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Cav 3.2 inhibitor 4

Cat. No. M42165
Cav 3.2 inhibitor 4 Structure
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Biological Activity

Cav 3.2 inhibitor 4 is a potent, peripherally restricted, selective T-type calcium channel (Cav3.2) inhibitor, with an IC50 of 0.6 μM.

Chemical Information
Molecular Weight 459.41
Formula C21H32Cl2N4O3
CAS Number 1416984-93-4
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Santiago Ponce Aix et al. Lancet Respir Med. Combination lurbinectedin and doxorubicin versus physician's choice of chemotherapy in patients with relapsed small-cell lung cancer (ATLANTIS): a multicentre, randomised, open-label, phase 3 trial

[2] Anna Manzo et al. Front Oncol. Lurbinectedin in small cell lung cancer

[3] Somayeh Mirlohi et al. Br J Pharmacol. Inhibition of human recombinant T-type calcium channels by phytocannabinoids in vitro

[4] Gang Fan et al. Aging Cell. Age attenuates the T-type CaV 3.2-RyR axis in vascular smooth muscle

[5] Fumiko Sekiguchi et al. Br J Pharmacol. AKAP-dependent sensitization of Ca(v) 3.2 channels via the EP(4) receptor/cAMP pathway mediates PGE(2) -induced mechanical hyperalgesia

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