Talatisamine
CAS No. : 20501-56-8
Price and Availability of
CAS No. : 20501-56-8
| Size | Price | Stock |
|---|---|---|
| 5mg | $65 | In-stock |
| 10mg | $110 | In-stock |
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| Cat. No. : | HY-N0663 |
| M.Wt: | 421.57 |
| Formula: | C24H39NO5 |
| Purity: | >98 % |
| Solubility: | DMSO : 50 mg/mL (ultrasonic) |
Introduction of
20501-56-8
:
Talatisamine (10-200 μM) inhibits Ca2+-dependent mPTP opening in isolated rat heart mitochondria in a concentration-dependent manner in vitro, and its activity is weaker than that in rat liver mitochondria[1].
Talatisamine (10-200 μM) exhibits enhanced concentration-dependent inhibition of Ca2+-dependent mPTP opening in isolated rat liver mitochondria in the presence of cyclosporin A (CsA)[1].
Talatisamine (50-200 μM) inhibits Fe2+/ascorbic acid-induced MDA production in isolated rat liver mitochondria in vitro in a concentration-dependent manner[1].
Talatisamine (10-100 μM) inhibits Fe2+/ascorbic acid-induced lipid peroxidation (LPO) in isolated rat liver mitochondria in a concentration-dependent manner in vitro, with the maximum inhibitory effect observed at 100 μM[1].
Talatisamine exhibits no inhibitory effect on voltage-gated Na+ or Ca2+ currents at concentrations up to 3 mM[2]. In Vivo:Talatisamine (1 mg/kg; i.v.; single dose; 2-8 mg/kg; p.o.; single dose) exhibits rapid elimination in male ICR mice following intravenous or oral administration, with absolute oral bioavailability ranging from 65.0% to 79.2% across tested doses[2].
Talatisamine is an orally active cyclophilin D activator isolated from the roots of Aconitum carmichaeli Debx. Talatisamine exerts biological functions by activating cyclophilin D, inhibiting Ca2+-dependent opening of the mitochondrial permeability transition pore (mPTP) (IC50=78 μM), and blocking delayed rectifier K+ channels (IC50=146 μM). Talatisamine possesses both antioxidant and membrane-stabilizing properties, effectively inhibits lipid peroxidation and protects mitochondrial membrane function. Talatisamine exhibits multiple activities including antiarrhythmic, hypotensive, anti-inflammatory, anticancer and neuroprotective effects. Talatisamine finds applications in the research of ischemic diseases, rheumatoid arthritis, inflammation-related diseases and Alzheimer's disease[1][2][3].
In Vitro:Talatisamine (10-200 μM) inhibits Ca2+-dependent mPTP opening in isolated rat liver mitochondria in a concentration-dependent manner, with an IC50 of 78 μM[1].Talatisamine (10-200 μM) inhibits Ca2+-dependent mPTP opening in isolated rat heart mitochondria in a concentration-dependent manner in vitro, and its activity is weaker than that in rat liver mitochondria[1].
Talatisamine (10-200 μM) exhibits enhanced concentration-dependent inhibition of Ca2+-dependent mPTP opening in isolated rat liver mitochondria in the presence of cyclosporin A (CsA)[1].
Talatisamine (50-200 μM) inhibits Fe2+/ascorbic acid-induced MDA production in isolated rat liver mitochondria in vitro in a concentration-dependent manner[1].
Talatisamine (10-100 μM) inhibits Fe2+/ascorbic acid-induced lipid peroxidation (LPO) in isolated rat liver mitochondria in a concentration-dependent manner in vitro, with the maximum inhibitory effect observed at 100 μM[1].
Talatisamine exhibits no inhibitory effect on voltage-gated Na+ or Ca2+ currents at concentrations up to 3 mM[2]. In Vivo:Talatisamine (1 mg/kg; i.v.; single dose; 2-8 mg/kg; p.o.; single dose) exhibits rapid elimination in male ICR mice following intravenous or oral administration, with absolute oral bioavailability ranging from 65.0% to 79.2% across tested doses[2].
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