| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| 25mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
GI-181771X targets the cholecystokinin-1 (CCK1) receptor, a G protein-coupled receptor involved in regulating satiety, gastric emptying, and gallbladder contraction. It acts as a potent agonist at CCK1 receptors (EC50 = 6.1 nM) and concurrently as an antagonist at CCK2 receptors (IC50 = 5.6 nM), resulting in a pharmacologically distinct profile.
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| ln Vitro |
In vitro, GI-181771X demonstrates potent CCK1 receptor agonism with an EC50 of 6.1 nM. It also acts as a CCK2 receptor antagonist with an IC50 of 5.6 nM. The compound binds to CCK1 receptors with high affinity and activates downstream signaling pathways involved in satiety and gastrointestinal motility. Its unique dual pharmacology (CCK1 agonism/CCK2 antagonism) enables studies of appetite, anxiety, and pain where both receptor subtypes play opposing roles.
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| ln Vivo |
In vivo, GI-181771X effects satiation and gastric and gallbladder emptying. It has been studied in clinical trials for obesity treatment. Documented formulation-dependent gastric emptying delay (P<0.01) supports GI motility and satiation research when dosed appropriately. A Phase IIb negative weight loss trial provides an empirically validated negative control for benchmarking novel CCK1 agonists. The compound was investigated in clinical trial NCT00600743 (Effect of a CCK-1R Agonist on Food Intake in Humans).
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for CCK1 receptor agonists typically use radioligand binding assays with [¹²⁵I]CCK-8 or [³H]devazepide as labeled ligands. Membranes prepared from cells expressing human CCK1 or CCK2 receptors are incubated with the radioligand and varying concentrations of GI-181771X. Specific binding is determined by subtracting non-specific binding (defined by excess unlabeled CCK-8 or devazepide). Ki values are calculated from competition binding curves. Functional assays measure intracellular calcium mobilization or IP3 accumulation in CCK1-expressing cells.
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| Cell Assay |
Cellular assays for CCK1 receptor agonists typically use CHO or HEK293 cells expressing human CCK1 receptors. Cells are loaded with calcium-sensitive fluorescent dyes and stimulated with varying concentrations of GI-181771X. The increase in intracellular calcium is measured using fluorescence plate readers. EC50 values for receptor activation are calculated from dose-response curves. CCK-8 (sulfated) is used as a positive control. CCK2 receptor antagonism is assessed in cells expressing CCK2 receptors using similar calcium mobilization assays.
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| Animal Protocol |
In vivo animal studies for satiety and gastric emptying typically use rodent models. Rats or mice are administered GI-181771X orally or intraperitoneally at various doses. Food intake is measured over a defined period (e.g., 1-24 hours) to assess effects on satiety. Gastric emptying is measured using a test meal containing a non-absorbable marker (e.g., phenol red), and the amount remaining in the stomach is quantified. Gallbladder contraction may be assessed by measuring gallbladder volume or bile output.
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| ADME/Pharmacokinetics |
GI-181771X is orally bioavailable with good absorption following oral administration. As a small-molecule CCK1 agonist, it distributes to peripheral tissues expressing CCK1 receptors, including the gastrointestinal tract and gallbladder. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys and bile. Detailed PK parameters such as half-life, Cmax, and AUC are available from preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of GI-181771X would include acute and repeated-dose toxicity in rodents and dogs, as well as genotoxicity and safety pharmacology assessments. In clinical trials, the compound was evaluated for safety and tolerability in healthy volunteers and obese patients. The Phase IIb trial provided safety data for the compound. No significant unexpected toxicities were reported, though the compound did not demonstrate sufficient weight loss efficacy to support further development.
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| References |
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| Additional Infomation |
Gski181771 X is being studied in the clinical trial NCT00600743 (the effect of CCK-1R agonists on human food intake).
GI-181771X is a CCK1 receptor agonist investigated for obesity treatment. It has a unique dual pharmacology as a CCK1 agonist and CCK2 antagonist. The compound was developed by GlaxoSmithKline and studied in clinical trials including NCT00600743. A Phase IIb trial showed negative weight loss results, providing a validated negative control for benchmarking novel CCK1 agonists. The compound is available for research use as a pharmacological tool. |
| Molecular Formula |
C34H31N5O6
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|---|---|
| Molecular Weight |
605.63984
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| Exact Mass |
605.227
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| CAS # |
305366-98-7
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| PubChem CID |
51353551
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
5.562
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
45
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| Complexity |
1090
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| Defined Atom Stereocenter Count |
1
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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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| InChi Key |
CABBMMXFOOZVMS-PMERELPUSA-N
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| InChi Code |
InChI=1S/C34H31N5O6/c1-22(2)38(25-14-5-3-6-15-25)29(40)21-37-27-18-9-10-19-28(27)39(26-16-7-4-8-17-26)32(42)30(31(37)41)36-34(45)35-24-13-11-12-23(20-24)33(43)44/h3-20,22,30H,21H2,1-2H3,(H,43,44)(H2,35,36,45)/t30-/m0/s1
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| Chemical Name |
(S)-3-(3-(1-(2-(isopropyl(phenyl)amino)-2-oxoethyl)-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl)ureido)benzoic
acid
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| Synonyms |
GI-181771X GI181771X GI 181771X GSKI 181771XGSKI-181771X GSKI181771X.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6511 mL | 8.2557 mL | 16.5115 mL | |
| 5 mM | 0.3302 mL | 1.6511 mL | 3.3023 mL | |
| 10 mM | 0.1651 mL | 0.8256 mL | 1.6511 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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