Ca2+ channel agonist 1 |
| Catalog No.GC30977 |
El agonista 1 del canal Ca2+ es un agonista del canal Ca2+ de tipo N y un inhibidor de Cdk2, con EC50 de 14,23 μM y 3,34 μM, respectivamente, y se utiliza como un tratamiento potencial para la disfunciÓn de las terminales nerviosas motoras .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1402821-24-2
Sample solution is provided at 25 µL, 10mM.
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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.
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].
[1]. Liang M, et al. Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist. ACS Med Chem Lett. 2012 Oct 1;3(12):985-990.
Cell experiment: | 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. |
References: [1]. Liang M, et al. Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist. ACS Med Chem Lett. 2012 Oct 1;3(12):985-990. | |
| Cas No. | 1402821-24-2 | SDF | |
| Canonical SMILES | CC[C@@H](NC1=NC(NCC2=CC=CC=C2)=C3C(N(CCC)C=N3)=N1)CO | ||
| Formula | C19H26N6O | M.Wt | 354.45 |
| Solubility | DMSO : 50 mg/mL (141.06 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8213 mL | 14.1064 mL | 28.2127 mL |
| 5 mM | 0.5643 mL | 2.8213 mL | 5.6425 mL |
| 10 mM | 0.2821 mL | 1.4106 mL | 2.8213 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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