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抑制剂&激动剂
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  • 抑制剂&激动剂
    18
    TargetMol | Inhibitors_Agonists
  • 天然产物
    4
    TargetMol | Natural_Products
  • 同位素
    1
    TargetMol | Isotope_Products
  • 检测抗体
    2
    TargetMol | Antibody_Products
  • Epaminurad HCl
    URC-102 HCl, UR-1102 HCl, Epaminurad HCl(1198153-15-9 Free base)
    T27275L1198153-46-6In house
    Epaminurad HCl 是一种可口服且具有特异性和高效性的尿酸转运体 1 (URAT1 ) 抑制剂( Ki:57 nM),对 OAT1 和 OAT3 (有机阴离子转运体)有部分抑制作用。Epaminurad HCl 是一种促尿酸排泄剂,可用于预防和治疗痛风和高尿酸血症。
    • ¥ 1430 TargetMol
    In stock
    规格
    数量
  • Lesinurad
    RDEA594, 雷西那德, 来司诺雷
    T6875878672-00-5
    Lesinurad (RDEA594) 是URAT1和OAT 抑制剂。Lesinurad 用作肾转运蛋白OAT1OAT3 的底物,Km 分别为 0.85 和 2 μM。
    • ¥ 313
    In stock
    规格
    数量
  • Indican
    NSC-87517, 3-Indoxyl-beta-D-glucopyranoside, 3-吲哚基-beta-D-吡喃葡萄糖苷, NSC 87517, NSC87517, Indoxyl-β-D-glucoside
    T19866487-60-5
    Indican (Indoxyl-β-D-glucoside) 是吲哚酚的一种糖苷,染料靛蓝和靛玉红的前体。它的主要代谢物是硫酸吲哚酚 (IS)。其中 IS 是尿毒症毒素,是有机阴离子转运蛋白1 (OAT 1)、OAT 3 和多药耐药相关蛋白4 (MRP 4) 的底物 抑制剂。
    • ¥ 145
    In stock
    规格
    数量
  • OAT1/3-IN-2
    T816292195434-05-8
    OAT1 3-IN-2(化合物8)是一种针对OAT1OAT3的双重抑制剂。该化合物能够以10 μM的浓度逆转Cys-Hg对HEK-OAT1细胞的毒害作用,并可能对肾脏具有保护效应。OAT1 3-IN-2适用于研究汞导致的肾脏损伤。
    • 待询
    规格
    数量
  • OAT1/3-IN-1
    T8163038393-73-6
    OAT1 3-IN-1(化合物7)是针对OAT1OAT3的双重抑制剂。该化合物能逆转Cys-Hg(10 μM)对HEK-OAT1细胞引起的毒害,表明其对肾脏有潜在的保护效应。OAT1 3-IN-1适合用于探究汞引起的肾脏损伤机制研究。
    • 待询
    规格
    数量
  • MFH290
    T699312088715-91-5
    MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12 13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib.
    • ¥ 11700
    6-8周
    规格
    数量
  • OAT-1441
    T699322088453-79-4
    OAT-1441 is a hAMCase inhibitor.
    • ¥ 10600
    6-8周
    规格
    数量
  • P7170
    T701761799702-72-9
    P7170 is an anti-cancer agent active as an mTORC1 C2 and activin receptor-like kinase 1 (ALK1) inhibitor.
    • ¥ 18300
    10-14周
    规格
    数量
  • OAT-177
    T701771799548-33-6
    OAT-177 is a potent, selective, orally active acidic mammalian chitinase (AMCase) inhibitor.
    • ¥ 10600
    6-8周
    规格
    数量
  • Cabotegravir
    卡博特韦, S GSK1265744, GSK744, GSK-1265744
    T60981051375-10-0
    Cabotegravir (S GSK1265744) 是一种HIV 整合酶抑制剂,可研究艾滋病。它抑制OAT1OAT3,IC50值为 0.81 和0.41 μM。
    • ¥ 415
    In stock
    规格
    数量
  • Cyazofamid
    氰霜唑, IKF-916
    T201605120116-88-3
    Cyazofamid 抑制细菌中的 ATP 生成能力来发挥其杀菌效果。此外,该化合物对有机阳离子转运蛋白 3 (OCT3) 和 OAT1 的抑制作用表现出了显著的差异,其 IC50 值分别是 1.54 μM 和 17.3 μM。
    • 待询
    10-14周
    规格
    数量
  • Lesinurad sodium
    雷西那德钠盐, RDEA-594 sodium, RDEA594 sodium, RDEA 594 sodium
    T213011151516-14-1
    Lesinurad sodium (RDEA594 sodium) 是一种具有选择性的尿酸重吸收抑制剂,可用于研究心血管疾病。
    • ¥ 196
    In stock
    规格
    数量
  • Diclofenac Acyl Glucuronide
    Diclofenac Acyl-β-D-Glucuronide, D-1-O-G
    T2716764118-81-6
    Diclofenac Acyl Glucuronide (Diclofenac glucuronide) 是一种肠道代谢物,可加速肠道溃疡。
    • ¥ 7199
    35日内发货
    规格
    数量
  • Epaminurad
    T272751198153-15-9
    Epaminurad (UR-1102) 是一种口服有效的和选择性的URAT1(尿酸转运体 1) 抑制剂,其Ki 为 0.057 μM。Epaminurad 适度地抑制OAT1OAT3(有机阴离子转运体)。Epaminurad 是一种促尿酸排泄剂。Epaminurad 可用于痛风和高尿酸血症的研究。
    • ¥ 2650
    5日内发货
    规格
    数量
  • 4'-hydroxy Trazodone
    T3572153818-10-3
    4’-hydroxy Trazodone is a metabolite of the antidepressant and sedative trazodone.1It is an inhibitor of organic anion transporter 3 (OAT3; Ki= 16.9 μM) and is selective for OAT3 over OAT1 (Ki= >200 μM).2 1.Yamato, C., Takahashi, T., Fujita, T., et al.Studies on metabolism of trazodone, II. Metabolic fate after intravenous administration and effects on liver microsomal drug-metabolizing enzymes in ratsXenobiotica4(12)765-777(1974) 2.Zou, L., Matsson, P., Stecula, A., et al.Drug metabolites potently inhibit renal organic anion transporters, OAT1 and OAT3J. Pharm. Sci.110(1)347-353(2021)
    • ¥ 4970
    35日内发货
    规格
    数量
  • KPH2f
    T624322760615-09-4
    KPH2f 是一种安全、口服有效的 URAT1 GLUT9双抑制剂,对 URAT1和 GLUT9 的 IC50分别为 0.24 μM 和 9.37 μM。KPH2f 对 OAT1 和 ABCG2 几乎没有影响 (IC50分别为 32.14 和 26.74 μM)。
    • ¥ 10600
    10-14周
    规格
    数量
  • JBP485
    T69889211868-63-2
    JBP485 is an inhibitor of renal transporters OAT1 and OAT3. JBP485 is an antihepatitis agent as a substrate for intestinal PEPT1.
    • ¥ 10600
    6-8周
    规格
    数量
  • Indoxyl Sulfate-d5 potassium salt
    T703131644451-34-2
    Indoxyl sulfate-d5 is intended for use as an internal standard for the quantification of indoxyl sulfate by GC- or LC-MS. Indoxyl sulfate is a uremic toxin and a metabolite of tryptophan. It is formed via sulfation of indole, an intermediate generated from tryptophan by intestinal bacteria, by the sulfotransferase (SULT) isoform 1A1 variant 2 (SULT1A1*2) in the liver. Indoxyl sulfate activates the aryl hydrocarbon receptor (AhR) in HepG2 40 6 hepatoma cells (EC50 = 12.1 nM in a reporter assay). It also inhibits the organic anion transporter (OAT) isoforms OAT1 and OAT3 (Kis = 34.2 and 74.4 µM, respectively for the rat transporters) in S2 proximal tubule cells. Indoxyl sulfate (0.2 and 1 mM) increases superoxide anion and nitric oxide levels in isolated human mononuclear blood cells. It increases serum creatinine and blood urea nitrogen (BUN) levels in the 5 6 nephrectomized rat model of chronic renal failure when administered at a dose of 50 mg kg.
    • ¥ 9850
    6-8周
    规格
    数量
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