Talatisamine
Based on 1 Customer Validation
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.
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- Pureté: 99.77%
- CAS No.: 20501-56-8
- Formule: C24H39NO5
- Masse moléculaire:421.57
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Activité biologique
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Cyclophilin D |
IKr |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | CL | Vd | Cmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[2] | 1 mg/kg | i.v. | 970.4 ng·h/mL | 986.7 ng·h/mL | 1.6 h | 1.8 h | 1.3 h | 0.1 h | 1.2 L/h/kg | 2.1 L/kg | 583.4 ng/mL | / |
| Mice[2] | 2 mg/kg | p.o. | 1261.6 ng·h/mL | 1419.6 ng·h/mL | 2.1 h | 3.2 h | 2.5 h | 0.8 h | 1.5 L/h/kg | 4.9 L/kg | 614.8 ng/mL | 65.0 % |
| Mice[2] | 4 mg/kg | p.o. | 3023.6 ng·h/mL | 3050.8 ng·h/mL | 1.6 h | 1.7 h | 1.2 h | 0.8 h | 1.4 L/h/kg | 2.4 L/kg | 1716.6 ng/mL | 77.9 % |
| Mice[2] | 8 mg/kg | p.o. | 6149.6 ng·h/mL | 6208.9 ng·h/mL | 1.6 h | 1.7 h | 1.1 h | 0.8 h | 1.3 L/h/kg | 2.0 L/kg | 3045.6 ng/mL | 79.2 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 20501-56-8
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Appearance Solid
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Masse moléculaire 421.57
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Formule C24H39NO5
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Color White to off-white
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SMILES
CO[C@@H]1C(C(N(CC)C2)C3C4)([C@@](C[C@@]5([H])[C@@H]6O)([H])[C@@]6([H])[C@@]3(C[C@@H]5OC)O)[C@@]4([H])[C@@]2(COC)CC1
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : 50 mg/mL (118.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3721 mL | 11.8604 mL | 23.7209 mL | 59.3021 mL |
| 5 mM | 0.4744 mL | 2.3721 mL | 4.7442 mL | 11.8604 mL | |
| 10 mM | 0.2372 mL | 1.1860 mL | 2.3721 mL | 5.9302 mL | |
| 15 mM | 0.1581 mL | 0.7907 mL | 1.5814 mL | 3.9535 mL | |
| 20 mM | 0.1186 mL | 0.5930 mL | 1.1860 mL | 2.9651 mL | |
| 25 mM | 0.0949 mL | 0.4744 mL | 0.9488 mL | 2.3721 mL | |
| 30 mM | 0.0791 mL | 0.3953 mL | 0.7907 mL | 1.9767 mL | |
| 40 mM | 0.0593 mL | 0.2965 mL | 0.5930 mL | 1.4826 mL | |
| 50 mM | 0.0474 mL | 0.2372 mL | 0.4744 mL | 1.1860 mL | |
| 60 mM | 0.0395 mL | 0.1977 mL | 0.3953 mL | 0.9884 mL | |
| 80 mM | 0.0297 mL | 0.1483 mL | 0.2965 mL | 0.7413 mL | |
| 100 mM | 0.0237 mL | 0.1186 mL | 0.2372 mL | 0.5930 mL |
- Talatisamine
- 20501-56-8
- Mitochondrial Metabolism
- Cyclophilin
- Potassium Channel
- ischemia
- rheumatoid arthritis
- mitochondrial membranes
- rat hippocampal neurons
- ICR mice
- delayed rectifier K+channels
- Aconitum carmichaeli Debx.
- Ca2+-dependent mitochondrial permeability transition pore
- cyclophilin D
- alzheimer's disease
- Inhibitor
- inhibitor
- inhibit