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.
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- Pureza: 97.55%
- Fòrmula: C299H468N90O87S10.xC2HF3O2
- Peso molecular:7036.12 (free base)
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Almacenamiento:
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)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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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.
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Animal Model:Isolated hearts from mice[1]
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Dosage:100 nM
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Administration:perfusion; continuous; 7 minutes
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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.
Chemical Information
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Appearance Solid
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Peso molecular 7036.12 (free base)
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Fòrmula C299H468N90O87S10.xC2HF3O2
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Color White to off-white
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Sequence
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)
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Sequence Shortening
RICYIHKASLPRATKTCVENTCYKMFIRTQREYISERGCGCPTAMWPYQTECCKGDRCNK (Disulfide bridge:Cys3-Cys22;Cys17-Cys39;Cys41-Cys52; Cys53-Cys58)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Solvente y solubilidad
H2O : ≥ 100 mg/mL
* "≥" means soluble, but saturation unknown.
Pureza y Documentación
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Ficha de datos (309 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Calciseptine TFA Related Classifications
HY-P3269A Related Classifications
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