). This toxin inhibits activation by shifting the
voltage-dependence of channel activation to more positive potentials. The toxin potently inhibits all sodium channel
subtypes tested (Nav1.2/SCN2A, Nav1.5/SCN5A, Nav1.7/SCN9A, and Nav1.8/SCN10A). It is approximately 15-fold more
potent on Nav1.7/SCN9A than on Nav1.5/SCN5A channels and 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.
Protoxin II also binds to phospholipids. ProTx-II, a selective inhibitor of Nav1.7 sodium channels, blocks action potential
propagation in nociceptors.
Details
|
AA sequence: |
|
Biotin-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 |
|
|
|
(Disulfide bonds between Cys2-Cys16, Cys9-Cys21 and Cys15-Cys25) |
|
Length (aa): |
|
30 |
|
Formula: |
|
C178H254N48O43S9 |
|
Molecular Weight: |
|
4052.74 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
|
Water and saline buffer |
|
CAS number: |
|
Not available |
|
Source: |
|
Synthetic |
|
Purity rate: |
|
> 95 % |
References
1. Edgerton, G. B., et al. (2008) Evidence for multiple effects of ProTxII on activation gating in Na(V)1.5, Toxicon.
2. Priest, B. T., et al. (2007) ProTx-I and ProTx-II: gating modifiers of voltage-gated sodium channels, Toxicon.
3. 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
4. Middleton, R. E., et al. (2002) Two tarantula peptides inhibit activation of multiple sodium channels, Biochemistry.
Ordering informations
|
Catalog No. |
Product Name |
Size |
|
12PTX001 |
ProTx I |
0.1mg, 0.5mg & 1.0mg |
|
12GSF001 |
GsAF-I |
0.1mg, 0.5mg & 1.0mg |
|
12GSF002 |
GsAF-II |
0.1mg, 0.5mg & 1.0mg |
|
12JZH003 |
Jingzhaotoxin-III |
0.1mg, 0.5mg & 1.0mg |
|
12PTB002 |
Biotinyl-ProTx II |
0.1mg & 0.5mg |
* 다른 사이즈나 bulk 공급도 가능하오니 별도로 문의하여 주십시오.
* 관련 제품
Hainantoxin-IV / Protoxin II (ProTx II) / Huwentoxin IV / Huwentoxin I / μ Conotoxin PIIIA (mu conotoxin PIIIA)
▣ 관련 페이지 ; Smartox Biotechnology
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Omega conotoxin MVIIA
• 화학 합성의 각종 Potassium Channel Blocker Peptide Toxin
Iberiotoxin (IbTx) / Charybdotoxin / Leiurotoxin 1 / Tamapin / Guangxitoxin 1E / ShK (Stichodactyla toxin)/
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• 화학 합성의 각종 Sodium Channel Blocker Peptide Toxin
Protoxin I (ProTx-1) / GsAF-I / GsAF-II / Jingzhaotoxin III / Biotinyl-Protoxin II (ProTx II) / Hainantoxin-IV /
Protoxin II (ProTx II) / Huwentoxin IV / Huwentoxin I / μ Conotoxin PIIIA / mu conotoxin PIIIA
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