Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 1H-Benzimidazole-6-carboxylicacid, 5-methyl-2-[[(3-methyl-2-pyridinyl)methyl]sulfinyl]-, methyl ester
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Purity: 98.0%
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78090-11-6

78090-11-6 structure

78090-11-6 structure

Name: Picoprazole
Chemical Name: methyl 6-methyl-2-[(3-methylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole-5-carboxylate
CAS Number: 78090-11-6
Molecular Formula: C₁₇H₁₇N₃O₃S
Molecular Weight: 343.40000
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Proton Pump
Create Date: 2018-08-16 19:33:48
Modify Date: 2024-01-11 19:02:14
Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.

Name	methyl 6-methyl-2-[(3-methylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole-5-carboxylate
Synonyms	Picoprazolum methyl 6-methyl-2-[[(3-methyl-2-pyridyl)methyl]sulfinyl]-5-benzimidazolecarboxylate Picoprazol Picoprazole Picoprazole (INN)

Description	Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Proton Pump Research Areas >> Metabolic Disease
Target	IC50: 3.1±0.4 μM (H+/K+-ATPase)[1]
In Vitro	Picoprazole inhibits the H+/K+-ATPase activity in a concentration-dependent manner. The IC50 value is 3.1±0.4 μM[1]. Picoprazole is a specific inhibitor of H+/K+-ATPase and binds to 100-kDa polypeptides of the enzyme, dose dependently inhibited opening of the Cl- conductance by Cu2+-o-phenanthroline, indicating that the Cl- conductance is part of the function of the H+/K+-ATPase[2]. The inhibitory effect of the three benzimidazole derivatives Timoprazole, Picoprazole, and Omeprazole on histamine and dbcAMP stimulated 14C-aminopyrine accumulation (H+ secretion) has been studied in isolated and enriched guinea-pig parietal cells. All compounds tested inhibit H+ secretion in a concentration dependent manner with IC50 values of 8.5±1.9 μM for Timoprazole, 3.9±0.7 μM for Picoprazole, and 0.13±0.03 μM for Omeprazole[3].
References	[1]. Beil W, et al. Inhibition of partially purified H⁺/K⁺-ATPase from guinea-pig isolated and enriched parietal cells by substituted benzimidazoles. Br J Pharmacol. 1984 Jul;82(3):651-7. [2]. Takeguchi N, et al. Disulfide cross-linking of H,K-ATPase opens Cl- conductance, triggering proton uptake in gastric vesicles. Studies with specific inhibitors. J Biol Chem. 1986 Feb 25;261(6):2560-6. [3]. Sewing KF, et al. Effect of substituted benzimidazoles on acid secretion in isolated and enriched guinea pig parietal cells. Gut. 1983 Jun;24(6):557-60.

Density	1.41g/cm3
Boiling Point	597.1ºC at 760 mmHg
Molecular Formula	C₁₇H₁₇N₃O₃S
Molecular Weight	343.40000
Flash Point	314.9ºC
Exact Mass	343.09900
PSA	104.15000
LogP	3.53480
Index of Refraction	1.684
Storage condition	2-8℃