BI-671800|1093108-50-9|-陌孚医药/Medlife

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BI-671800

目录号: PL02171 纯度: ≥99%

CAS No. :1093108-50-9

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中文名称	BI-671800
中文别名	2-[4,6-bis(dimethylamino)-2-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrimidin-5-yl]acetic acid
英文名称	BI-671800
英文别名	BI-671800;BI 671800;721F767LHB;5-Pyrimidineacetic acid, 4,6-bis(dimethylamino)-2-((4-((4-(trifluoromethyl)benzoyl)amino)phenyl)methyl)-;Actimis;2-[4,6-bis(dimethylamino)-2-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]pyrimidin-5-yl]acetic acid;2-(4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl)acetic acid;5-Pyrimidineacetic acid, 4,6-bis(dimethylamino)-2-[[4-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methyl]-
Cas No.	1093108-50-9
分子式	C₂₅H₂₆F₃N₅O₃
分子量	501.50
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

BI-671800 是高特异性的、有效的前列腺素 D2 受体 (DP2/CRTH2) 的拮抗剂，对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC₅₀ 值分别为 4.5 nM 和 3.7 nM。有研究哮喘的潜力。

生物活性

BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC 50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.

性状

Solid

IC50 & Target[1][2]

hCRTH2 4.5 nM (IC50) mCRTH2 3.7 μM (IC

体外研究(In Vitro)

BI-671800 (compound A) exhibits low nM potency as an antagonist of human or mouse CRTH2 in transfected cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice.
BI-671800 (compound A), effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

参考文献

[1]. Boehme SA, et al. A small molecule CRTH2 antagonist inhibits FITC-induced allergic cutaneous inflammation. Int Immunol. 2009 Jan;21(1):81-93.
[2]. Miller D, et al. A randomized study of BI 671800, a CRTH2 antagonist, as add-on therapy in poorly controlled asthma. Allergy Asthma Proc. 2017 Mar 1;38(2):157-164.

溶解度数据	In Vitro: DMSO : 135 mg/mL (269.19 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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