2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. Calciseptine TFA

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.

For research use only. We do not sell to patients.

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Calciseptine TFA

Calciseptine TFA Chemical Structure

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Calciseptine TFA Related Antibodies

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Description

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[1][2].

IC50 & Target[1]

Cav1.2

92 nM (IC50)

In Vitro

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.

Calciseptine TFA Related Antibodies
In Vivo

Calciseptine (100 nM; perfusion; continuous; 7 minutes) TFA inhibits contraction and spares automaticity of
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.
Molecular Weight

7036.12 (free base)

Formula

C299H468N90O87S10.xC2HF3O2
Appearance

Solid

Color

White to off-white

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)
Sequence Shortening

RICYIHKASLPRATKTCVENTCYKMFIRTQREYISERGCGCPTAMWPYQTECCKGDRCNK (Disulfide bridge:Cys3-Cys22;Cys17-Cys39;Cys41-Cys52; Cys53-Cys58)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL

*"≥" means soluble, but saturation unknown.

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This equation is commonly abbreviated as: C1V1 = C2V2

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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Calciseptine TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CalciseptineCalcium ChannelCa2+ channelsCa channelsL-type calcium channelsCav1.2 selectivityCav1.3 resistanceNegative inotropyHeart automaticitySnake venom toxinInhibitorinhibitorinhibit

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