weak base

Revaprazan hydrochloride (YH1885) is the hydrochloride salt form of a lipophilic, weak base with potassium-competitive acid blocking (P-CAB) activity.

Pantoprazole sodium (Pantecta) is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole sodium is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+ K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.

Glypromate acetate is a neuroprotective agent, is a weak NMDA receptor agonist.

M40 acetate is a potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.

AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

Ilaprazole sodium (IY-81149 sodium) , a substituted benzimidazole prodrug, is a selective and irreversible proton pump inhibitor. A weak base, Ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+ K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.

Sitamaquine hydrochloride (WR 6026) is an orally active 8-aminoquinoline analog with antileishmanial activity. This compound inhibits mitochondrial complex II (succinate dehydrogenase) and is characterized by its lipophilic weak base properties. It rapidly accumulates in the acidic compartments of Leishmania parasites, predominantly localizing within the acidocalcisomes.

Prostaglandin B2 (PGB2) is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the rabbit at relatively high doses (5 ug/kg). [1]

Nepaprazole Na is the salt form of Nepaprazole Free Base, also known as TY-11345, is a proton pump inhibitor potentially for treatment of gastric ulcer. TY-11345 potently inhibited H+ K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes; and the inhibitory effect was enhanced under weak acid conditions, the IC50 (concentrations that inhibit the enzyme activity by 50%) being 5.8 microM and 9.9 microM at pH 6.0 and pH 7.4, respectively. TY-11345 should be useful for the clinical treatment of peptic ulcer diseases.

Sucrose phosphorylase, a bacterial transglucosidase, catalyzes the conversion of sucrose and phosphate into α-D-glucose-1-phosphate and D-fructose. This enzyme can also hydrolyze glucosylated sucrose into α-D-glucose or transfer the glucosyl group to a receptor's hydroxyl group, resulting in new α-D-glucoside products. Its enzymatic activity towards the base, substrate, and product is weak [1].

Tetramethylammonium fluoride tetrahydrate (TMAF) is a quaternary ammonium salt. It serves as a weak base and a fluoride ion source in various organic reactions, such as nucleophilic substitutions, deprotection of functional groups, and ring-opening polymerizations. Unlike other sources of fluoride, TMAF is compatible with numerous functional groups, making it a versatile reagent in synthetic chemistry. Additionally, TMAF is utilized as a fluorinating agent in medicinal chemistry for the preparation of radioactive tracers and in biochemistry for protein modification. The tetrahydrate form of TMAF is more stable and easier to handle than its anhydrous counterpart.