Rodatristat ethyl KAR5585|cas:1673571-51-1|西域试剂

Rodatristat ethyl KAR5585

产品编号：Bellancom-101124| CAS NO：1673571-51-1| 分子式：C₂₉H₃₁ClF₃N₅O₃| 分子量：590.04

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-101124		￥9200.00	杭州北京（现货）
Bellancom-101124		￥14500.00	杭州北京（现货）

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Rodatristat ethyl KAR5585

产品介绍

Rodatristat ethyl (KAR5585) 是一种首创的,具有口服活性的 tryptophan hydroxylase 1 (TPH1) 抑制剂，具有体外纳摩尔浓度，可降低 5-hydroxytryptamine (5-HT) 的水平并显着降低肺动脉高压 (PAH)，

生物活性

Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH).

体外研究

体内研究

Rodatristat ethyl (100 or 200 mg/kg; oral administration; once daily; for 28 days; male Sprague-Dawley rats) treatment decreases erum, gut and lung 5-HT levels in a dose-dependent manner and significantly reduces pulmonary arterial pressure, and pulmonary vessel wall thickness and occlusion in male rats with monocrotaline (MCT).

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

Animal Model:	Male Sprague-Dawley rats (175-200 g)
Dosage:	100 mg/kg or 200 mg/kg
Administration:	Oral administration; once daily; for 28 days
Result:	Decreased serum, gut and lung 5-HT levels in a dose-dependent manner and significantly reduced pulmonary arterial pressure, and pulmonary vessel wall thickness and occlusion in male rats.

体内研究

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

Animal Model:	Male Sprague-Dawley rats (175-200 g)
Dosage:	100 mg/kg or 200 mg/kg
Administration:	Oral administration; once daily; for 28 days
Result:	Decreased serum, gut and lung 5-HT levels in a dose-dependent manner and significantly reduced pulmonary arterial pressure, and pulmonary vessel wall thickness and occlusion in male rats.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (423.70 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6948 mL	8.4740 mL	16.9480 mL
5 mM	0.3390 mL	1.6948 mL	3.3896 mL
10 mM	0.1695 mL	0.8474 mL	1.6948 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。-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 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.53 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。