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抑制剂&激动剂
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  • 抑制剂&激动剂
    34
    TargetMol | Inhibitors_Agonists
  • 多肽产品
    12
    TargetMol | Peptide_Products
  • 天然产物
    3
    TargetMol | Natural_Products
  • 同位素
    2
    TargetMol | Isotope_Products
  • Annaosanchun
    雄甾-3,5,6三醇, YC-6, YC6, YC 6
    T196594725-51-3
    Annaosanchun (YC-6) 有可能用于治疗急性缺血性中风(AIS)。
    • ¥ 378
    In stock
    规格
    数量
  • Dapansutrile
    T1505254863-37-5
    Dapansutrile 是一种口服有活性的 NLRP3 炎性小体选择性抑制剂。它具有抗炎特性,可用于研究缓解疼痛。
    • ¥ 185
    In stock
    规格
    数量
  • SCH79797 dihydrochloride
    T128701216720-69-2
    SCH79797 dihydrochloride 是一种有效的特异性蛋白酶激活受体 1 (PAR1) 拮抗剂,IC50 为 70 nM,Ki 为 35 nM。SCH79797 dihydrochloride 具有抗增殖和促凋亡作用。
    • ¥ 267
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • P7C3-A20
    T24231235481-90-9
    P7C3-A20 是促神经原性和神经保护活性的 P7C3 衍生物。它具有抗抑郁活性,能够透过血脑屏障,并可用于研究脑损伤。
    • ¥ 176
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • Cinepazide maleate
    马来酸桂哌齐特, MD-67350, Vasodistal, Brendil
    T036826328-04-1
    Cinepazide maleate (MD-67350) 是哌嗪衍生物,是一种钙通道阻滞剂,也是一种强效血管扩张剂,可用于脑血管疾病的研究,如缺血性中风和脑梗塞等。
    • ¥ 143
    In stock
    规格
    数量
  • Muscone
    麝香酮, Methylexaltone, 3-Methylcyclopentadecanone
    T2893541-91-3
    Muscone (3-Methylcyclopentadecanone) 是中药麝香的一种主要活性单体。它抑制NF-κB 和NLRP3炎性小体的活化,显著降低炎性细胞因子水平,并最终改善心脏功能和存活率。
    • ¥ 282
    In stock
    规格
    数量
  • Temocapil
    T7714111902-57-9
    Temocapil 是一种酪氨酸激酶抑制剂。
    • ¥ 119
    In stock
    规格
    数量
  • Temocapril hydrochloride
    CS-622 HCl, Temocapril HCl, 盐酸替莫普利
    T6698110221-44-8
    Temocapril hydrochloride (CS-622 HCl) 是血管紧张素转化酶 (ACE) 抑制剂。Temocapril HCl 能够用于充血性心力衰竭、急性心肌梗死、高血压、胰岛素抵抗和肾脏疾病的研究。
    • ¥ 122
    In stock
    规格
    数量
  • Astragaloside IV
    黄芪皂苷 IV, 黄芪甲苷IV, AST-IV, AS-IV
    T297384687-43-4
    Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷,抑制ERK1 2和JNK 激活,在乳腺癌细胞 MDA-MB-231 中,下调(MMP)-2和(MMP)-9的信号通路。
    • ¥ 230
    In stock
    规格
    数量
    TargetMol | Inhibitor Hot
  • Pinokalant
    LOE-908
    T70540149759-26-2In house
    Pinokalant (LOE-908) 是一种新型非选性阳离子通道抑制剂。Pinokalant 在体内实验中可显著减少皮质梗死体积,可改善缺血半影区的代谢和电生理状态,可减少大鼠大脑中动脉闭塞后急性期磁共振图像上的病变大小。Pinokalant是一种潜在的SARS-CoV-2蛋白酶抑制剂,可用于研究脑卒中。
    • ¥ 1300
    In stock
    规格
    数量
  • Pyrithioxin
    吡硫醇(维生素B6衍生品), 吡硫醇, Vitamin B6 disulfide, Pyritinol, Pyridoxine disulfide, Encefabol, Bonifen
    T09051098-97-1
    Pyrithioxin (Encefabol) 是神经动力化合物,能够促进脑内葡萄糖及氨基酸的代谢,改善全身同化作用,增加颈动脉血流量,改善脑血流。
    • ¥ 279
    In stock
    规格
    数量
  • NLRP3-IN-2
    5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide, 4-[2-(5-氯-2-甲氧基苯甲酰氨基)乙基]苯磺酰胺, NLRP3 Inflammasome Inhibitor I
    T323016673-34-0
    NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide) 是一种能够合成格列本脲的中间物,对心肌细胞中NLRP3炎症小体的形成具有抑制作用,在小鼠心肌缺血 再灌注后限制梗死面积,且对代谢无影响。
    • ¥ 176
    In stock
    规格
    数量
  • SSR 69071
    T21989344930-95-6In house
    SSR69071 是一种有效的,具有口服活性的选择性中性粒细胞弹性蛋白酶 (neutrophil elastase) 抑制剂。SSR69071 对人弹性蛋白酶 (Ki=0.0168 nM) 的亲和力高于对大鼠 (Ki=3 nM)、小鼠 (Ki=1.8 nM) 和兔 (Ki=58 nM) 弹性蛋白酶。SSR69071 减少缺血再灌注损伤后的心肌梗死面积。SSR69071 还具有治疗慢性阻塞性肺病、哮喘、肺气肿、囊性纤维化和多种炎症性疾病的潜力。
    • 待估
    35日内发货
    规格
    数量
  • MTP 131 acetate
    T356891334953-95-5
    MTP 131 acetate 是一种小的线粒体靶向四肽。
    • ¥ 287
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • L-NIO dihydrochloride
    T11806159190-44-0
    L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats. L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively.
    • ¥ 5850
    6-8周
    规格
    数量
  • (9R)-RO7185876
    T2043582226077-86-5
    (9R)-RO7185876 (Compound example 16) 是一种γ-secretase抑制剂,能够抑制Αβ42的分泌。此化合物可应用于阿尔茨海默病、脑淀粉样变性血管病、遗传性脑出血伴淀粉样变性、多梗塞性痴呆、老年性痴呆或唐氏综合征的研究。
    • 待询
    10-14周
    规格
    数量
  • (±)14(15)-EET
    (±)14,15-EET, (±)14,15-EpETrE, (±)14(15)-EET
    T35463197508-62-6
    (±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage of the area at risk in a canine model of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) occlusion when administered at a dose of 0.128 mg kg prior to occlusion or reperfusion.[5] Reference:[1]. Chacos, N., Falck, J.R., Wixtrom, C., et al. Novel epoxides formed during the liver cytochrome P-450 oxidation of arachidonic acid. Biochem. Biophys. Res. Commun. 104(3), 916-922 (1982).[2]. Oliw, E.H., Guengerich, F.P., and Oates, J.A. Oxygenation of arachidonic acid by hepatic monooxygenases. Isolation and metabolism of four epoxide intermediates. J. Biol. Chem. 257(7), 3771-3781 (1982).[3]. Jiang, J.-X., Zhang, S.-J., Xiong, Y.-K., et al. EETs attenuate ox-LDL-induced LTB4 production and activity by inhibiting p38 MAPK phosphorylation and 5-LO BLT1 receptor expression in rat pulmonary arterial endothelial cells. PLoS One 10(6), e0128278 (2015).[4]. Oltman, C.L., Weintraub, N.L., VanRollins, M., et al. Epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids are potent vasodilators in the canine coronary microcirculation. Circ. Res. 83(9), 932-939 (1998).[5]. Nithipatikom, K., Moore, J.M., Isbell, M.A., et al. Epoxyeicosatrienoic acids in cardioprotection: Ischemic versus reperfusion injury. Am. J. Physiol. Heart Circ. Physiol. 291(2), H537-H542 (2006).
    • 待估
    35日内发货
    规格
    数量
  • CAY10608
    CAY10608
    T37671457897-92-6
    N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.
    • 待估
    35日内发货
    规格
    数量
  • Nicotiflorin
    山奈酚-3-O-芸香糖苷, Nictoflorin, Nicotifloroside, Kaempferol-3-O-Rutinoside
    T6S129417650-84-9
    Nicotiflorin (Kaempferol-3-O-Rutinoside) 是一种黄酮苷,从传统中药Flos Carthami 中提取得到。它有抗糖化活性和神经保护作用。
    • ¥ 369
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • Moexipril-d5
    T708831356929-49-1
    Moexipril-d5 intended for use as an internal standard for the quantification of moexipril by GC- or LC-MS. Moexipril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor moexiprilat. It is converted to moexiprilat in vivo by side chain ester hydrolysis. Moexipril inhibits ACE in a cell-free assay (IC50 = 2.7 µM for the rabbit enzyme). It also inhibits phosphodiesterase 4 (IC50s = 38, 160, and 230 µM for PDE4B2, PDE4A5 and PDE4D5, respectively). Moexipril (0.1-30 mg kg per day) reduces blood pressure in spontaneously hypertensive rats.1 It also reduces infarct volume in a rat model of focal cerebral ischemia when used at a concentration of 0.01 mg kg.
    • 待估
    35日内发货
    规格
    数量
  • Nicorandil-d4
    T714021132681-23-2
    Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B Kir6.2 over the SUR2A Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.
    • 待估
    35日内发货
    规格
    数量
  • PI3K/Akt/CREB activator 1
    T722272708177-73-3
    PI3K Akt CREB activator 1 (AE-18) 是一种可穿过血脑屏障且具有选择性的诱导型一氧化氮合酶 (iNOS) 抑制剂,可以减少大鼠缺血再灌注后的梗死体积并恢复血液供应不足,可用于研究血管性痴呆和帕金森。
    • ¥ 765
    In stock
    规格
    数量
  • MRS4719
    T734532840581-32-8
    MRS4719 是一种有效的P2X4受体拮抗剂,对人 P2X4 受体的IC50为 0.503 μM。MRS4719 可减少脑梗死体积,减少脑萎缩,在缺血性脑中风模型中具有神经保护和神经康复作用。MRS4719 还能减少 ATP 诱导的人单核细胞源性巨噬细胞 [Ca2+]i 内流。MRS4719 可用于研究缺血性脑中风。
    • ¥ 10600
    6-8周
    规格
    数量
  • PR-39 TFA
    T75870
    PR-39 TFA 是富含脯氨酸和精氨酸的天然抗菌肽,是一种非竞争性,可逆和变构的蛋白酶体 (proteasome) 抑制剂。PR-39 TFA 可逆地结合到蛋白酶体的 α7 亚基上,并通过泛素-蛋白酶体途径阻断 NF-κB 抑制剂 IκBα 的降解。PR-39 TFA 刺激小鼠的血管生成,抑制炎症反应并显着减小心肌梗死面积。
    • 待询
    规格
    数量