Ca2+ channel agonist 1

Cat. No.: HY-41076 Purity: 99.71%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Ca2+ channel agonist 1 Chemical Structure

CAS No. : 1402821-24-2

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 462	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 462	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CDK2

3.34 μM (EC₅₀)

N-type calcium channel

14.23 μM (EC₅₀)

In Vitro

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.

Molecular Weight

354.45

Formula

C₁₉H₂₆N₆O

CAS No.

1402821-24-2

Appearance

Solid

Color

White to off-white

SMILES

CC[C@@H](NC1=NC(NCC2=CC=CC=C2)=C3C(N(CCC)C=N3)=N1)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.71%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (252 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Cell Assay
^[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. [Content Brief]

Complete Stock Solution Preparation Table

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