ProTx-I
Based on 1 Customer Validation
ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.15%
- CAS 番号: 484598-35-8
- 分子式: C171H245N53O47S6
- 分子量:3987.49
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Calcium Channel アイソフォーム固有の製品をすべて表示
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生物活性
|
T-type calcium channel |
Nav1.2 104 nM (IC50) |
Nav1.6 21 nM (IC50) |
Nav1.7 95 nM (IC50) |
KV2.1 411 nM (IC50) |
TRPA1 389 nM (IC50) |
hNav1.5 358 nM (IC50) |
ProTx-I (0.01-10 μM; ~7-30 min) potently inhibits Ba2+ currents through hCav3.1-expressing Xenopus laevis oocytes with an IC50 of 0.20 μM, causes voltage-dependent inhibition and a small positive shift in activation potential, and exhibits partial to nearly irreversible binding[2].
ProTx-I (0.1-10 μM; ~2-7 min) weakly inhibits Ba2+ currents through hCav3.2-expressing Xenopus laevis oocytes with an IC50 of 31.8 μM, does not alter channel activation properties, and exhibits fully reversible binding[2].
ProTx-I (multiple concentrations) shows drastically reduced sensitivity when the domain IV S3-S4 linker of hCav3.1 is replaced with that of hCav3.2, resulting in an IC50 of 17.8 μM in hCav3.1/S3S4-expressing Xenopus laevis oocytes[2].
ProTx-I (multiple concentrations) shows increased sensitivity when the domain IV S3-S4 linker of hCav3.2 is replaced with that of hCav3.1, resulting in an IC50 of 15.8 μM in hCav3.2/S3S4-expressing Xenopus laevis oocytes[2].
ProTx-I (70 nM) inhibits heterologously expressed Cav3.1 voltage-gated calcium channels by shifting their voltage dependence of activation to more positive potentials, with an apparent IC50 of 70 nM during weak depolarizations[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 484598-35-8
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性状 Solid
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分子量 3987.49
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分子式 C171H245N53O47S6
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Color white
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配列
Glu-Cys-Arg-Tyr-Trp-Leu-Gly-Gly-Cys-Ser-Ala-Gly-Gln-Thr-Cys-Cys-Lys-His-Leu-Val-Cys-Ser-Arg-Arg-His-Gly-Trp-Cys-Val-Trp-Asp-Gly-Thr-Phe-Ser (Disulfide bridge:Cys2-Cys16;Cys9-Cys21;Cys15-Cys28)
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シーケンスの短縮
ECRYWLGGCSAGQTCCKHLVCSRRHGWCVWDGTFS (Disulfide bridge:Cys2-Cys16;Cys9-Cys21;Cys15-Cys28)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 100 mg/mL (25.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (297 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Rupasinghe DB, et al. Mutational analysis of ProTx-I and the novel venom peptide Pe1b provide insight into residues responsible for selective inhibition of the analgesic drug target NaV1.7. Biochem Pharmacol. 2020;181:114080. [Content Brief]
[2]. Ohkubo T, et al. Tarantula toxin ProTx-I differentiates between human T-type voltage-gated Ca2+ Channels Cav3.1 and Cav3.2. J Pharmacol Sci. 2010;112(4):452-458. [Content Brief]
[3]. Priest BT, et al. ProTx-I and ProTx-II: gating modifiers of voltage-gated sodium channels. Toxicon. 2007;49(2):194-201. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2508 mL | 1.2539 mL | 2.5078 mL | 6.2696 mL |
| 5 mM | 0.0502 mL | 0.2508 mL | 0.5016 mL | 1.2539 mL | |
| 10 mM | 0.0251 mL | 0.1254 mL | 0.2508 mL | 0.6270 mL | |
| 15 mM | 0.0167 mL | 0.0836 mL | 0.1672 mL | 0.4180 mL | |
| 20 mM | 0.0125 mL | 0.0627 mL | 0.1254 mL | 0.3135 mL | |
| 25 mM | 0.0100 mL | 0.0502 mL | 0.1003 mL | 0.2508 mL |
ProTx-I 関連分類
HY-P1073 関連分類
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