Palosuran hydrochloride ACT-058362 hydrochloride|cas:2469274-58-4|西域试剂

Palosuran hydrochloride ACT-058362 hydrochloride,98.67%

产品编号：Bellancom-10655A| CAS NO：2469274-58-4| 分子式：C₂₅H₃₁ClN₄O₂| 分子量：454.99

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货号	价格	库存与货期
Bellancom-10655A	￥2325.00	杭州北京（现货）
Bellancom-10655A	￥3534.00	杭州北京（现货）
Bellancom-10655A	￥9950.00	杭州北京（现货）

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Palosuran hydrochloride ACT-058362 hydrochloride

产品介绍

Palosuran hydrochloride (ACT-058362 hydrochloride) 是一种有效，选择性和具有口服活性的 urotensin II receptor 受体拮抗剂，对于表达人重组受体的 CHO 细胞膜的 IC₅₀ 值为 3.6 nM。Palosuran hydrochloride 可改善糖尿病大鼠的胰腺和肾脏功能。

生物活性

Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC₅₀ of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats.

体外研究

Palosuran (8 h) inhibits ¹²⁵I-U-II binding to human UT receptor, with IC₅₀s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells.
Palosuran inhibits Ca²⁺ mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC₅₀s of 17 and >10000 nM, respectively.
Palosuran (0.12-10000 nM; 20 min) inhibits human U-II induced MAPK phosphorylation in a dose-dependent manner in recombinant CHO cells, with an IC₅₀ of 150 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure.
Palosuran (300 mg/kg/d; p.o. for 16 weeks) improves the survival, increases insulin, and slows the increase in glycemia, glycosylated hemoglobin, and serum lipids in streptozotocin-induced diabetic rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar rats with renal ischemia and reperfusion
Dosage:	20 mg/kg/h for 135 min
Administration:	I.v. (continuous infusion) for 135 min
Result:	Restored renal blood flow to baseline values at 30 min after reperfusion and by 60 min increased renal blood flow by 12% above baseline values. Did not significantly alter mean arterial blood pressure (MAP) and heart rate (HR).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar rats with renal ischemia and reperfusion
Dosage:	20 mg/kg/h for 135 min
Administration:	I.v. (continuous infusion) for 135 min
Result:	Restored renal blood flow to baseline values at 30 min after reperfusion and by 60 min increased renal blood flow by 12% above baseline values. Did not significantly alter mean arterial blood pressure (MAP) and heart rate (HR).

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (109.89 mM; Need ultrasonic)

H₂O : 7.14 mg/mL (15.69 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1979 mL	10.9893 mL	21.9785 mL
5 mM	0.4396 mL	2.1979 mL	4.3957 mL
10 mM	0.2198 mL	1.0989 mL	2.1979 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.49 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。