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。

Carbonic anhydrase/AChE-IN-1 (compound 16) 是一种碳酸酐酶 (carbonic anhydrase) 和 AChE 的抑制剂，其对 hCA I、hCA II 和 AChE 的 Ki 值分别为 24.42 nM、19.95 nM 和 5.07 nM。

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。

2-Methoxy-4-propylphenol是human carbonic anhydrase isoenzyme 1/2/9/12的抑制剂，具有抗真菌活性。

2-Ethylhexanoic acid是一种羧酸，对Carbonic anhydrase 1和2具有抑制作用，可用于生物化学实验和药物合成研究。

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。

Carbonic anhydrase inhibitor30 (compound 17) 是一种碳酸酐酶抑制剂，其对 hCA I 和 hCA II 的Ki值分别为 2.13 μM 和 0.161 μM[1]。

Anti-inflammatory agent 67 (compound 7a) 是一种靶向碳酸酐酶 (Carbonic Anhydrase) 和COX-2的双重抑制剂，以及Polmacoxib的磺胺类衍生物，具备抗炎和镇痛功效。Anti-inflammatory agent 67 的IC50s 针对COX-1和COX-2分别为10.4 μM和50 nM。它与多种碳酸酐酶亚型的结合 Ki 值为48.3 nM (CA I)，42.2 nM (CAII)，52.3 nM (CAIX)，13.3 nM (CA XII)。

Anti-inflammatory agent 68 (compound 7b) 是 Polmacoxib 的磺胺类衍生物，亦为碳酸酐酶 (Carbonic Anhydrase) 与 COX-2 的双重抑制剂，具有显著的抗炎和镇痛作用。其对 COX-1 和 COX-2 的 IC50 分别为 12.6 μM 和 60 nM。同时，Anti-inflammatory agent 68 与不同亚型碳酸酐酶结合的 Ki 值为 52.6 nM (CA I)，79.1 nM (CA II)，58.1 nM (CA IX)，17.2 nM (CA XII)。

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。