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Laropiprant

Cat. No. 7343 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective prostaglandin D2 receptor antagonist
化学名： (3R)-4-[(4-Chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)cyclopent[b]indole-3-acetic acid
纯度： ≥98% (HPLC)
说明书
引用文献
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Laropiprant

Laropiprant is a potent and selective prostaglandin D2 receptor antagonist (IC50 = 0.09 nM in washed platelets; Ki = 0.57). It exhibits selectivity for binding to PGD2 receptors over other prostanoid receptors (Ki values are ≥ 2.95 nM for TP, EP1, EP2, EP3, EP4, FP and IP). Laropiprant promotes coagulation of whole blood ex vivo and reduces bleeding time in mice in vivo. In a mouse model of intracerebral hemorrhage, Laropiprant reduces lesion volume and attenuates neurological deficit scores. The compound also reduces Niacin (Cat. No. 4106) induced vasodilation.

化合物库 for Laropiprant

Laropiprant is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for Laropiprant

分子量 435.9
公式 C21H19ClFNO4S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 571170-77-9
PubChem ID 9867642
InChI Key NXFFJDQHYLNEJK-CYBMUJFWSA-N
Smiles C(N1C=2C(C3=C1[C@@H](CC(O)=O)CC3)=CC(F)=CC2S(C)(=O)=O)C4=CC=C(Cl)C=C4

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Laropiprant

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 43.59 100
ethanol 21.8 50

制备储备液 for Laropiprant

以下数据基于产品分子量 435.9。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.29 mL 11.47 mL 22.94 mL
5 mM 0.46 mL 2.29 mL 4.59 mL
10 mM 0.23 mL 1.15 mL 2.29 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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参考文献 for Laropiprant

参考文献是支持产品生物活性的出版物。

Sturino et al (2007) Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J.Med.Chem. 50 794 PMID: 17300164

Kong et al (2017) Niacin promotes cardiac healing after myocardial infarction through activation of the myeloid prostaglandin D2 receptor subtype 1. J.Pharmacol.Exp.Ther. 360 435 PMID: 28057839

Ahmad et al (2017) Efficacy of Laropiprant in minimizing brain injury following experimental intracerebral hemorrhage. Sci.Rep. 7 9489 PMID: 28842638

If you know of a relevant reference for Laropiprant, please let us know.

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关键词: Laropiprant, Laropiprant supplier, prostaglandin, D2, receptor, antagonist, potent, selective, PGD2, DP, Prostanoid, Receptors, 7343, Tocris Bioscience

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