carbonic anhydrase i (ca-i)

Dorzolamide hydrochloride (MK507 hydrochloride) 是一种碳酸酐酶carbonic anhydrase II 抑制剂，能够抑制红细胞CA-II(IC50:0.18 nM) 和CA-I(IC50:600 nM) 。

Benzolamide (CL 11366) 是碳酸酐酶 (CA) 抑制剂，抑制hCA I(Ki:15 nM)、hCA II(Ki:9 nM)、EcoCAγ(Ki:94 nM)、VchCAγ(Ki:78 nM)、CAS3(Ki:54 nM)。它可用于研究青光眼和癫痫。

hCAI II-IN-6 是一种具有选择性和口服活性的human carbonic anhydrase(CA) 抑制剂。hCAI II-IN-6对 hCA I，hCA II，hCA VII 和 hCA XII 有抑制作用，Ki 值分别为 220，4.9，6.5 和 ＞50000 nM。hCAI II-IN-6 在体内显示抗惊厥活性。hCAI II-IN-6 可以用于研究癫痫。

AChE hCA I-IN-1 (Compound L3) 是一种针对乙酰胆碱酯酶 (AChE) 和碳酸酐酶 (CA) 的抑制剂，其抑制乙酰胆碱酯酶、hCA I 和 hCA II 的 IC50 值分别为 302 nM、265 nM 和 283 nM。

CAIX Inhibitor S4 (S4) 是一种有效的碳酸酐酶 IX XII 抑制剂，Ki 分别为 7 nM 和 2 nM。 CA II 和 CA I 的 Ki 分别为 546 和 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) 是一种碳酸酐酶 (CA) 抑制剂，具有出色的 hCA IX XII 选择性，对 hCA I 和 hCA II 的Ki 值分别为 93.9 和 85.7 nM。hCAIX XII-IN-5 对癌细胞具有抗增殖活性，可延迟细胞周期并诱导细胞凋亡。

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. Furthermore, Carbonic anhydrase inhibitor 14 demonstrates significant antitumor activity [1].

碳酸酐酶抑制剂12是针对CA II具有高效抑制作用的化合物，其Kis值仅为1.72 nM，对CA I亦表现出有效抑制（Kis为271 nM）。此外，该化合物在多种肿瘤细胞系中显示出显著的抗癌活性。

hCAIX XII-IN-6 是具有口服活性的碳酸酐酶（CA）抑制剂，能够抑制人体 CA 亚型 hCA I、II、IV、IX 及 XII，其 Ki 值分别为 6697 nM、2950 nM、4093 nM、4.1 nM 和 7.7 nM。适用于类风湿关节炎（RA）研究。

DPP IV hCA II-IN-1 是一种有效的选择性二肽肽酶 IV (DPP IV) 和碳酸酐酶 (CA) 抑制剂，抑制 DPP IV 的 IC50值为 0.049 μM, 抑制 CA II、CA VB、CA VA、CA IX、CA I 和 CA IV 的 Ki 值分别为 0.0361、0.0428、0.0941、0.1328、0.2615 和 3.034 μM。

Carbonic anhydrase inhibitor 16 (compound 1) 是一种具有高效性和选择性的碳酸酐酶 （CA I CA II）抑制剂，具有潜在的抗病毒活性，可用于研究病毒感染。

hCAI II-IN-7 (compound 1F) 作为一种效能显著的碳酸酐酶 (CA) 抑制剂，其对 hCA-I、hCA-II 以及牛 CA 的 Ki 值分别为 23 nM、44 nM 和 20.57 μM。

hCAIX-IN-18 (compound 30) 作为一种碳酸酐酶抑制剂，对不同亚型碳酸酐酶的Ki值表现出得相应抑制效果，具体为hCAI的Ki值为3.5 nM，hCAII的Ki值为9.4 nM，hCAIX的Ki值为43.0 nM，以及hCAXII的Ki值为8.2 nM。