TTA-A8
TTA-A8 (Compound 13) is a short-acting T-type calcium channel antagonist with oral activity, exhibiting an IC50 value of 31.3 nM in the FLIPR depolarization assay. TTA-A8 possesses favorable pharmacokinetic properties, making it suitable for research on epilepsy and sleep.
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- CAS. Nr.: 1146395-46-1
- Formel: C22H21F3N4O2
- Molecular Weight:430.42
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>30 μM
Compound: 13, TTA-A8
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Displacement of [3S]MK499 from human ERG in HEK293 cells
Displacement of [3S]MK499 from human ERG in HEK293 cells
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[PMID: 24900239] |
In Vivo
TTA-A8 (5 mg/kg; p.o.; single dose) exhibited moderate to high plasma clearance (CLp), low to moderate distribution volume (Vss), and short half-life (T1/2) across three preclinical species (rat, dog, rhesus)[1].
Pharmacokinetic parameters in rat, dog, rhesus[1]
| species | administration | dosage | CL (predicted)a(mL/min/kg) | CLp(observed)(mL/min/kg) | T1/2(h) | Vss (L/kg) | F (%) | plasma PB (% unbound)b |
| rat | p.o. | 5 mg/kg | 8 | 30.3 | 0.24 | 0.59 | 71 | 12.3 |
| dog | p.o. | 5 mg/kg | 13 | 11.8 | 0.81 | 0.36 | 23 | 15.5 |
| rhesus | p.o. | 5 mg/kg | 22 | 19.3 | 0.53 | 0.74 | 5 | 14.6 |