化合物Palosuran hydrochloride T4689

Product Introduction
Bioactivity


英文名: Palosuran hydrochloride 540769-28-6(free base）

描述: Palosuran hydrochloride 540769-28-6(free base) (ACT-058362 hydrochloride) 是一种新型强效特异性人 UT 受体拮抗剂，IC50 为 3.6±0.2 nM。

体外活性: Palosuran inhibited 125I-U-II binding to human UT receptors in membrane preparations from CHO cells carrying the human UT receptors almost as potently as cold U-II, with an IC50 of 3.6 ± 0.2 nM. On cells, the inhibitory binding potency of palosuran against human UT receptor was lower than on membranes (IC50 = 46.2 ± 13 nM on TE 671 cells and 86 ± 30 nM on recombinant CHO cells). Compared with the human UT receptor, the binding inhibitory potency of palosuran against the rat UT receptor was lower in membrane preparation (400-fold), as well as in cells (>120-fold) [1].

体内活性: Long-term treatment of streptozotocin-induced diabetic rats with palosuran improved survival, increased insulin, and slowed the increase in glycemia, glycosylated hemoglobin, and serum lipids. Furthermore, palosuran increased renal blood flow and delayed the development of proteinuria and renal damage [2]. Palosuran was rapidly absorbed with maximum plasma concentrations at 1 hour after drug administration. The accumulation factor was 1.7 (geometric mean) (95% confidence interval, 1.3 to 2.1).Palosuran was well tolerated [3]. In mesenteric vessels, palosuran treatment up-regulated expression of RhoA and Rho-kinase, increased Rho-kinase-activity, and diminished nitric oxide (NO)/cyclic guanosine 3',5'-monophosphate (cGMP) signaling. Moreover, palosuran increased renal blood flow, sodium, and water excretion in BDL rats [4].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : >30 mg/mL


关键字: Palosuran hydrochloride 540769-28-6(free base) | ACT058362 Hydrochloride | ACT-058362 Hydrochloride | Palosuran hydrochloride 540769286(free base） | Palosuran hydrochloride 540769 28 6(free base） | ACT 058362 Hydrochloride

相关产品: ATC 0175 hydrochloride | GPR120 Agonist 1 | Ginsenoside Rb2 | Kisspeptin 234 acetate(1145998-81-7 free base) | TUG-891 | MK 1903 | AZD1981 | GSK256073 | TUG-469 | Questiomycin A

相关库: Endocrinology-Hormone Compound Library | NO PAINS Compound Library

化合物Palosuran hydrochloride T4689信息由TargetMol中国为您提供，如您想了解更多关于化合物Palosuran hydrochloride T4689报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途