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^[1].

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.

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.

447.57

C₂₆H₃₃N₅O₂

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

Room temperature in continental US; may vary elsewhere.

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

• [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.