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抑制剂&激动剂
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  • 抑制剂&激动剂
    16
    TargetMol | Inhibitors_Agonists
  • 化合物库
    1
    TargetMol | Compound_Libraries
  • 重组蛋白
    11
    TargetMol | Recombinant_Protein
  • 天然产物
    2
    TargetMol | Natural_Products
  • Co 102862
    V 102862
    T22675181144-66-1
    Co 102862 是一种电压门控钠通道阻滞剂。 Co 102862 可用于抗惊厥的研究。
    • ¥ 196
    In stock
    规格
    数量
  • Ordopidine
    奥多匹定, ACR-325, ACR325, ACR 325
    T33816871351-60-9In house
    Ordopidine (ACR325) 是一种多巴胺能稳定剂,可抑制精神刺激剂引起的多动症,并在不活动时刺激行为。Ordopidine 在体外作为多巴胺 D2 受体拮抗剂起作用,尽管亲和力低,但其依赖于特定状态的行为效应特征是 D2 受体拮抗剂所不具备的。
    • ¥ 415
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • CBR-5884
    T14884681159-27-3
    CBR-5884 是一种磷酸甘油酸脱氢酶抑制剂,IC50为 33 μM。 它抑制癌细胞中的丝氨酸合成,选择性地抑制黑素瘤和乳腺癌细胞系的增殖,对具有高丝氨酸生物合成活性的癌细胞系有选择性毒性。
    • ¥ 287
    In stock
    规格
    数量
  • Raxatrigine hydrochloride
    GSK-1014802 hydrochloride, CNV1014802 (hydrochloride)
    T14992934240-31-0
    Raxatrigine hydrochloride is a state-dependent sodium channel blocker and a Nav1.7 sodium channel inhibitor.
    • ¥ 740
    5日内发货
    规格
    数量
  • Ro 44-3888
    RO-44-3888, RO443888
    T202774144412-18-0
    Ro 44-3888作为sibrafiban的活性成分,在其前药形式Ro 48-3657口服给药下,实现了可预测的Ro 44-3888血浆浓度,自第二剂量后达到稳定状态,并表现出浓度依赖性的血小板聚集抑制以及出血时间延长。这些结果表明Ro 44-3888是一个值得进一步评估的候选物,特别是在动脉血栓形成高风险和急性冠状动脉综合症患者中,由于其吸收可重复性强。
    • 待询
    10-14周
    规格
    数量
  • AFD-21
    AFD21,NS-2 Class 1 antiarrhythmic agent
    T2365299465-44-8
    AFD-21是一种 I 类抗心律失常药物。它在钠通道失活状态下与钠通道结合,对钠通道具有使用和电压依赖性抑制作用,其解结合率与具有中等动力学的I 类抗心律失常药物相当。
    • ¥ 10600
    6-8周
    规格
    数量
  • TROX-1
    TROX1,TROX 1
    T249021309601-26-0
    TROX-1 is the activation state-dependent Cav2 channel antagonist.
    • ¥ 12800
    8-10周
    规格
    数量
  • 17(r)-resolvin d1
    Aspirin-triggered Resolvin D1, 17(R)-Resolvin D1
    T35946528583-91-7
    Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid.[1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D1 is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase.[1] 17(R)-RvD1 is an aspirin-triggered epimer of RvD1 that reduces human polymorphonuclear leukocyte (PMN) transendothelial migration, the earliest event in acute inflammation, with equipotency to RvD1 (EC50 = ~30 nM).[3] 17(R)-RvD1 exhibits a dose-dependent reduction in leukocyte infiltration in a mouse model of peritonitis with maximal inhibition of ~35% at a 100 ng dose.[3] In contrast to RvD1, the aspirin-triggered form resists rapid inactivation by eicosanoid oxidoreductases. Analytical and biological comparisons of synthetic 17(R)-RvD1 with endogenously derived 17(R)-RvD1 have confirmed its identity as matching the natural product.[4]
    • 待估
    35日内发货
    规格
    数量
  • RWJ-56110 dihydrochloride
    T367172387505-58-8
    RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2]. Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 [1].RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin's action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1 2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1 2[2].RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2 M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells [1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62. [2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54.
    • ¥ 4665
    待询
    规格
    数量
  • aps-2-79
    T700042002381-25-9
    APS-2-79 是一种 KSR 依赖性的MEK 拮抗剂。APS-2-79 与 ATPbiotin 竞争性地结合到 KSR2-MEK1 复合物内的KSR2,IC50为 120 nM。APS-2-79 与 KSR 结合可将 KSR 固定在一个非活性的状态,使其无法再结合RAF 和激活MEK,从而阻断了 Ras-MAPK 信号通路。
    • ¥ 578
    1-2周
    规格
    数量
  • CNV-2197944
    T712391204535-44-3
    CNV-2197944 is a novel, small molecule, state-dependent calcium channel blocker, designed to selectively inhibit highly active Cav2.2 channels.
    • ¥ 10600
    6-8周
    规格
    数量
  • Nav1.3 channel inhibitor 1
    T79280
    Nav1.3 channel inhibitor 1 (化合物 15b) 为状态依赖性电压门控钠通道Nav1.3的抑制剂,具有IC50值为20 nM。该化合物能穿透血脑屏障,适用于神经系统疾病研究。
    • 待询
    规格
    数量
  • PF-05186462
    PF-05150122
    T87111235406-03-7
    PF-05186462 (PF-05150122)是选择性的人Nav1.7电压依赖性钠通道抑制剂,IC50为 21 nM,与其他钠通道 (Nav 1.1、1.2、1.3、1.4、1.5、1.6 和 1.8) 相比,它对 Nav1.7显示出显著的选择性。PF-05186462在急性或慢性疼痛中具有研究价值。
    • ¥ 1280
    In stock
    规格
    数量
  • OX-201
    T891582460722-03-4
    OX-201 是一种选择性 OX2R 激动剂,其 EC50 值为 8 nM.此化合物能诱导神经元的觉醒状态,进而促进 tau 蛋白向间质液 (ISF) 中的释放,这一过程依赖于神经活动.尽管 OX-201 并不改变海马中 tau 蛋白的水平,但它的使用有助于调解由神经活动引起的 tau 蛋白的流出,特别是在阿尔茨海默病 (AD) 的睡眠 觉醒节律失调状况下.此外,释放到 ISF 中的 tau 可通过淋巴系统从大脑中清除.
    • 待询
    10-14周
    规格
    数量
  • 26-Nor-8-oxo-alpha-onocerin
    TN2830125124-68-7
    26-Nor-8-oxo-alpha-onocerin can promote the osteoblast proliferation rate, the effect is time-dependent,concentration-dependent and differentiation state-dependent.
    • ¥ 4040
    待询
    规格
    数量
  • Didrovaltrate
    TN384418296-45-2
    Didrovaltrate shows cytotoxic against human cancer cell lines. Didrovaltrate blocks I(Ca-L) in a concentration-dependent manner and probably inhibits I(Ca-L) in its inactive state, which may contribute to its cardiovascular effect.
    • ¥ 10790
    5日内发货
    规格
    数量
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