Calciseptine TFA
Based on 1 Customer Validation
Calciseptine TFA, a polypeptide found in black mamba venom, is a selcetive Cav1.2 L-type calcium channel inhibitor with an IC50 of 92 nM. Calciseptine TFA binds to the pore domain shoulder at repeats III and IV of Cav1.2, stabilizing an inactivated conformation. Calciseptine TFA exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine TFA can be used for the research of cardiovascular diseases.
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: 97.55%
- 分子式: C299H468N90O87S10.xC2HF3O2
- 分子量:7036.12 (free base)
-
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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Calcium Channel アイソフォーム固有の製品をすべて表示
More
生物活性
|
Cav1.2 92 nM (IC50) |
Calciseptine (100 nM-1 μM) TFA potently inhibits recombinant Cav1.2-mediated L-type Ca2+ currents in HEK-293T cells with an IC50 of 92 ± 18 nM, while having no significant effect on recombinant Cav1.342α- or Cav1.342-mediated currents at concentrations up to 1 μM[1].
Calciseptine (40-1000 nM) TFA inhibits Cav1.2 channel activity in HEK293T cells and 0.2 μM reducing peak Cav1.2 current by more than half[2].
Calciseptine TFA requires Cav1.2 residues Asp1117, Val1501, Asn1113, and Ala1123 for specific blockage of Cav1.2, as mutation of these residues reduces sensitivity Calciseptine[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Langendorff perfused hearts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Isolated hearts from mice[1]
-
Dosage:100 nM
-
Administration:perfusion; continuous; 7 minutes
-
Result:Reduced left ventricular contraction amplitude from 51±3 mmHg to 9±2 mmHg.
Decreased dP/dt max (contraction velocity) from 1.7±0.2 mmHg/ms to 0.4±0.1 mmHg/ms.
Decreased dP/dt min (relaxation velocity) from -1.2±0.1 mmHg/ms to -0.1±0.1 mmHg/ms.
Left baseline diastolic pressure unchanged (8±2 mmHg vs 8±3 mmHg).
Left averaged inter-beat (RR) intervals unaffected (273±17 ms vs 271±17 ms, p > 0.05).
Caused no arrhythmias during perfusion.
化学情報
-
性状 Solid
-
分子量 7036.12 (free base)
-
分子式 C299H468N90O87S10.xC2HF3O2
-
Color White to off-white
-
配列
Arg-Ile-Cys-Tyr-Ile-His-Lys-Ala-Ser-Leu-Pro-Arg-Ala-Thr-Lys-Thr-Cys-Val-Glu-Asn-Thr-Cys-Tyr-Lys-Met-Phe-Ile-Arg-Thr-Gln-Arg-Glu-Tyr-Ile-Ser-Glu-Arg-Gly-Cys-Gly-Cys-Pro-Thr-Ala-Met-Trp-Pro-Tyr-Gln-Thr-Glu-Cys-Cys-Lys-Gly-Asp-Arg-Cys-Asn-Lys (Disulfide bridge:Cys3-Cys22;Cys17-Cys39;Cys41-Cys52; Cys53-Cys58)
-
シーケンスの短縮
RICYIHKASLPRATKTCVENTCYKMFIRTQREYISERGCGCPTAMWPYQTECCKGDRCNK (Disulfide bridge:Cys3-Cys22;Cys17-Cys39;Cys41-Cys52; Cys53-Cys58)
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
H2O : ≥ 100 mg/mL
* "≥" means soluble, but saturation unknown.
純度とドキュメンテーション
-
データシート (309 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Mesirca P, et al. Selective blockade of Cav1.2 (α1C) versus Cav1.3 (α1D) L-type calcium channels by the black mamba toxin calciseptine. Nat Commun. 2024 Jan 2;15(1):54. [Content Brief]
[2]. Gao S, et al. Structural basis for human Cav1.2 inhibition by multiple drugs and the neurotoxin calciseptine. Cell. 2023;186(24):5363-5374.e16. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Calciseptine TFA 関連分類
HY-P3269A 関連分類
Powered by Bioz