Ca2+ channel agonist 1
Based on 1 publication(s) in Google Scholar
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
For research use only. We do not sell to patients.
- Purity: 98.87%
- CAS No.: 1402821-24-2
- Formula: C19H26N6O
- Molecular Weight:354.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Ca2+ channel agonist 1
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Biological Activity
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CDK2 3.34 μM (EC50) |
N-type calcium channel 14.23 μM (EC50) |
Ca2+ channel agonist 1 (Compound 13d) is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively. Ca2+ channel agonist 1 exhibits a ca. 2-fold increased agonism and a 22-fold decreased cdk2 kinase activity versus the standard, (R)-roscovitine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1402821-24-2
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Appearance Solid
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Molecular Weight 354.45
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Formula C19H26N6O
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Color White to off-white
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SMILES
CC[C@@H](NC1=NC(NCC2=CC=CC=C2)=C3C(N(CCC)C=N3)=N1)CO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 50 mg/mL (141.06 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, 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: ≥ 2.5 mg/mL (7.05 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.
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.
Protocol
Briefly, the pipet solution consists of 70 nM Cs2SO4, 60 mM CsCl, 1 mM MgCl2, and 10 mM HEPES at pH 7.4. Cultured cells are bathed in a saline composed of 130 mM choline chloride (ChCl), 10 mM tetraethylammonium chloride (TEA-Cl), 2 mM CaCl2, 1 mM MgCl2, and 10 mM HEPES at pH 7.4. Patch pipettes are fabricated from borosilicate glass, and capacitive currents and passive membrane responses to voltage commands are subtracted. Currents are amplified by an amplifier, filtered at 5 kHz, and digitized at 10 kHz for subsequent analysis. A liquid junction potential of −11.3 mV is subtracted during recordings. To measure effects on calcium channel tail currents, the tail current integral is measured before and after application of a derivative (including Ca2+ channel agonist 1), with the integral of each trace being normalized to its peak.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 | 2.8213 mL | 14.1064 mL | 28.2127 mL | 70.5318 mL |
| 5 mM | 0.5643 mL | 2.8213 mL | 5.6425 mL | 14.1064 mL | |
| 10 mM | 0.2821 mL | 1.4106 mL | 2.8213 mL | 7.0532 mL | |
| 15 mM | 0.1881 mL | 0.9404 mL | 1.8808 mL | 4.7021 mL | |
| 20 mM | 0.1411 mL | 0.7053 mL | 1.4106 mL | 3.5266 mL | |
| 25 mM | 0.1129 mL | 0.5643 mL | 1.1285 mL | 2.8213 mL | |
| 30 mM | 0.0940 mL | 0.4702 mL | 0.9404 mL | 2.3511 mL | |
| 40 mM | 0.0705 mL | 0.3527 mL | 0.7053 mL | 1.7633 mL | |
| 50 mM | 0.0564 mL | 0.2821 mL | 0.5643 mL | 1.4106 mL | |
| 60 mM | 0.0470 mL | 0.2351 mL | 0.4702 mL | 1.1755 mL | |
| 80 mM | 0.0353 mL | 0.1763 mL | 0.3527 mL | 0.8816 mL | |
| 100 mM | 0.0282 mL | 0.1411 mL | 0.2821 mL | 0.7053 mL |