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抑制剂&激动剂
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  • 抑制剂&激动剂
    35
    TargetMol | Inhibitors_Agonists
  • 化合物库
    2
    TargetMol | Compound_Libraries
  • 重组蛋白
    1
    TargetMol | Recombinant_Protein
  • 多肽产品
    5
    TargetMol | Peptide_Products
  • 天然产物
    1
    TargetMol | Natural_Products
  • 同位素
    2
    TargetMol | Isotope_Products
  • 1-Octanol
    正辛醇, Octanol
    T10024111-87-5
    1-Octanol (Octanol) 是一种饱和脂肪醇,是一种 T 型钙通道抑制剂,对天然 T 电流的IC50为 4 μM。它是一种具有类似柴油特性的极具吸引力的生物燃料。
    • ¥ 123
    In stock
    规格
    数量
  • rq-00203078
    T20071254205-52-1
    RQ00203078是一种口服有效的TRPM8高选择性拮抗剂,对大鼠和人类TRPM8通道的IC50分别为 5.3 nM 和 8.3 nM。它对 TRPV1,TRPA1,TRPV4 或 TRPM2 通道基本没有抑制作用。
    • ¥ 169
    In stock
    规格
    数量
  • Zonisamide
    AD 810, 唑尼沙胺, CI 912
    T026768291-97-4
    Zonisamide (AD 810) 是锌酶碳酸酐酶 (carbonic anhydrase) 的有效抑制剂,对人类线粒体同工酶 hCA II 和 hCA V 作用的 Ki 值分别为 35.2 nM 和 20.6 nM。Zonisamide 具有抗癫痫活性,在癫痫、癫痫发作和帕金森病的研究中具有价值。
    • ¥ 348
    In stock
    规格
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  • Lomerizine dihydrochloride
    盐酸洛美利嗪, Terranas, Lomerizine 2HCl, Lomerizine hydrochloride, KB-2796
    T6571101477-54-7
    Lomerizine dihydrochloride (KB-2796) 是双重 L 和 T 型电压门控钙通道拮抗剂。
    • ¥ 189
    In stock
    规格
    数量
  • Atagabalin
    PD 0200390,PD-0200390,PD0200390
    T30188223445-75-8In house
    Atagabalin, also known as PD 0200390, is a gabamimetic agent under development for the treatment for insomnia. Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2). It was discontinued following unsatisfactory t
    • ¥ 10600
    待询
    规格
    数量
  • ICILIN
    AG-3-5
    T181436945-98-9
    ICILIN (AG-3-5) 是一种有效的的瞬时受体电位 M8 (TRPM8) 离子通道激动剂。 Icilin 激活 EGTA 中的 TRPM8,该激活作用具有剂量依赖性, EC50=1.4 μM。Icilin 通过调节 T 细胞反应减轻自身免疫性神经炎症。
    • ¥ 128
    In stock
    规格
    数量
  • Mibefradil
    米贝地尔, Ro 40-5967
    TQ0153116644-53-2
    Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).
    • ¥ 17200
    10-14周
    规格
    数量
  • Efonidipine
    (±)-Efonidipine, 依福地平, NZ-105
    T2323111011-63-3
    Efonidipine (NZ-105) 是一种二氢吡啶类钙通道阻滞剂,可阻断 T 型和 L 型钙通道。
    • ¥ 169
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • UK 78282 hydrochloride
    T23497136647-02-4
    UK 78282 hydrochloride,一种新型有效且具有选择性的 Kv1.3 阻滞剂。UK 78282 hydrochloride 抑制 Kv1.3 电压门控钾通道,抑制人 T 细胞活化。
    • ¥ 579
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • Trimethadione
    三甲双酮, 3,5,5,-Trimethyloxazolidine-2,4-dione
    T0283127-48-0
    Trimethadione (3,5,5,-Trimethyloxazolidine-2,4-dione) 是恶唑烷二酮类抗惊厥剂,也是一种 T 型钙通道阻滞剂,具有抗痛觉过敏作用,可用于研究失神发作。
    • ¥ 143
    In stock
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  • Mibefradil dihydrochloride
    盐酸米贝地尔, 米贝拉地尔, Ro 40-5967 (dihydrochloride)
    T12032116666-63-8
    Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) 是一种钙离子通道抑制剂,选择性作用于 T 型 Ca2+通道,对 T 型和 L 型通道的IC50分别为 2.7 和 18.6 μM。
    • ¥ 713
    In stock
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    数量
  • ML218 hydrochloride
    T120762319922-08-0
    ML218 hydrochloride is a selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor (Cav3.2 and Cav3.3 with IC50s of 310 nM and 270 nM , respectively).
    • 待估
    35日内发货
    规格
    数量
  • ML218
    T12076L1346233-68-8
    ML218 是一种具有口服活性、选择性、高效性且可穿透血脑屏障的 T 型 Ca2+ 通道抑制剂(Cav3.2 和 Cav3.3 的 IC50 分别为 310 nM 和 270 nM)。ML218 可抑制丘脑下核(STN)神经元的突发性活动。
    • ¥ 597
    In stock
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  • T16Ainh-A01
    T13059552309-42-9
    T16Ainh-A01 是氨基苯基噻唑,是有效的跨膜蛋白 16A 的抑制剂,抑制 TMEM16A 介导的氯离子电流,IC50约为1 µM。TMEM16A (ANO1)起钙激活氯离子通道(CaCC)的作用。
    • ¥ 280
    In stock
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  • NMP-7
    NMP7,NMP 7
    T258741358039-07-2
    NMP-7 is a non-selective CB1 and CB2 cannabinoid receptor agonist that works by blocking T-type calcium channels.
    • ¥ 10600
    6-8周
    规格
    数量
  • Z944
    Z 944, Z-944
    T292011199236-64-0
    Z944 是有效的 T 型钙通道拮抗剂,对跨模态和视觉识别记忆障碍有缓解作用。
    • ¥ 438
    In stock
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  • n-arachidonoyl taurine
    T35918119959-65-8
    N-Arachidonoyl taurine is an arachidonoyl amino acid. It is oxygenated by 12(S)- and 15(S)-lipoxygenase and is converted to 12-HETE-taurine (12-HETE-T) in murine resident peritoneal macrophages. N-Arachidonoyl taurine is an activator of the transient receptor potential vanilloid (TRPV) channels TRPV1 and TRPV4 (EC50s = 28 and 21 μM, respectively). It increases calcium flux in HIT-T15 pancreatic β-cells and INS-1 rat islet cells when used at a concentration of 10 μM and increases insulin secretion from 832 13 INS-1 pancreatic β-cells. The levels of N-arachidonoyl taurine are changed in mouse brain following administration of δ9-tetrahydrocannabinol (δ9-THC).
    • 待估
    35日内发货
    规格
    数量
  • (±)5(6)-EET
    T3607087173-80-6
    5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50 = 0.54 μM), and Cav3.3 and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5(6)-EET is provided as a mixture of the free acid and lactone.
    • 待估
    35日内发货
    规格
    数量
  • (2R/S)-6-PNG
    6-Prenylnaringenin, (±)-6-Prenylnaringenin
    T3742768682-01-9
    (2R S)-6-PNG (6-Prenylnaringenin) 是新型天然组蛋白脱乙酰酶抑制剂,具有抗癌抗肿瘤活性,可阻断T型钙通道可减轻小鼠的神经性和内脏疼痛。
    • ¥ 962
    In stock
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    数量
  • Zonisamide-13C2,15N
    Zonisamide-13C2,15N
    T378471188265-58-8
    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).
    • ¥ 6930
    35日内发货
    规格
    数量
  • Suvecaltamide
    MK-8998
    T5632953778-58-0
    Suvecaltamide (MK-8998) 是一种选择性的 T 型钙通道抑制剂。
    • ¥ 297
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • IAA65
    T613932987139-96-6
    IAA65 是一种有效的 T 型钙通道抑制剂 (T-type calcium channel),IC50值为 18.9 μM。IAA65 可用于癫痫研究。
    • ¥ 10600
    10-14周
    规格
    数量
  • TTA-P1
    T61747918333-06-9
    TTA-P1 is a highly potent compound that effectively inhibits human T-type calcium channels, which are involved in various physiological processes such as neuronal burst firing, hormone secretion, and cell growth. With its unique state-independent properties, TTA-P1 holds promising potential for advancing research on absence epilepsy [1].
    • ¥ 14900
    10-14周
    规格
    数量
  • TTA-P2
    T624021072018-68-8
    TTA-P2 (T-Type calcium channel inhibitor) 是一种 T 型钙通道的有效抑制剂。TTA-P2 能够有效的穿透 CNS 并阻断小脑深部核神经元中的天然 T 型电流,完全消除野生型和突变型 Cav3.1 通道的窗口电流。TTA-P2 具有潜力进行神经疾病的研究。
    • ¥ 14900
    6-8周
    规格
    数量