1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Cav 3.2 inhibitor 2

Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain.

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Cav 3.2 inhibitor 2 Chemical Structure

Cav 3.2 inhibitor 2 Chemical Structure

CAS No. : 2878598-92-4

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Description

Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain[1].

IC50 & Target

IC50: 0.09339 μM (-80mV Cav3.2), 1.109 μM (-110mV Cav3.2), 0.2167 μM (Cav3.1)[1]

In Vitro

Cav 3.2 inhibitor 2 (0.3 μM) shows a produced inhibition of Cav3.2 comparable to that of pimozide[1].
Cav 3.2 inhibitor 2 (1 and 10 μM; 90 min) shows a binding affinity to D2 receptor significantly less than pimozide[1].
Cav 3.2 inhibitor 2 (0.01-10 μM) inhibits T channels isoforms with IC50s of 0.09339, 1.109 and 0.2167 μM for -80mV Cav3.2, -110mV Cav3.2 and Cav3.1, respectively[1].

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

In Vivo

Cav 3.2 inhibitor 2 (1-10 mg/kg; i.p. 30 min before i.pl. Na2S) affects the Na2S-induced pain in vivo[1].
Cav 3.2 inhibitor 2 (10 mg/kg; i.p. 7 days after oxaliplatin treatment) affects oxaliplatin-induced allodynia in vivo[1].

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

Animal Model: Mice with Na2S intraplantar (i.pl.) administration[1]
Dosage: 1, 3 and 10 mg/kg
Administration: Intraperitoneal injection; 1-10 mg/kg 30 min before i.pl. Na2S
Result: Almost completely blocked the Na2S-induced colonic pain and referred hyperalgesia.
Animal Model: Wild-type (WT) or Cav3.2-kockout (KO) C57BL/6 mice with oxaliplatin (OHP) injection[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 10 mg/kg on day 7 after oxaliplatin treatment
Result: Attenuated the oxaliplatin-induced allodynia in WT C57BL/6 mice, while showed no effect on KO mice.
Molecular Weight

517.65

Formula

C32H37F2N3O

CAS No.
SMILES

O=C1N(CCCCC2=CC=CC(F)=C2)C3=CC=CC=C3N1C4CCN(CCCCC5=CC=CC(F)=C5)CC4

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Storage

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

Purity & Documentation
References
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Cav 3.2 inhibitor 2 Related Classifications

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Cav 3.2 inhibitor 2
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HY-151451
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