Vidupiprant AMG 853|cas:1169483-24-2|西域试剂

Vidupiprant AMG 853,98.08%

产品编号：Bellancom-14973| CAS NO：1169483-24-2| 分子式：C₂₈H₂₇Cl₂FN₂O₆S| 分子量：609.49

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-14973	￥2550.00	杭州北京（现货）
Bellancom-14973	￥7250.00	杭州北京（现货）
Bellancom-14973	￥11500.00	杭州北京（现货）

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Vidupiprant AMG 853

产品介绍

Vidupiprant (AMG 853) 是一种苯乙酸衍生物，也是一种有效的口服活性的 CRTH2 (DP2) 和 prostanoid D receptor (DP or DP1) 双重拮抗剂，在缓冲液中的 IC₅₀ 分别为 3 nM 和 4 nM，在人血浆中的 IC₅₀ 分别为 8 nM 和 35 nM。Vidupiprant 可用于哮喘的研究。

生物活性

Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC₅₀s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment.

体外研究

Vidupiprant (AMG 853, Compound 2) inhibits the prostaglandin D2 (PGD2)-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a K_b of 0.2 nM. Vidupiprant also inhibits PGD2-induced cAMP response in platelets in 80% human whole blood with a K_b of 4.7 nM, which is significantly improved, as compared to the K_b of 148 nM of AMG 009. In addition, Vidupiprant demonstrates similar antagonist activity in an aequorin assay using CRTH2-transfected HEK 293 cells and an eosinophil shape change assay, as compared to the CRTH2 receptor down-modulation human whole blood assay.

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

体内研究

The significant improvement of DP potency of Vidupiprant (AMG 853, Compound 2) over AMG 009 is also demonstrated in vivo in a guinea pig model of PGD2-induced airway constriction. In this model, airway resistance is measured in response to PGD2 challenge. The in vitro guinea pig DP potency is evaluated in guinea pig whole blood cAMP assay.Vidupiprant has a K_b of 5 nM, while the K_b of AMG 009 is 82 nM.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (164.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6407 mL	8.2036 mL	16.4072 mL
5 mM	0.3281 mL	1.6407 mL	3.2814 mL
10 mM	0.1641 mL	0.8204 mL	1.6407 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: ≥ 2.5 mg/mL (4.10 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.10 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。