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Referencia número: HY-186122

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CCK2R agonist-1

CCK2R agonist-1 (Compound 2S) is a CCK2R agonist, with an IC₅₀ of 48 nM against wild-type CCK-2R and an IC₅₀ of 450 nM against mutant CCK-2R (N353L). CCK2R agonist-1 stimulates the production of inositol phosphate. The changes in pH and HDC induced by CCK2R agonist-1 in mice are comparable to those induced by the full-length peptide agonist Gastrin. CCK2R agonist-1 can be used in studies of gastric diseases and pain.

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₂₆H₃₃N₅O₂
Peso molecular:447.57

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

CCK2R agonist-1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
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Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

CCKBR

48 nM (IC₅₀)

Ver todos los productos específicos de isoformas Cholecystokinin Receptor :

CCKAR
CCKBR

In Vitro

CCK2R agonist-1 binds to wild-type CCK-2R expressed in COS-7 cells, with an IC₅₀ value of 48 ± 3.6 nM^[1].
CCK2R agonist-1 binds to the N353L mutant CCK-2R expressed in COS-7 cells, with an IC₅₀ value of 450 ± 61 nM^[1].
CCK2R agonist-1 (1 × 10^-5 M; 1 h) stimulates inositol phosphate (IP) production in COS-7 cells expressing wild-type hCCK-2R, reaching 77% of the maximal level induced by CCK-8^[1].
CCK2R agonist-1 stimulates IP production in COS-7 cells expressing wild-type mouse CCK-2R, reaching 92±7.5% of the maximum stimulation induced by CCK-8, with an EC₅₀ value of 0.4 nM^[1].

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

In Vivo

Subcutaneous injection of CCK2R agonist-1 induces changes in pH and HDC in mice that are comparable to those elicited by the full-length peptide agonist Gastrin^[1].

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

Chemical Information

Peso molecular 447.57
Fòrmula C₂₆H₃₃N₅O₂
SMILES

CC1=CC(NC(N[C@H]2N=C(N3[C@@H](C)C[C@@H](C)C[C@H]3C)C4=CC=CC=C4N(C)C2=O)=O)=CC=C1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Kopin AS, et al. Identification of a series of CCK-2 receptor nonpeptide agonists: sensitivity to stereochemistry and a receptor point mutation. Proc Natl Acad Sci U S A. 2003;100(9):5525-5530. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Actividad biológica
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- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias

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CCK2R agonist-1

Ver todos los productos específicos de isoformas Cholecystokinin Receptor