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抑制剂描述: 产品名称:4-Aminohippuric Acid 产品别名:见爱必信官网 英文别名:4-Aminohippuric Acid 靶点:Human Endogenous Metabolite CAS:61-78-9 纯度:>98% 外观:见爱必信官网 保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述: 4-Aminohippuric Acid是有机阴离子转运系统中典型的底物。4-Aminohippuric acid通过上皮细胞表达的有机阴离子转运体(OAT)而进行转运。 Xenopus laevisoocytes 表达的OAT1调节钠非依赖性的4-Aminohippuric acid吸收,Km 值为 14.3 μM。4-Aminohippuric acid也通过OAT以外的转运体进行转运,包括NPT1和MRP2。 溶解性:Ethanol :2 mg/mL (10.29 mM) 体外研究: 4-Aminohippuric acid is transported via organic anion transporters (OAT) expressed on epithelial cells. OAT1 expressed on Xenopus laevisoocytes mediated sodium-independent 4-Aminohippuric acid uptake with Km of 14.3 μM. 4-Aminohippuric acid is also found to be transported by transporters other than OAT, which includes NPT1 and MRP2. 4-Aminohippuric acid uptake via NPT1 which is transfected and expressed on HEK293 cell, is saturable and followed Michaelis–Menten kinetics with a Km of nearly 2.66 mM and a Vmax value of 940 pmol/mg protein/30 s. Transport rates of 10 mM 4-Aminohippuric acid are 21.9 pmol/ mg protein/ min with membrane vesicles from MRP2 expressed HEK293 cells. This Km for 4-Aminohippuric acid is 880 mM and a Vmax value is 2.3 nmol/mg protein/ min. 体内研究:4-Aminohippuric acid is an endogenous end product which then extracted by kidney cortical cells form plasma. Kinetics of 4-Aminohippuric acid uptake into cortical tubular cells has been measured by stopped flow capillary perfusion methods in rat kidney. A Km for 4-Aminohippuric acid of 0.08 mM and a Jmax of 1.1 pmol/ s/ cm proximal tubular length is determinated. Assuming equal concentrations at equilibrium, a ratio (r) of extracellular space: intracellular space is calculated to be 0.93. The renal extraction ratio of 4-Aminohippuric acid in a normal individual is approximately 0.92.After extraction, most of 4-Aminohippuric acid is actively secreted primarily by the proximal tubules and exclusively eliminated through the kidneys. The 4-Aminohippuric acid clearance is a measure of renal plasma flow, as more than 90% of 4-Aminohippuric acid is extracted by the kidneys from the plasma in a single pass. 4-Aminohippuric acid is also used to measure the functional capacity of the renal tubular secretory mechanism or transport maximum (TmPAH). In rat model of renal failure, tail vein injection of 3.0 mg/kg Uranyl nitrate induced a significant reduced CLPAH (0.89 mL/min/kg) compared with normal rat (29.30 mL/min/kg). Rats with chronic renal failure (CRF) displayed altered pharmacokinetics and renal excretion of 4-Aminohippuric acid. The excreted, filtered and secreted loads of 4-Aminohippuric acid in CRF rats are diminished as compared with Sham rats (μL/min/g, 145 vs. 100, 39 vs. 20, and 108 vs. 70, respectively), accompanied by decrement of approximately 40% OAT1 expression in both homogenates and membranes. Thus, renal elimination of 4-Aminohippuric acid is often measured to reflect the organic anions transport capability of kidney.
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