ACT-709478


Catalog No. Size PriceQuantity
M20057-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.

Product information

CAS Number: 1838651-58-3

Molecular Weight: 425.41

Formula: C22H18F3N5O

Chemical Name: N-{1-[(5-cyanopyridin-2-yl)methyl]-1H-pyrazol-3-yl}-2-{4-[1-(trifluoromethyl)cyclopropyl]phenyl}acetamide

Smiles: N#CC1=CN=C(CN2C=CC(NC(=O)CC3C=CC(=CC=3)C3(CC3)C(F)(F)F)=N2)C=C1

InChiKey: LSYANGLAZUZYFX-UHFFFAOYSA-N

InChi: InChI=1S/C22H18F3N5O/c23-22(24,25)21(8-9-21)17-4-1-15(2-5-17)11-20(31)28-19-7-10-30(29-19)14-18-6-3-16(12-26)13-27-18/h1-7,10,13H,8-9,11,14H2,(H,28,29,31)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 125 mg/mL (293.83 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

ACT-709478 (Compound 66b) blocks Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. ACT-709478 blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM). ACT-709478 blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM. ACT-709478 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:

ACT-709478 (Compound 66b, 100, 300 mg/kg, p.o., 12 hours) potently decreases the cumulative duration of absence-like seizures in mice.

Products are for research use only. Not for human use.

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