Cav 3.2 inhibitor 3

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Cav 3.2 inhibitor 3 (Compound 4) is a potent Ca_v3.2 T-type Ca²⁺ channel inhibitor with an IC₅₀ of 0.1534 μM, and has little binding affinity to D₂ receptors.

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

Cav 3.2 inhibitor 3 Chemical Structure

CAS No. : 2878598-69-5

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

Biological Activity
Purity & Documentation
References
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Description

Cav 3.2 inhibitor 3 (Compound 4) is a potent Ca_v3.2 T-type Ca²⁺ channel inhibitor with an IC₅₀ of 0.1534 μM, and has little binding affinity to D₂ receptors^[1].

IC₅₀ & Target^[1]

Ca_v3.2

0.1534 μM (IC₅₀)

In Vivo

Cav 3.2 inhibitor 3 (Compound 4) (1-10 mg/kg; i.p.; once) potently suppresses T-channel-dependent somatic and visceral pain in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6J mice, Ca_v3.2-dependent somatic and visceral pain model^[1]
Dosage:	1, 3 and 10 mg/kg
Administration:	Intraperitoneal administration, once
Result:	Reduced the mechanical allodynia in the hindpaw and colonic pain/referred hyperalgesia following i.pl. and i.col. administrations of Na₂S, a donor of H₂S, respectively. Suppressed the i.pl. Na₂S-induced paw allodynia in a dose-dependent manner, and the maximally effective doses were roughly estimated at 10 mg/kg.

Molecular Weight

495.66

Formula

C₃₂H₃₇N₃O₂

CAS No.

2878598-69-5

SMILES

O=C1N(C2CCN(C(CCCC3=CC=CC=C3)=O)CC2)C4=CC=CC=C4N1CCCCC5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kasanami Y, et al. Discovery of pimozide derivatives as novel T-type calcium channel inhibitors with little binding affinity to dopamine D2 receptors for treatment of somatic and visceral pain. Eur J Med Chem. 2022 Aug 27;243:114716. [Content Brief]