Description
Ro18-5362 is the less active prodrug of Ro 18-5364. Even at concentrations as high as 0.1 mM Ro 18-5362 fails to affect significantly (H++K+)-ATPase activity and associated proton translocation.
Product information
CAS Number: 101387-97-7
Molecular Weight: 395.52
Formula: C22H25N3O2S
Chemical Name: 2-{[(4-methoxy-3-methylpyridin-2-yl)methyl]sulfanyl}-5,5,7,7-tetramethyl-1H,5H,6H,7H-indeno[5,6-d]imidazol-6-one
Smiles: CC1C(CSC2NC3=CC4=C(C=C3N=2)C(C)(C)C(=O)C4(C)C)=NC=CC=1OC
InChiKey: RUTMNCYLHDVUCJ-UHFFFAOYSA-N
InChi: InChI=1S/C22H25N3O2S/c1-12-17(23-8-7-18(12)27-6)11-28-20-24-15-9-13-14(10-16(15)25-20)22(4,5)19(26)21(13,2)3/h7-10H,11H2,1-6H3,(H,24,25)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Marked differences are seen between Ro 18-5364 (sulfoxide) and Ro18-5362 (sulfide) with regard to inhibitory activity. Even at concentrations as high as 0.1 mM Ro18-5362 fails to affect significantly (H++K+)-ATPase activity and associated proton translocation. The sulfoxide Ro 18-5364, a potential metabolite of the IND Ro18-5362, is a powerful inhibitor of gastric mucosal (H++K+)-ATPase, decreasing enzymatic activity with an apparent Ki of 0.1 μM.
References:
- Sigrist-Nelson K, et al. Ro 18-5364, a potent new inhibitor of the gastric (H+ + K+)-ATPase. Eur J Biochem. 1987 Jul 15;166(2):453-9.
- Sigrist-Nelson K, et al. Gastric (H+ + K+)-ATPase: modulation of the inhibitory properties of the novel potent antisecretagogue Ro 18-5364 by sulfhydryl reagents and nucleotides. FEBS Lett. 1986 Mar 3;197(1-2):187-91.
Products are for research use only. Not for human use.
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