1. GPCR/G Protein Neuronal Signaling
  2. Cholecystokinin Receptor
  3. GI 181771

GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.

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GI 181771

GI 181771 Chemical Structure

CAS No. : 305366-98-7

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Description

GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.

IC50 & Target

Target: Cholecystokinin 1 receptor[1]

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.8 nM
Compound: A, G1181771X
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
[PMID: 25862198]
CHO EC50
10 pM
Compound: A, G1181771X
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
[PMID: 25862198]
CHO EC50
13 pM
Compound: A, G1181771X
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
[PMID: 25862198]
CHO EC50
190 pM
Compound: A, G1181771X
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
[PMID: 25862198]
CHO EC50
2.4 pM
Compound: A, G1181771X
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.316 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.316 nM (Rvb = 7 to 14 pM)
[PMID: 25862198]
CHO EC50
283 nM
Compound: 1, GI181771X
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
[PMID: 20851601]
CHO EC50
63.8 nM
Compound: 1, GI181771X
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
[PMID: 20851601]
CHO IC50
105 nM
Compound: A, G1181771X
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
[PMID: 25862198]
CHO IC50
128 nM
Compound: A, G1181771X
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
[PMID: 25862198]
CHO IC50
131 nM
Compound: 1, GI181771X
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
[PMID: 20851601]
CHO IC50
2.7 nM
Compound: A, G1181771X
Displacement of [125I]BDZ2 from CCK2R (unknown origin) expressed in CHO cells
Displacement of [125I]BDZ2 from CCK2R (unknown origin) expressed in CHO cells
[PMID: 25862198]
CHO IC50
5.6 nM
Compound: A, G1181771X
Displacement of [125I]CCK from CCK2R (unknown origin) expressed in CHO cells
Displacement of [125I]CCK from CCK2R (unknown origin) expressed in CHO cells
[PMID: 25862198]
CHO IC50
52.6 nM
Compound: 1, GI181771X
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
[PMID: 20851601]
Molecular Weight

605.64

Formula

C34H31N5O6

CAS No.
SMILES

O=C(O)C1=CC=CC(NC(N[C@H]2C(N(CC(N(C(C)C)C3=CC=CC=C3)=O)C4=CC=CC=C4N(C5=CC=CC=C5)C2=O)=O)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GI 181771
Cat. No.:
HY-11076
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