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.
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- Formule: C26H33N5O2
- Masse moléculaire:447.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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.
In Vivo
Chemical Information
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Masse moléculaire 447.57
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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