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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-103354
Proglumide sodiumCCK-A/B Receptors Antagonist -
HY-B2154
LoxiglumideCholecystokinin Receptor Antagonist -
HY-106301
DevazepideCCK Receptor Antagonist -
HY-B1330
ProglumideCCK-A/B Receptors Antagonist -
HY-103354R
Proglumide sodium (Standard)CCK-A/B Receptors Antagonist -
HY-11077
SR 146131Cholecystokinin Receptor Agonist -
HY-128878
DexloxiglumideCCKR Inhibitor -
HY-14850
SograzepideGastrin/CCK-B Antagonist -
HY-101764
LintitriptCCK1 Receptor Antagonist -
HY-17617
NastorazepideCCK-2 Receptor Antagonist -
HY-B1439B
Lorglumide sodiumCholecystokinin Receptor Antagonist -
HY-129357
CCK-B Receptor Antagonist 2Gastrin/CCK-B Antagonist
Biological Activity
Description
IC50 & Target
Target: Cholecystokinin 1 receptor[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.8 nM
Compound: A, G1181771X
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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
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[PMID: 25862198] |
| CHO | EC50 |
10 pM
Compound: A, G1181771X
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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)
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[PMID: 25862198] |
| CHO | EC50 |
13 pM
Compound: A, G1181771X
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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)
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[PMID: 25862198] |
| CHO | EC50 |
190 pM
Compound: A, G1181771X
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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)
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[PMID: 25862198] |
| CHO | EC50 |
2.4 pM
Compound: A, G1181771X
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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)
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[PMID: 25862198] |
| CHO | EC50 |
283 nM
Compound: 1, GI181771X
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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
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[PMID: 20851601] |
| CHO | EC50 |
63.8 nM
Compound: 1, GI181771X
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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
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[PMID: 20851601] |
| CHO | IC50 |
105 nM
Compound: A, G1181771X
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Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
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[PMID: 25862198] |
| CHO | IC50 |
128 nM
Compound: A, G1181771X
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Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
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[PMID: 25862198] |
| CHO | IC50 |
131 nM
Compound: 1, GI181771X
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Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
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[PMID: 20851601] |
| CHO | IC50 |
2.7 nM
Compound: A, G1181771X
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Displacement of [125I]BDZ2 from CCK2R (unknown origin) expressed in CHO cells
Displacement of [125I]BDZ2 from CCK2R (unknown origin) expressed in CHO cells
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[PMID: 25862198] |
| CHO | IC50 |
5.6 nM
Compound: A, G1181771X
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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
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Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
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[PMID: 20851601] |
Chemical Information
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CAS No. 305366-98-7
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Molecular Weight 605.64
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Formula C34H31N5O6
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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
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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.
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (82.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6511 mL | 8.2557 mL | 16.5115 mL | 41.2786 mL |
| 5 mM | 0.3302 mL | 1.6511 mL | 3.3023 mL | 8.2557 mL | |
| 10 mM | 0.1651 mL | 0.8256 mL | 1.6511 mL | 4.1279 mL | |
| 15 mM | 0.1101 mL | 0.5504 mL | 1.1008 mL | 2.7519 mL | |
| 20 mM | 0.0826 mL | 0.4128 mL | 0.8256 mL | 2.0639 mL | |
| 25 mM | 0.0660 mL | 0.3302 mL | 0.6605 mL | 1.6511 mL | |
| 30 mM | 0.0550 mL | 0.2752 mL | 0.5504 mL | 1.3760 mL | |
| 40 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 1.0320 mL | |
| 50 mM | 0.0330 mL | 0.1651 mL | 0.3302 mL | 0.8256 mL | |
| 60 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6880 mL | |
| 80 mM | 0.0206 mL | 0.1032 mL | 0.2064 mL | 0.5160 mL |
GI 181771 Related Classifications
HY-11076 Related Classifications
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