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RP-72540

Catalog No. T28612   CAS 139088-45-2
Synonyms: RPR 102681, RPR-102681, RPR102681

RP-72540 is a cholecystokinin B receptor antagonist. RP 72540 showed selectivity factors in express of 200 for CCKA versus CCKB receptors and also had high affinity for gastrin binding sites in the stomach. Administration of RP-72540 resulted in a dose-dependent inhibition of [3H]pCCK-8 binding in mouse brain homogenate. However, the relative penetration of RP-72540 into the forebrain after peripheral administration was below 0.01%.

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RP-72540 Chemical Structure
RP-72540, CAS 139088-45-2
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RP-72540 is a cholecystokinin B receptor antagonist. RP 72540 showed selectivity factors in express of 200 for CCKA versus CCKB receptors and also had high affinity for gastrin binding sites in the stomach. Administration of RP-72540 resulted in a dose-dependent inhibition of [3H]pCCK-8 binding in mouse brain homogenate. However, the relative penetration of RP-72540 into the forebrain after peripheral administration was below 0.01%.
Synonyms RPR 102681, RPR-102681, RPR102681
Molecular Weight 518.56
Formula C28H30N4O6
CAS No. 139088-45-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Bertrand P, Böhme GA, Durieux C, Guyon C, Capet M, Jeantaud B, Boudeau P, Ducos B, Pendley CE, Martin GE, et al. Pharmacological properties of ureido-acetamides, new potent and selective non-peptide CCKB/gastrin receptor antagonists. Eur J Pharmacol. 1994 Sep 12;262(3):233-45. PubMed PMID: 7813588. 2. Jensen RT. CCKB/gastrin receptor antagonists: recent advances and potential uses in gastric secretory disorders. Yale J Biol Med. 1996 May-Jun;69(3):245-59. Review. PubMed PMID: 9165693; PubMed Central PMCID: PMC2589015. 3. Bierkamp C, Kowalski-Chauvel A, Dehez S, Fourmy D, Pradayrol L, Seva C. Gastrin mediated cholecystokinin-2 receptor activation induces loss of cell adhesion and scattering in epithelial MDCK cells. Oncogene. 2002 Oct 31;21(50):7656-70. PubMed PMID: 12400008.

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Keywords

RP-72540 139088-45-2 RPR 102681 RPR-102681 RPR102681 RP72540 RP 72540 inhibitor inhibit

 

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