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ACT 709478

Chemical Structure : ACT 709478

CAS No.: 1838651-58-3

ACT 709478 (Apinocaltamide, ACT709478)

Catalog No.: PC-62008Not For Human Use, Lab Use Only.

Apinocaltamide (ACT 709478) is a potent, selective, orally-bioavailable, brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Apinocaltamide (ACT 709478) is a potent, selective, orally-bioavailable, brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively.
ACT 709478 displays >100-fold selectivity over Cav1.2 channels.
ACT 709478 shows a significant decrease of the seizure severity in vivo (100 mg/kg, p.o.).

Physicochemical Properties

M.Wt 425.415
Formula C22H18F3N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)-phenyl)acetamide

References

1. Bezençon O, et al. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b01236.

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