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抑制剂&激动剂
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  • 抑制剂&激动剂
    34
    抑制剂&激动剂
  • 重组蛋白
    1
    重组蛋白
  • 多肽产品
    2
    多肽产品
  • 天然产物
    2
    天然产物
  • 试剂盒
    2
    试剂盒
  • 同位素
    4
    同位素
  • 标准品
    3
    标准品
  • 寡核苷酸
    1
    寡核苷酸
  • Sambutoxin
    TN4937160047-56-3
    Sambutoxin, a new mycotoxin produced by toxic Fusarium isolates obtained from rotted potato tubers, it can cause toxic effects in rats, including body weight loss, feed refusal, hemorrhage in the stomach and intestines, and, finally, death when rats were
    • ¥ 4420
    待询
    规格
    数量
  • Aglafoline
    Rocaglamide U, Aglafolin, (-)-Methyl rocaglate
    T10260143901-35-3In house
    Aglafoline inhibits in a concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of Aglafoline on PAF (3.6 nM)-induced platelet aggregation were about 50 μM.
    • ¥ 18900
    3-6月
    规格
    数量
  • Dibutyryl-cGMP sodium
    Bt2cGMP sodium
    T1103851116-00-8In house
    Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma
    • ¥ 1950
    5日内发货
    规格
    数量
  • Myosin V-IN-1
    T720601259177-59-7In house
    Myosin V-IN-1是一种有效且具有选择性的 Myosin V 抑制剂,Ki 值为 6 μM。Myosin V-IN-1 抑制肌动蛋白 V 发生作用, 通过选择性抑制肌动球蛋白复合物释放 ADP 来减缓肌动蛋白激活的肌球蛋白 V ATP 酶。
    • ¥ 3320
    现货
    规格
    数量
  • Salbutamol
    沙丁胺醇, Albuterol, AH-3365
    T113918559-94-9
    Salbutamol (Albuterol) 是短效的 β2 肾上腺素受体激动剂,用于哮喘和慢性阻塞性肺疾病(COPD) 引发的支气管痉挛的研究。
    • ¥ 211
    现货
    规格
    数量
  • TNKS-2-IN-1
    T776754765-59-7
    TNKS-2-IN-1 是一种 TNKS-2 抑制剂。TNKS-2-IN-1 对 TNKS-1 和 TNKS-2有抑制作用,IC50 分别为 259 nM 和 1100 nM。TNKS-2-IN-1 具有抗菌活性,对大肠杆菌和金黄色葡萄球菌具有抑制作用。TNKS-2-IN-1 抑制 NLRP3 炎症小体 (IC505μM)通过抑制ATP刺激的J1A.774细胞释放IL-1β。
    • ¥ 99
    现货
    规格
    数量
    TargetMol | Inhibitor Sale
  • Gliclazide
    格列齐特, SE1702, S1702
    T152721187-98-4
    Gliclazide (SE1702) 是一种有效的全细胞的 β 细胞 ATP 敏感型钾流阻断剂,IC50为 184 nM,用作降糖药。
    • ¥ 186
    现货
    规格
    数量
  • Tpl2 Kinase Inhibitor 1
    Tpl2 激酶抑制剂 1
    T17145871307-18-5
    Tpl2 Kinase Inhibitor 1 是一种强效、可逆且高选择性的 ATP 竞争性 Tpl2(MAP3K8/COT)丝氨酸 / 苏氨酸激酶抑制剂,对 Tpl2 激酶的抑制活性 IC₅₀为 50 nM。Tpl2 Kinase Inhibitor 1 在体外可抑制 LPS 诱导的人原代单核细胞 TNF-α 释放(IC₅₀=0.7 μM)。Tpl2 Kinase Inhibitor 1 可用于炎症反应和某些癌症的研究。
    • ¥ 826
    现货
    规格
    数量
  • P2X4 antagonist-4
    T2044413108486-39-8
    P2X4 antagonist-4 (compound 64) 是一种高效的P2X4R拮抗剂,其IC50值为8 µM。该化合物能够阻断ATP诱导的NLRP3炎症小体活化以及IL-1β的释放。
    • ¥ 12800
    10-14周
    规格
    数量
  • GAT2711
    T209856
    GAT2711 是一种全激动剂,作用于 α9nAChR,EC50 为 230 nM。其对 α9 的选择性比对 α7nAChR 高出 340 倍。GAT2711 可抑制 THP-1 细胞中 ATP 诱导的 IL-1β 释放,并在 α7nAChR 基因敲除小鼠中仍保持镇痛活性。
    • 待询
    规格
    数量
  • NLRP3/URAT1-IN-1
    T2131702994637-53-3
    NLRP3/URAT1-IN-1 是一种口服活性的NLRP3和URAT1双重抑制剂 (IC50= 3.81 μM)。它抑制LPS和ATP刺激的小鼠骨髓源性巨噬细胞 (BMDMs) 中IL-1β的释放,IC50值为2.61 μM。此外,NLRP3/URAT1-IN-1 能够降低急性高尿酸血症 (HUA) 小鼠的血清尿酸 (SUA) 水平,并减轻肝/肾损伤,适用于痛风和高尿酸血症的研究。
    • 待询
    10-14周
    规格
    数量
  • NLRP3-IN-84
    T213371
    NLRP3-IN-84 (Compound 32) 是一种NLRP3炎症小体抑制剂,它通过抑制NLRP3 ATP酶 (NLRP3 ATPase) 的活性(IC50= 158.4 nM),干扰NLRP3的寡聚化。此外,NLRP3-IN-84 抑制Caspase-1(IC50= 27.7 nM)、IL-1β的释放(PBMC:IC50= 19.5 nM;mPBMC:IC50= 24.2 nM)以及ASC斑点的形成(IC50= 131 nM)。该化合物对NLRC4和AIM2炎症小体无抑制活性,并且在小鼠急性腹膜炎模型中表现出显著的体内抗炎效果。NLRP3-IN-84 可用于研究与NLRP3相关的炎症性疾病。
    • 待询
    规格
    数量
  • Bimakalim
    SR-44866, EMD-52692
    T213838117545-11-6
    Bimakalim (EMD-52692) 是一种 ATP 敏感的钾通道 (potassium channel) 开放剂。Bimakalim 可以降低髓过氧化物酶 (MPO) 的跨壁活性。它模拟缺血预适应作用,能够减少犬的梗死面积、腺苷释放以及中性粒细胞的功能。
    • 待询
    10-14周
    规格
    数量
  • 2DG-ODDA
    T214101
    2DG-ODDA 是 2-脱氧葡萄糖 (2-DG) 的一种高效抗肿瘤衍生物。它能够诱导细胞凋亡 (apoptosis) 并且减少 ATP 的生成。该化合物主要通过脂肪酸和葡萄糖转运蛋白被细胞摄取,然后被α-Mannosidase 裂解,释放出 2DG,进而抑制 N-糖基化并干扰细胞代谢。研究表明,2DG-ODDA 能够在 4T1 小鼠模型中有效抑制肿瘤生长,并可应用于三阴性乳腺癌 (TNBC) 的研究。
    • 待询
    规格
    数量
  • nAChR antagonist 2
    T215124
    nAChRantagonist 2 是一种选择性nAChR拮抗剂,在非洲爪蟾卵母细胞中对人源α9α10、α9和α7等nAChR亚型表现出抑制效果,其IC50分别为16.0 nM、26.2 nM和336.3 nM。它能够在纳摩尔浓度下抑制ATP诱导的IL-1β释放。此化合物可应用于非阿片类镇痛药和免疫调节剂的相关研究。
    • 待询
    规格
    数量
  • Ganglioside GM1 Asialo Mixture
    T3729571012-19-6
    Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.
    • ¥ 6360
    35日内发货
    规格
    数量
  • ITH15004
    T37313
    ITH15004 is a non-nucleotide antagonist of the purinergic P2X7receptor (IC50= 9 μM in HEK293 cells expressing the human receptor).1It inhibits ATP-induced currents inX. laevisoocytes expressing the human P2X7receptor when used at a concentration of 100 μM. ITH15004 (1 μM) decreases IL-1β release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA). 1.Calzaferri, F., Narros-Fernández, P., de Pascual, R., et al.Synthesis and pharmacological evaluation of novel non-nucleotide purine derivatives as P2X7 antagonists for the treatment of neuroinflammationJ. Med. Chem.64(4)2272-2290(2021)
    • ¥ 319
    待询
    规格
    数量
  • JC-171
    T381062112809-98-8
    JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. Cell Viability Assay[1] Cell Line: J774A.1 murine macrophage cells JC-171 treatment delays the progression and reduces the severity of experimental autoimmune encephalomyelitis (EAE) in mouse[1]. Animal Model: Mice immunized subcutaneously with 200 μg Myelin oligodendrocyte glycoprotein (MOG) 35-55 peptide emulsified in Complete Freund's Adjuvant (CFA) on day 0 followed by injection of 200 ng of pertussis toxin. [1]. Chunqing Guo, et al. Development and Characterization of a Hydroxyl-Sulfonamide Analogue, 5-Chloro-N-[2-(4-hydroxysulfamoyl-phenyl)-ethyl]-2-methoxy-benzamide, as a Novel NLRP3 Inflammasome Inhibitor for Potential Treatment of Multiple Sclerosis. ACS Chem Neurosci. 2017 Oct 18;8(10):2194-2201.
    • ¥ 2130
    5日内发货
    规格
    数量
  • NBC 19
    T383602068818-75-5
    Potent NLRP3 inflammasome inhibitor (IC50 = 60-80 nM). Inhibits nigericin- and ATP-induced IL-1β release. Baldwin et al (2017) Boron-Based Inhibitors of the NLRP3 Inflammasome. Cell Chem.Biol. 24 1321 PMID:28943355 |Redondo-Castro et al (2018) Development of a characterised tool kit for the interrogation of NLRP3 inflammasome-dependent responses. Sci.Rep. 8 5667 PMID:29618797
    • ¥ 6770
    35日内发货
    规格
    数量
  • TAT-Gap19(I130A)
    TAT-Gap19(I130A)
    T41204
    TAT-Gap19(I130A) is a control peptide for TAT-Gap19, a Cx43 hemichannel blocker. TAT-Gap19(I130A) consists of TAT-GAP19 with a I130A amino acid residue change at a key residue for GAP19 activity. In C6 glioma cells expression Cx43, TAT-GAP19(1130A) does not inhibit [Ca2+]i-triggered ATP release at 200 μM. TAT-Gap19(I130A) is cell permeable.
    • ¥ 4830
    35日内发货
    规格
    数量
  • AZ-DF 265
    T6860283901-40-0
    AZ-DF 265 is a hypoglycaemic drug which stimulates insulin release. AZ-DF-265 inhibits ATP-sensitive potassium channels and displaces [3H]-glibenclamide from the sulphonylurea receptor.
    • ¥ 10600
    6-8周
    规格
    数量
  • GSK1370319A
    T716511001389-31-6
    GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM). GSK1370319A inhibits ATP-induced increase in IL-1β release and caspase 1 activation in lipopolysaccharide (LPS)-primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-related deficits in long-term potentiation (LTP) and inhibits the accompanying age-related caspase 1 activity. We conclude that inhibiting P2X(7) receptor-activated NLRP3 inflammasome formation and the consequent IL-1β release from glia preserve neuronal viability and synaptic activity.
    • ¥ 10600
    6-8周
    规格
    数量
  • Dimethyl L-glutamate
    Dimethyl glutamate
    T724606525-53-7
    Dimethyl L-glutamate (Dimethyl glutamate), 一种可透膜的谷氨酸类似物,可刺激葡萄糖诱导的胰岛素 (insulin) 释放。Dimethyl L-glutamate 抑制KATP 通道的活性。Dimethyl L-glutamate 抑制E. gracilis 生长并导致细胞异常分裂。Dimethyl L-glutamate 可用于糖尿病、葡萄糖转运、磷酸化和进一步代谢的研究。
    • ¥ 10600
    6-8周
    规格
    数量
  • Thapsigargicin
    Thapsigargicine
    T8099867526-94-7
    Thapsigargicin 是一种从毒胡萝卜(Thapsia garganica) 中分离的倍半萜内酯类天然产物。Thapsigargicin 是肌浆 / 内质网钙 ATP 酶(SERCA)的强效非竞争性抑制剂(IC₅₀ ≈ 10–30 nM),通过特异性阻断 SERCA 泵导致内质网钙库耗竭和细胞质钙水平升高,进而激活肥大细胞 / 白细胞释放组胺、诱导内质网应激和细胞凋亡。Thapsigargicin 可用于钙信号通路、炎症反应研究。
    • ¥ 1590
    现货
    规格
    数量