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Palosuran

更新时间:2026-07-06 21:45:39 采购访问:3次

常用名 ACT 058362; PALOSURAN, CAS号 540769-28-6
价格 ¥需询单/100mg ¥需询单/500mg ¥需询单/1g ¥需询单/5g 纯度 98.0%
备货期 需询单 库存 现货
 产品详情(用途,包装等)
用途:
Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM. IC50 Value: 3.6±0.2 nM [1]Target: Urotensin Receptor (GPR14)in vitro: 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].in vivo: 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].Toxicity: Palosuran was well tolerated. No serious adverse events or dose-related adverse events were reported. No treatment-related pattern was detected for vital signs, clinical laboratory parameters, or electrocardiography parameters [5].
物理化学性质:
CAS号:540769-28-6
常用中文名:ACT 058362; PALOSURAN,
常用英文名:Palosuran
分子式:C25H30N4O2
分子量:418.53100
密度:N/A
沸点:N/A
熔点:N/A
闪点:N/A
储存条件:-20℃

供应商信息

长沙福臻生物科技有限公司 认证供应商

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商品数:2430件
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地址:湖南省长沙市芙蓉区隆平高科技园隆园五路2号
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  • 长沙福臻生物科技有限公司
  • 湖南省 长沙市 芙蓉区
  • 产品名:Palosuran
  • 价格: ¥需询单/100mg ¥需询单/500mg ¥需询单/1g ¥需询单/5g
  • 纯度:98.0%
  • 备货期:需询单
  • 联系人:张经理
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参考价格:$290/10mM*1mLinDMSO
其他供应商价格:
2025-02-05 Palosuran
价格:¥539.9
2024-07-15 Palosuran
价格:需询单
2021-02-06 Palosuran
价格:¥7939.0

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