carbonic anhydrase iv

Dorzolamide hydrochloride (MK507 hydrochloride) is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis.

hCAI/II/IV-IN-28(WAY-638358) is a potent carbonic anhydrase inhibitor with potential anticonvulsant activity.

Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) and, to a lesser extent, CAI, CAII, IV, VA, and VI (Kis = 138-1,347 nM), which may mediate its sustained vasodilatory activity. Dietary administration of chlorthalidone (8 mg per animal per day) reduces arterial hypertension and prevents or reduces ventricular hypertrophy induced by deoxycorticosterone acetate (DOCA) in salt-hypertensive rats. Formulations containing chlorthalidone have been used alone or in combination with other antihypertensive agents to lower arterial blood pressure and as adjuvants to address edema caused by cardiac or renal disorders.

Carbonic anhydrase inhibitor 8 (compound R-13) is a potent human carbonic anhydrase (hCA) with K i values of 60.7 nM, 320.7 nM, and 2298 nM for hCA I, hCA II, and hCA IV, respectively.

Human carbonic anhydrase II-IN-1 (Compound S-13) is a potent human carbonic anhydrase II (hCA II) inhibitor. Human carbonic anhydrase II-IN-1 shows Kis of 4.4 nM, 9.2 nM, 480.2 nM and 14.7 nM for hCA II, I, IV and IX, respectively. Human carbonic anhydrase II-IN-1 can be used for glaucoma research.

Human carbonic anhydrase II-IN-24 (Compound R-13) is a potent human carbonic anhydrase (hCA) inhibitor. Human carbonic anhydrase II-IN-24 shows K i s of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively.

hCAIX/XII-IN-6, an orally active carbonic anhydrase (CA) inhibitor, targets human CA isoforms hCA I, II, IV, IX, and XII with inhibition constants (K i) of 6697 nM, 2950 nM, 4093 nM, 4.1 nM, and 7.7 nM, respectively. This compound is utilized in rheumatoid arthritis (RA) research.

hCAII-IN-6 (Compound S-13), a potent inhibitor of human carbonic anhydrase II (hCA II) with a K i of 4.4 nM, also exhibits inhibitory activity against other hCA isoforms, namely I, IV, and IX, with K i values of 9.2 nM, 480.2 nM, and 14.7 nM, respectively. It is utilized in glaucoma research [1].

Compound R-13, also known as hCAII-IN-7, is a powerful inhibitor of human carbonic anhydrase (hCA), exhibiting inhibition constants (Ki) of 60.7 nM for hCA I, 320.7 nM for hCA II, 2298 nM for hCA IV, and 35.2 nM for hCA IX, respectively [1].

DPP IV/hCA II-IN-1 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA), exhibiting an IC50 of 0.049 μM for DPP IV and K_i values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively [1].

hCAIX/VII-IN-1 is a selective inhibitor of human carbonic anhydrase isoforms VII and IX, displaying inhibitory activity against hCA I, II, IV, VII, and IX with respective K_i values of 336.2 nM, 185.8 nM, 1055 nM, 35.6 nM, and 28.0 nM. This compound is applicable in cancer and neurological disease research [1].

N-Desethyl Brinzolamide oxalate functions as a dual inhibitor targeting Carbonic anhydrase II and Carbonic anhydrase IV, exhibiting inhibitory concentrations (IC50) of 1.28 nM and 128 nM, respectively [1].

O-Desmethyl Brinzolamide hydrochloride (compound 6a), a potent metabolite derived from Brinzolamide, serves as a carbonic anhydrase (CA) inhibitor. It exhibits a dissociation constant (Kd) of 0.136 nM for CA II and an inhibitory concentration (IC50) of 165 nM for CA IV [1].