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Cat. No.: HY-11076

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GI 181771

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

For research use only. We do not sell to patients.

CAS No.: 305366-98-7
Formula: C₃₄H₃₁N₅O₆
Molecular Weight:605.64

Storage:

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

Data Sheet (275 KB)

GI 181771 Chemical Structure

CAS No.: 305366-98-7

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

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

IC₅₀ & Target

Target: Cholecystokinin 1 receptor^[1]

All Cholecystokinin Receptor Isoforms :

CCKAR
CCKBR

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]

Chemical Information

CAS No. 305366-98-7
Molecular Weight 605.64
Formula C₃₄H₃₁N₅O₆
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Myer JR, et al. Species- and dose-specific pancreatic responses and progression in single- and repeat-dose studies with GI181771X: a novel cholecystokinin 1 receptor agonist in mice, rats, and monkeys. Toxicol Pathol. 2014 Jan;42(1):260-74. [Content Brief]

[2]. Roses AD, et al. Stimulation of cholecystokinin-A receptors with Gl181771X: a failed clinical trial that did not test the pharmacogenetic hypothesis for reduction of food intake. Clin Pharmacol Ther. 2009 Apr;85(4):362-5. [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.

Keywords

100 mg

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