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Home - Products - GPCR/G Protein - Calcium Channel - ACT 709478

ACT 709478

CAS No. 1838651-58-3

ACT 709478( ACT709478 )

Catalog No. M12840 CAS No. 1838651-58-3

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.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    ACT 709478
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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; displays >100-fold selectivity over Cav1.2 channels; shows a significant decrease of the seizure severity in vivo (100 mg/kg, p.o.).Epilepsy Phase 2 Clinical.
  • In Vitro
    Apinocaltamide (Compound 66b) blocks Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. Apinocaltamide blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM). Apinocaltamide blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM.Apinocaltamide also inhibits P450 enzymes with IC50s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively.
  • In Vivo
    Apinocaltamide (Compound 66b, 100, 300 mg/kg, p.o., measured 12 hours later) potently decreases the cumulative duration of absence-like seizures in mice. Animal Model:Male juvenile DBA/2J mice (22-24 days old)Dosage:100, 300 mg/kg, 1 hour or 3 hours before exposure to the stimulus.Administration:P.O., for 12 hours Result:Decreased the cumulative duration of absence-like seizures over the next 12 h period by 93%.
  • Synonyms
    ACT709478
  • Pathway
    GPCR/G Protein
  • Target
    Calcium Channel
  • Recptor
    Calcium Channel
  • Research Area
    Neurological Disease
  • Indication
    Epilepsy

Chemical Information

  • CAS Number
    1838651-58-3
  • Formula Weight
    425.415
  • Molecular Formula
    C22H18F3N5O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 125 mg/mL 293.83 mM
  • SMILES
    O=C(NC1=NN(CC2=NC=C(C#N)C=C2)C=C1)CC3=CC=C(C4(C(F)(F)F)CC4)C=C3
  • Chemical Name
    N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)-phenyl)acetamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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