Apinocaltamide
Based on 1 Customer Validation
Apinocaltamide (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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.59%
- No. CAS: 1838651-58-3
- Fòrmula: C22H18F3N5O
- Peso molecular:425.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas Calcium Channel
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Actividad biológica
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Cav1.2 2410 nM (IC50) |
CaV3.1 6.4 nM (IC50) |
Cav3.2 18 nM (IC50) |
CaV3.3 7.5 nM (IC50) |
Apinocaltamide (Compound 66b) blocks Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. Apinocaltamide blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM). Apinocaltamide blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM[1].
Apinocaltamide 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male juvenile DBA/2J mice (22-24 days old)[1]
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Dosage:100, 300 mg/kg, 1 hour or 3 hours before exposure to the stimulus.
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Administration:P.O., for 12 hours
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Result:Decreased the cumulative duration of absence-like seizures over the next 12 h period by 93%.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1838651-58-3
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Appearance Solid
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Peso molecular 425.41
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Fòrmula C22H18F3N5O
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Color White to off-white
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SMILES
O=C(NC1=NN(CC2=NC=C(C#N)C=C2)C=C1)CC3=CC=C(C4(C(F)(F)F)CC4)C=C3
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Synonyms
ACT-709478
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : ≥ 125 mg/mL (293.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (4.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3507 mL | 11.7534 mL | 23.5067 mL | 58.7668 mL |
| 5 mM | 0.4701 mL | 2.3507 mL | 4.7013 mL | 11.7534 mL | |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3507 mL | 5.8767 mL | |
| 15 mM | 0.1567 mL | 0.7836 mL | 1.5671 mL | 3.9178 mL | |
| 20 mM | 0.1175 mL | 0.5877 mL | 1.1753 mL | 2.9383 mL | |
| 25 mM | 0.0940 mL | 0.4701 mL | 0.9403 mL | 2.3507 mL | |
| 30 mM | 0.0784 mL | 0.3918 mL | 0.7836 mL | 1.9589 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5877 mL | 1.4692 mL | |
| 50 mM | 0.0470 mL | 0.2351 mL | 0.4701 mL | 1.1753 mL | |
| 60 mM | 0.0392 mL | 0.1959 mL | 0.3918 mL | 0.9794 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7346 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2351 mL | 0.5877 mL |
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