GI-181771X

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525167

CAS#: 305366-98-7

Description: GI-181771X is a novel oral CCK-1 agonist. GI-181771X effects satiation and gastric and gallbladder emptying.


Chemical Structure

img
GI-181771X
CAS# 305366-98-7

Theoretical Analysis

MedKoo Cat#: 525167
Name: GI-181771X
CAS#: 305366-98-7
Chemical Formula: C34H31N5O6
Exact Mass: 605.23
Molecular Weight: 605.640
Elemental Analysis: C, 67.43; H, 5.16; N, 11.56; O, 15.85

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: GI-181771X; GI181771X; GI 181771X; GSKI 181771X;GSKI-181771X; GSKI181771X.

IUPAC/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

InChi Key: CABBMMXFOOZVMS-PMERELPUSA-N

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

SMILES Code: CC(C)N(c1ccccc1)C(=O)CN2c3ccccc3N(C(=O)[C@H](C2=O)NC(=O)Nc4cccc(c4)C(=O)O)c5ccccc5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 605.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Myer JR, Romach EH, Elangbam CS. 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. doi: 10.1177/0192623313506792. Epub 2013 Oct 31. PubMed PMID: 24178573.

2: Harikumar KG, Cawston EE, Lam PC, Patil A, Orry A, Henke BR, Abagyan R, Christopoulos A, Sexton PM, Miller LJ. Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor. J Biol Chem. 2013 Jul 19;288(29):21082-95. doi: 10.1074/jbc.M113.480715. Epub 2013 Jun 10. PubMed PMID: 23754289; PubMed Central PMCID: PMC3774375.

3: Roses AD. 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. doi: 10.1038/clpt.2008.192. Review. PubMed PMID: 19295535.

4: Berger R, Zhu C, Hansen AR, Harper B, Chen Z, Holt TG, Hubert J, Lee SJ, Pan J, Qian S, Reitman ML, Strack AM, Weingarth DT, Wolff M, Macneil DJ, Weber AE, Edmondson SD. 2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4833-7. doi: 10.1016/j.bmcl.2008.07.083. Epub 2008 Jul 24. PubMed PMID: 18684621.

5: Jordan J, Greenway FL, Leiter LA, Li Z, Jacobson P, Murphy K, Hill J, Kler L, Aftring RP. Stimulation of cholecystokinin-A receptors with GI181771X does not cause weight loss in overweight or obese patients. Clin Pharmacol Ther. 2008 Feb;83(2):281-7. Epub 2007 Jun 27. PubMed PMID: 17597711.

6: Castillo EJ, Delgado-Aros S, Camilleri M, Burton D, Stephens D, O'Connor-Semmes R, Walker A, Shachoy-Clark A, Zinsmeister AR. Effect of oral CCK-1 agonist GI181771X on fasting and postprandial gastric functions in healthy volunteers. Am J Physiol Gastrointest Liver Physiol. 2004 Aug;287(2):G363-9. PubMed PMID: 15246968.