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Setipiprant

Name: Setipiprant
Brand: TargetMol
SKU: T3520
Price: 132 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.16%

货号 T3520Cas号 866460-33-5

别名 塞替匹仑, KYTH-105, ACT-129968

Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。

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Setipiprant

一键复制产品信息

很棒

纯度: 99.16%

货号 T3520 别名 塞替匹仑, KYTH-105, ACT-129968Cas号 866460-33-5

Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。

规格	价格	库存
2 mg	¥ 132	现货
5 mg	¥ 198	现货
10 mg	¥ 278	现货
25 mg	¥ 446	现货
50 mg	¥ 693	现货
100 mg	¥ 1,090	现货
200 mg	¥ 1,560	待询
1 mL x 10 mM (in DMSO)	¥ 253	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

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常见问题解答

选择批次:

纯度: 99.16%

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资源下载:

COA HNMR LCMS 产品操作手册

产品介绍

Setipiprant AI Summary

Setipiprant exhibits prolonged elimination half-life in human and rat plasma, along with a favorable volume of distribution in Wistar rats. It demonstrates potent antagonist activity at the CRTH2 receptor with high selectivity over the DP1 receptor and significant protein binding in plasma. The compound shows promising oral bioavailability in both beagle dogs and Wistar rats, potent inhibition of CYP enzymes, various antagonist activities at different prostanoid receptors, and strong affinity for the CRTH2 receptor with a low IC50 value. Additionally, it has moderate intrinsic clearance in liver microsomes and hepatocytes, and satisfactory clearance rates in beagle dogs and Wistar rats. Furthermore, Setipiprant exhibits antiviral activity against SARS-CoV-2. It inhibits SARS-CoV-2 induced cytotoxicity of Caco-2 cells by 8.44% at a 10 µM concentration after 48 hours, and shows a slight inhibitory effect (-0.12%) on the cytotoxicity of VERO-6 cells under similar conditions. It also demonstrates inhibition of the SARS-CoV-2 3CL-Pro protease, with an observed effect of -7.312% at a 20 µM concentration. Despite these activities, the compound shows moderate potency (IC50 > 20,000 nM) in inhibiting virus-induced cytotoxic effects in VERO-6 cells. Setipiprant also shows inhibitory activity on the human HDAC6 enzyme, with 34.49% inhibition in an enzymatic assay using a commercial peptide substrate, though it showed -7.96% inhibition with a custom peptide substrate, suggesting a varied interaction dependent on the substrate used..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells.
靶点活性	DP1 (human):1290 nM, CRTH2:6.0 nM, EP2:2600 nM
别名	塞替匹仑, KYTH-105, ACT-129968

化学信息

分子量	402.42
分子式	C₂₄H₁₉FN₂O₃
CAS No.	866460-33-5
Smiles	C(C(O)=O)N1C2=C(C=3C1=CC=C(F)C3)CN(C(=O)C=4C5=C(C=CC4)C=CC=C5)CC2
密度	1.37 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 45 mg/mL (111.82 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.97 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4850 mL	12.4248 mL	24.8497 mL	124.2483 mL
5 mM	0.4970 mL	2.4850 mL	4.9699 mL	24.8497 mL
10 mM	0.2485 mL	1.2425 mL	2.4850 mL	12.4248 mL
20 mM	0.1242 mL	0.6212 mL	1.2425 mL	6.2124 mL
50 mM	0.0497 mL	0.2485 mL	0.4970 mL	2.4850 mL
100 mM	0.0248 mL	0.1242 mL	0.2485 mL	1.2425 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。