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.
For research use only. We do not sell to patients.
- Formula: C26H33N5O2
- Molecular Weight:447.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CCKBR 48 nM (IC50) |
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. Further protocols information, click here.
In Vivo
Chemical Information
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Molecular Weight 447.57
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Formula C26H33N5O2
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CCK2R agonist-1 Related Classifications
HY-186122 Related Classifications
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Keywords
- CCK2R agonist-1
- Cholecystokinin Receptor
- wild-type human CCK-2R
- HEK293 cells
- inositol phosphate
- cholecystokinin 2 receptor
- COS-7 cells
- oxyntic mucosal histidine decarboxylase
- mouse gastric mucosa
- wild-type mouse CCK-2R
- mutant human CCK-2R (N353L)
- constitutively active mutant human CCK-2R (L325E)
- Inhibitor
- inhibitor
- inhibit