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MedKoo Cat#: 584335 | Name: Proglumide
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Description:

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

Proglumide, also known as W-5219 and CR-242, is a cholecystokinin-1 receptor (CCK1) antagonist. Proglumide exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. Proglumide enhances the antinociceptive effect of cyclooxygenase inhibitors in diabetic rats in the formalin test. Proglumide dose dependently protected rats against acetic acid-induced increase in colon weight, diarrhea, MPO activity and colonic injury. Inhibition of CCK exerts a beneficial effect in experimental colitis.

Chemical Structure

Proglumide
Proglumide
CAS#6620-60-6 (free acid)

Theoretical Analysis

MedKoo Cat#: 584335

Name: Proglumide

CAS#: 6620-60-6 (free acid)

Chemical Formula: C18H26N2O4

Exact Mass: 334.1893

Molecular Weight: 334.42

Elemental Analysis: C, 64.65; H, 7.84; N, 8.38; O, 19.14

Price and Availability

Size Price Availability Quantity
50mg USD 350.00 2 Weeks
100mg USD 550.00 2 Weeks
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Related CAS #
99247-33-3 (sodium) 6620-60-6 (free acid)
Synonym
Proglumide; W 5219; W-5219; W-5219; CR 242; CR-242; CR242;
IUPAC/Chemical Name
Pentanoic acid, 4-(benzoylamino)-5-(dipropylamino)-5-oxo-, (+-)-
InChi Key
DGMKFQYCZXERLX-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H26N2O4/c1-3-12-20(13-4-2)18(24)15(10-11-16(21)22)19-17(23)14-8-6-5-7-9-14/h5-9,15H,3-4,10-13H2,1-2H3,(H,19,23)(H,21,22)
SMILES Code
O=C(O)CCC(NC(C1=CC=CC=C1)=O)C(N(CCC)CCC)=O
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
Ulcerative colitis is associated with altered contractile activity and transit time of colon. On the other hand, cholecystokinin (CCK) has been shown to play an important role in regulation of gastrointestinal motor function including colonic contraction and transit.

Preparing Stock Solutions

The following data is based on the product molecular weight 334.42 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
1: Ciofoaia V, Chen W, Tarek BW, Gay M, Shivapurkar N, Smith JP. The Role of a Cholecystokinin Receptor Antagonist in the Management of Chronic Pancreatitis: A Phase 1 Trial. Pharmaceutics. 2024 Apr 30;16(5):611. doi: 10.3390/pharmaceutics16050611. PMID: 38794273; PMCID: PMC11125239. 2: Abraham T, Armold M, McGovern C, Harms JF, Darok MC, Gigliotti C, Adair B, Gray JL, Kelly DF, Adair JH, Matters GL. CCK Receptor Inhibition Reduces Pancreatic Tumor Fibrosis and Promotes Nanoparticle Delivery. Biomedicines. 2024 May 7;12(5):1024. doi: 10.3390/biomedicines12051024. PMID: 38790986; PMCID: PMC11118934. 3: Varghese S, Jisha MS, Rajeshkumar KC, Gajbhiye V, Haldar N, Shaikh A. Molecular authentication, metabolite profiling and in silico-in vitro cytotoxicity screening of endophytic Penicillium ramusculum from Withania somnifera for breast cancer therapeutics. 3 Biotech. 2024 Mar;14(3):64. doi: 10.1007/s13205-023-03906-3. Epub 2024 Feb 9. PMID: 38344285; PMCID: PMC10858009. 4: Gay MD, Drda JC, Chen W, Huang Y, Yassin AA, Duka T, Fang H, Shivapurkar N, Smith JP. Implicating the cholecystokinin B receptor in liver stem cell oncogenesis. Am J Physiol Gastrointest Liver Physiol. 2024 Mar 1;326(3):G291-G309. doi: 10.1152/ajpgi.00208.2023. Epub 2024 Jan 22. PMID: 38252699; PMCID: PMC11211039. 5: Jolly G, Duka T, Shivapurkar N, Chen W, Bansal S, Cheema A, Smith JP. Cholecystokinin Receptor Antagonist Induces Pancreatic Stellate Cell Plasticity Rendering the Tumor Microenvironment Less Oncogenic. Cancers (Basel). 2023 May 18;15(10):2811. doi: 10.3390/cancers15102811. PMID: 37345148; PMCID: PMC10216345. 6: Shivapurkar N, Gay MD, He AR, Chen W, Golnazar S, Cao H, Duka T, Kallakury B, Vasudevan S, Smith JP. Treatment with a Cholecystokinin Receptor Antagonist, Proglumide, Improves Efficacy of Immune Checkpoint Antibodies in Hepatocellular Carcinoma. Int J Mol Sci. 2023 Feb 11;24(4):3625. doi: 10.3390/ijms24043625. PMID: 36835036; PMCID: PMC9965856. 7: Panganiban RAM, Yang Z, Sun M, Park CY, Kasahara DI, Schaible N, Krishnan R, Kho AT, Israel E, Hershenson MB, Weiss ST, Himes BE, Fredberg JJ, Tantisira KG, Shore SA, Lu Q. Antagonizing cholecystokinin A receptor in the lung attenuates obesity-induced airway hyperresponsiveness. Nat Commun. 2023 Jan 4;14(1):47. doi: 10.1038/s41467-022-35739-8. PMID: 36599824; PMCID: PMC9813361. 8: Bernard A, Danigo A, Mroué M, Rovini A, Richard L, Nizou A, Desmoulière A, Sturtz F, Demiot C, Bourthoumieu S. Blockade of Cholecystokinin Type 2 Receptors Prevents the Onset of Vincristine-Induced Neuropathy in Mice. Pharmaceutics. 2022 Dec 16;14(12):2823. doi: 10.3390/pharmaceutics14122823. PMID: 36559317; PMCID: PMC9788598. 9: Rabiee A, Gay MD, Shivapurkar N, Cao H, Nadella S, Smith CI, Lewis JH, Bansal S, Cheema A, Kwagyan J, Smith JP. Safety and Dosing Study of a Cholecystokinin Receptor Antagonist in Non-alcoholic Steatohepatitis. Clin Pharmacol Ther. 2022 Dec;112(6):1271-1279. doi: 10.1002/cpt.2745. Epub 2022 Sep 27. PMID: 36087237; PMCID: PMC9691615. 10: Hsu CC, Bansal S, Cao H, Smith CI, He AR, Gay MD, Li Y, Cheema A, Smith JP. Safety and Pharmacokinetic Assessment of Oral Proglumide in Those with Hepatic Impairment. Pharmaceutics. 2022 Mar 12;14(3):627. doi: 10.3390/pharmaceutics14030627. PMID: 35336003; PMCID: PMC8948956. 11: Gay MD, Cao H, Shivapurkar N, Dakshanamurthy S, Kallakury B, Tucker RD, Kwagyan J, Smith JP. Proglumide Reverses Nonalcoholic Steatohepatitis by Interaction with the Farnesoid X Receptor and Altering the Microbiome. Int J Mol Sci. 2022 Feb 8;23(3):1899. doi: 10.3390/ijms23031899. PMID: 35163821; PMCID: PMC8836891. 12: Zhao Y, Wang Q, Zeng Y, Xie Y, Zhou J. Gastrin/CCK-B Receptor Signaling Promotes Cell Invasion and Metastasis by Upregulating MMP-2 and VEGF Expression in Gastric Cancer. J Cancer. 2022 Jan 1;13(1):134-145. doi: 10.7150/jca.51854. PMID: 34976177; PMCID: PMC8692687. 13: Malchiodi ZX, Cao H, Gay MD, Safronenka A, Bansal S, Tucker RD, Weinberg BA, Cheema A, Shivapurkar N, Smith JP. Cholecystokinin Receptor Antagonist Improves Efficacy of Chemotherapy in Murine Models of Pancreatic Cancer by Altering the Tumor Microenvironment. Cancers (Basel). 2021 Sep 30;13(19):4949. doi: 10.3390/cancers13194949. PMID: 34638432; PMCID: PMC8508339. 14: Ou X, Xia T, Yang C, Yu C, Zhang S, Huang R, Chen C, Zhou C. Novel H2S donor proglumide-ADT-OH protects HUVECs from ox-LDL-induced injury through NF-κB and JAK/SATA pathway. Open Med (Wars). 2021 Sep 8;16(1):1318-1327. doi: 10.1515/med-2021-0287. PMID: 34568579; PMCID: PMC8428624. 15: Yue J, Guo D, Gao X, Wang J, Nepovimova E, Wu W, Kuca K. Deoxynivalenol (Vomitoxin)-Induced Anorexia Is Induced by the Release of Intestinal Hormones in Mice. Toxins (Basel). 2021 Jul 22;13(8):512. doi: 10.3390/toxins13080512. PMID: 34437383; PMCID: PMC8402572. 16: Kania BF, Wrońska D, Bracha U. Pain, Pathophysiological Mechanisms, and New Therapeutic Options for Alternative Analgesic Agents in Sheep: A Review and Investigation. Animals (Basel). 2021 Mar 22;11(3):909. doi: 10.3390/ani11030909. PMID: 33810059; PMCID: PMC8004948. 17: Abraham T, McGovern CO, Linton SS, Wilczynski Z, Adair JH, Matters GL. Aptamer-Targeted Calcium Phosphosilicate Nanoparticles for Effective Imaging of Pancreatic and Prostate Cancer. Int J Nanomedicine. 2021 Mar 19;16:2297-2309. doi: 10.2147/IJN.S295740. PMID: 33776434; PMCID: PMC7989532. 18: Li H, An C. Exploring the role of neurogenic pathway-linked cholecystokinin release in remote preconditioning-induced cardioprotection. Acta Cir Bras. 2020 Oct 30;35(9):e202000906. doi: 10.1590/s0102-865020200090000006. PMID: 33146235; PMCID: PMC7727451. 19: Gay MD, Safronenka A, Cao H, Liu FH, Malchiodi ZX, Tucker RD, Kroemer A, Shivapurkar N, Smith JP. Targeting the Cholecystokinin Receptor: A Novel Approach for Treatment and Prevention of Hepatocellular Cancer. Cancer Prev Res (Phila). 2021 Jan;14(1):17-30. doi: 10.1158/1940-6207.CAPR-20-0220. Epub 2020 Oct 28. PMID: 33115780; PMCID: PMC8079543. 20: Soopramanien M, Khan NA, Sagathevan K, Siddiqui R. Gut bacteria of Varanus salvator possess potential antitumour molecules. Int Microbiol. 2021 Jan;24(1):47-56. doi: 10.1007/s10123-020-00139-9. Epub 2020 Jul 31. PMID: 32737845.

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