GLPBio

Ca2+ channel agonist 1

Catalog No.: GC30977Purity:>99.50%
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 .

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Ca2+ channel agonist 1
Cas No.: 1402821-24-2
10mM (in 1mL DMSO)In Stock
$152.00
1
1mgIn Stock
$90.00
1
5mgIn Stock
$195.00
1
10mgIn Stock
$280.00
1
25mgIn Stock
$441.00
1

Citas (Citations)

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    Nature
    641, 529–536 (2025)
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    628, 630–638 (2024)
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    632, 686–694 (2024)
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    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    388(6745) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    34, 683–706 (2024)
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    31, 1291–1307 (2021)

Descripción (Description)

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.

Protocolo (Protocol)

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.

Documentos del producto (Product Documents)

Purity:>99.50%Appearance:A solid

Propiedades químicas (Chemical Properties)

N.º CAS
1402821-24-2
SMILES
CC[C@@H](NC1=NC(NCC2=CC=CC=C2)=C3C(N(CCC)C=N3)=N1)CO
Fórmula molecular
C19H26N6O
Peso molecular
354.45
Solubilidad
DMSO : 50 mg/mL (141.06 mM);Water : < 0.1 mg/mL (insoluble)
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

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