carbonic anhydrase 1

TSPO Carbonic Anhydrase Modulator 1 (Compound 3) 是一种同时调节线粒体转运蛋白和碳酸酐酶的化合物，其中 TSPOKi 为 1.340 μM，CAVII 的 KA 为 10.7 μM。该化合物促进神经类固醇生成，并增加 BDNF 基因表达，具有神经保护作用。

Human carbonic anhydrase II-IN-1 (Compound S-13) 是一种有效的人碳酸酐酶 II (hCA II) 抑制剂。Human carbonic anhydrase II-IN-1抑制 hCA II，其他 hCA 同工型 I、IV 和 IX 的分别 Ki 为 4.4 nM、 9.2 nM、480.2 nM 和 14.7 nM。Human carbonic anhydrase II-IN-1可用于青光眼的研究。

ALP Carbonic anhydrase-IN-1（Compound 1e）为碳酸酐酶（CA）与碱性磷酸酶（ALP）的双效抑制剂。对CA-II、CA-IX、CA-XII和ALP具有显著抑制活性，其IC50值分别为0.44 µM、1.61 µM、0.51 µM和0.107 µM。

2,3-dihydro-1H-indene-5-sulfonamide 是碳酸酐酶 12（人）抑制剂。

Urea (Carbonyldiamide) 在肝脏中由氨基酸脱氨产生的氨形成。它是蛋白质分解代谢的主要终代谢产物。

Eriocitrin (Eriodictyol-7-O-Rutinoside) 是从柠檬中分离出来的一种黄酮类天然产物，是强效的抗氧化剂。它通过激活线粒体涉及的内在信号传导途径来触发细胞凋亡。它通过上调 p53、cyclin A、cyclin D3 和 CDK6 使 S 期细胞周期停滞，从而抑制肝癌细胞的增殖。

Enpp Carbonic anhydrase-IN-1 (compound 1e) 是有效的 Enpp 和 carbonic anhydrase 抑制剂。Enpp Carbonic anhydrase-IN-1抑制 NPP1、NPP2、NPP3、CA-II、CA-IX 的 IC50 值分别 1.36、1.35、3.00、0.88、1.02 µM。Enpp Carbonic anhydrase-IN-1 选择性抑制癌细胞的增殖，对正常细胞毒性较低。

Carbonic Anhydrase Inhibitor28 (Compound 11) 作为一种有效的Pseudomonas aeruginosa碳酸酐酶抑制剂，展现出良好的抑菌活性。具体来说，其对P. aeruginosa 的最小抑菌浓度(MIC)为0.5 μg mL，最小杀菌浓度(MBC)为1 μg mL。因此，Carbonic Anhydrase Inhibitor28 在抗感染研究领域具有潜在应用价值。

Sulocarbilate（亦称W-1548-1）是一种磺胺类衍生物，同时也是碳酸脱水酶抑制剂。

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。

N-desethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1It inhibits CAII and CAIV activities (IC50s = 1.28 and 128 nM, respectively). 1.Kim, C.-Y., Whittington, D.A., Chang, J.S., et al.Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IVJ. Med. Chem.45(4)888-893(2002)

4-Amino-6-chloro-1,3-benzenedisulfonamide is a carbonic anhydrase inhibitor.1 Formulations containing this compound are diuretics.2 4-Amino-6-chloro-1,3-benzenedisulfonamide is detected as a hydrolysis product of chlorothiazide in the urine.2 Diuretics, including chlorothiazide, have been abused as performance-enhancing drugs and masking agents in sports doping.3References1. 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).2. Deventer, K., Pozo, O.J., Van Eenoo, P., et al. Detection of urinary markers for thiazide diuretics after oral administration of hydrochlorothiazide and altizide-relevance to doping control analysis. J. Chromatogr. A 1216(12), 2466-2473 (2009).3. Cadwallader, A.B., de la Torre, X., Tieri, A., et al. The abuse of diuretics as performance-enhancing drugs and masking agents in sport doping: Pharmacology, toxicology and analysis. Br. J. Pharmacol. 161(1), 1-16 (2010). 4-Amino-6-chloro-1,3-benzenedisulfonamide is a carbonic anhydrase inhibitor.1 Formulations containing this compound are diuretics.2 4-Amino-6-chloro-1,3-benzenedisulfonamide is detected as a hydrolysis product of chlorothiazide in the urine.2 Diuretics, including chlorothiazide, have been abused as performance-enhancing drugs and masking agents in sports doping.3 References1. 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).2. Deventer, K., Pozo, O.J., Van Eenoo, P., et al. Detection of urinary markers for thiazide diuretics after oral administration of hydrochlorothiazide and altizide-relevance to doping control analysis. J. Chromatogr. A 1216(12), 2466-2473 (2009).3. Cadwallader, A.B., de la Torre, X., Tieri, A., et al. The abuse of diuretics as performance-enhancing drugs and masking agents in sport doping: Pharmacology, toxicology and analysis. Br. J. Pharmacol. 161(1), 1-16 (2010).

O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tandem mass spectrometry method for determining carbonic anhydrase inhibitors and their metabolites in urine and hairDrug Test Anal.13(8)1552-1560(2021)

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).

Ethoxzolamide (L-643786) 对 carbonic anhydrase 有抑制作用，Ki 值为 1 nM。

hCA VB-IN-1 (compound 15) 是一种hCA VB(碳酸酐酶 VB)的强效选择性抑制剂，KI 值为 515.7 nM。

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 3 (compound 11g) 可降低青光眼兔的眼压，它是一种碳酸酐酶 II 的抑制剂，。

Carbonic anhydrase inhibitor 10 可用于研究癌症，它对 MCF-7 癌细胞表现出抗增殖活性， IC50值为 11.9 μM。Carbonic anhydrase inhibitor 10 是 hCA IX 的有效抑制剂，Ki 值为 6.2 nM。

Carbonic Anhydrase Inhibitor2 (compound 7c) 是一种针对 Carbonic Anhydrase II 抑制剂，有效降低青光眼兔眼压。

Topiramate lithium (McN 4853) is a wide-ranging antiepileptic compound with GluR5 receptor antagonistic properties. Its mechanism of action involves enhancing GABAergic activity, inhibiting kainate AMPA receptors, voltage-sensitive sodium and calcium channels, and increasing potassium conductance. Additionally, this compound inhibits carbonic anhydrase. [1][2][3]

hCAII-IN-3 (Compound 16) is an inhibitor of human carbonic anhydrase (hCA). It exhibits high affinity for hCA I, hCA II, hCA IX, and hCA XII, with Ki values of 403.8 nM, 5.1 nM, 10.2 nM, and 5.2 nM, respectively. Notably, hCA IX-IN-2 demonstrates anticancer activity [1].

Dichlorphenamide disodium is a specific, orally active carbonic anhydrase inhibitor. It effectively reduces intraocular pressure by impeding the secretion of aqueous humor. Notably, dichlorphenamide disodium holds potential for glaucoma research [1].

hCA IX-IN-1 (Compound 6f) 是一种人碳酸酐酶 (hCA) 抑制剂，对 hCA I、hCA II、hCA IX 和 hCA XII 的 Ki 值分别为 331.4、28.4、9.4 和 17.8 nM。