ca 10

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) 是一种来自狗舌草的口服有效类黄酮。它停在 PI3Kγ 的 ATP 结合口袋中，可导致癌细胞周期停滞，并诱导细胞凋亡和自噬。它有抗癌和抗炎活性，有潜力研究疼痛相关疾病。

Tanespimycin (KOS 953) 是一种 Hsp90 抑制剂，可选择性抑制 BT474 肿瘤细胞 Hsp90，IC50为 5 nM。它消耗细胞内 STK38 NDR1，并降低 STK38 激酶活性，还能下调stk38基因表达。

ICA-105665 (PF-04895162) 是一种有效的口服活性的神经元 Kv7.2 7.3和 Kv7.3 7.5钾通道激动剂。ICA-105665 在人肝细胞中具有低细胞毒性潜力，但抑制肝线粒体功能和胆盐输出蛋白 (BSEP) 转运 (IC50为 311 μM)。ICA-105665 可穿透中枢神经系统 (CNS)并具有抗癫痫作用。

Dalpiciclib (SHR-6390) 是一种高选择性、口服生物利用度和相当效力的 CDK4 和 CKD6 抑制剂，IC50 分别为 12.4 nM 和 9.9 nM。它通过抑制磷酸化 Rb 蛋白和诱导 G1 细胞周期阻滞在食管鳞状细胞癌中发挥有效的抗肿瘤活性。

ICA-105574 (ICA) 是 hERG 通道激活剂。它通过消除 hERG 通道的失活从而增强 hERG 通道活性。它可以把电流幅度急剧增加到原来的 10 倍以上，其EC50值为 0.5 + - 0.1 μM，Hill 斜率 (n(H)) 为 3.3 + - 0.2。

9-Oxooctadeca-10,12-dienoic acid 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN5835，CAS号为 54232-58-5。

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).

ts-SA is a metalloenzyme carbonic anhydrase (CA) inhibitor. It is active against 7 out of 10 human CA isoforms.

Dichlorphenamide-13C6is intended for use as an internal standard for the quantification of dichlorphenamide by GC- or LC-MS. Dichlorphenamide is a sulfonamide and an orally bioavailable carbonic anhydrase (CA) inhibitor (Kis = 1.20, 38, 50, and 50 nM for the human CA isoforms CAI, CAII, CAIX, and CAXII, respectively).1It lowers intraocular pressure in rabbits when 50 μl of a 10% solution is applied topically to the eye.2Dichlorphenamide rescues the potassium deficiency and prevents insulin-induced paralysis in a rat model of familial hypokalemic periodic paralysis when administered at a dose of 5.6 mg/kg per day for ten days.3Formulations containing dichlorphenamide have been used in the treatment of glaucoma and primary periodic paralysis.

RS-93522 is an antagonist of calcium channel. RS-93522 had the additional property of inhibiting phosphodiesterase activity in myocardial homogenates (IC50 = 1.6 x 10(-5)M), the potency and efficacy of phosphodiesterase inhibition was similar to that for

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9 . Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC 50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC 50 s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC 50 values of 2.8 and 2.6 nM, respectively.

Efonidipine(NZ-105)盐酸盐是T 型和L 型钙离子通道双重阻断剂。

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。