carbonic anhydrase i (ca-i)

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.

AChE/hCA I-IN-1 (Compound L3) is an inhibitor of acetylcholinesterase (AChE) and carbonic anhydrase (CA), effectively inhibiting AChE, hCA I, and hCA II with IC50 values of 302 nM, 265 nM, and 283 nM, respectively.

hCAIX/XII-IN-9 (compound 8) is a potent inhibitor of carbonic anhydrase (CA), with Ki values of 1658 nM for hCA I, 184.8 nM for hCA II, 8.9 nM for hCA IX, and 64.8 nM for hCA XII.

Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor targeting Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib. It exhibits anti-inflammatory and analgesic properties. The IC50 values for COX-1 and COX-2 are 10.4 μM and 50 nM, respectively. The Ki values for binding to various Carbonic Anhydrase isoforms are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII).

Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor that targets Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib, exhibiting anti-inflammatory and analgesic properties. The IC50 values of Anti-inflammatory agent 68 for COX-1 and COX-2 are 12.6 μM and 60 nM, respectively. It binds to different Carbonic Anhydrase isoforms with Ki values of 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII).

Antibacterialagent 215 (Compound 3b) acts as an inhibitor of carbonic anhydrase (CA), with Ki values of 17.61, 5.14, and 43.74 nM for hCA I, hCA II, and AChE, respectively. It exhibits antitubercular activity with an MIC of 62.5 µg/ml against M. tuberculosis, and demonstrates antifungal potency against Candida spp. strains ATCC 14053, ATCC 1369, and ATCC 15126, with an MIC of 125 µg/ml.

Carbonic anhydrase inhibitor23 (compound 40) is a potent inhibitor of carbonic anhydrase (CA), with Ki values of 617.2 nM for hCA I (α) and 434.1 nM for hCA II (α).

hCA-I/hCA-II-IN-1 (Compound P4) is a potent dual inhibitor of human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II), with Ki values of 0.22 μM and 0.33 μM respectively. hCA-I/hCA-II-IN-1 is useful for research into diseases related to CA enzymes, including glaucoma, hypertension, and ulcers.

Carbonic anhydrase activator 1 (Compound 17) is an orally active compound capable of penetrating the blood-brain barrier (BBB), and acts as an activator of carbonic anhydrase (CA). It exhibits KA values of 7.8 μM for hCA I, 3.9 μM for hCA VA, and 2.1 μM for hCA VII. Carbonic anhydrase activator 1 is applicable to research in cancer, glaucoma, cardiovascular diseases, and neurodegenerative disorders such as epilepsy.

Benzolamide (CL 11366) inhibits carbonic anhydrase effectively and low-threshold calcium currents in hippocampal pyramidal neurons.

CAIX Inhibitor S4 (S4) is an effective inhibitor of carbonic anhydrase IX/XII with a Ki of 7 nM and 2 nM, respectively. The Kis for CA II and CA I are 546 and 5600 nM.

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

hCAIX/XII-IN-5 (Coumarin 9a) is an inhibitor of carbonic anhydrase (CA) with excellent selectivity for hCA IX/XII, displaying Kis of 93.3 nM and 85.7 nM over hCA I and hCA II, respectively. It exhibits anti-proliferative activities in cancer cells, delaying the cell cycle and inducing apoptosis [1].

hCAI/II-IN-6 is a selective and orally active inhibitor of human carbonic anhydrase (CA). hCAI/II-IN-6 inhibited hCA I, hCA II, hCA VII, and hCA XII with Ki values of 220, 4.9, 6.5, and ＞50,000 nM. hCAI/II-IN-6 showed anticonvulsant activity in vivo. hCAI/II-IN-6 can be used to study epilepsy. hCAI/II-IN-6 showed anticonvulsant activity in vivo. hCAI/II-IN-6 can be used to study epilepsy.

Carbonic anhydrase inhibitor 14 (Compound 8b) is a potent CA inhibitor, exhibiting K i values of 1203, 99.7, 9.4, and 27.7 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. Additionally, it effectively inhibits CDK2 with an IC 50 of 20.3 μM and demonstrates significant antitumor activity [1].

Carbonic Anhydrase Inhibitor 12 is a potent inhibitor of CA II, with additional inhibitory activity against CA I, exhibiting K_i values of 1.72 nM for CA II and 271 nM for CA I. Moreover, it demonstrates significant anticancer activity across various cancer cell lines [1].

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.

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].

Carbonic anhydrase inhibitor 16 (compound 1) is a potent and selective carbonic anhydrase (CA I/CA II) inhibitor, with potential antiviral activity, used in viral infection research.

hCAI/II-IN-7 (compound 1F) is an effective carbonic anhydrase (CA) inhibitor with Ki values of 23 nM, 44 nM, and 21 μM for hCA-I, hCA-II, and bCA respectively.

hCAIX-IN-18 (compound 30), a potent inhibitor of the carbonic anhydrase enzyme family (CA), exhibits K i values of 3.5 nM for hCAI, 9.4 nM for hCAII, 43.0 nM for hCAIX, and 8.2 nM for hCAXII. This compound is applicable in cancer research [1].