Apinocaltamide
CAS No. : 1838651-58-3
(Synonyms: ACT-709478)
| Size | Price | Stock |
|---|---|---|
| 5mg | $190 | In-stock |
| 10mg | $290 | In-stock |
| 25mg | $450 | In-stock |
| 50mg | $790 | In-stock |
| 100mg | $1350 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-112723 |
| M.Wt: | 425.41 |
| Formula: | C22H18F3N5O |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 125 mg/mL |
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[1].
IC50 & Target:IC50: 6.4 nM (Cav3.1), 18 nM (Cav3.2), 7.5 nM (Cav3.3), 2410 nM (Cav1.2)[1]
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[1].
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[1].
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[1].
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- Apinocaltamide
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- HY-112723
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