BI-671800 - Prostaglandin Receptor Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBI-671800Cat. No.: HY-114141CAS No.: 1093108-50-9分式: CHFNO分量: 501.5作靶點(diǎn): Prostaglandin Receptor作通路: GPCR/G Protein儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 135 mg/

2、mL (269.19 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.9940 mL 9.9701 mL 19.9402 mL5 mM 0.3988 mL 1.9940 mL 3.9880 mL10 mM 0.1994 mL 0.9970 mL 1.9940 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)

3、配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.25 mg/mL (4.49 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.25 mg/mL (4.49 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChem

4、E物活性 BI-671800特異性的、有效的前列腺素 D2 受體 (DP2/CRTH2) 的拮抗劑，其對(duì)和 CRTH2 轉(zhuǎn)染細(xì)胞中PGD2 結(jié)合 CRTH2 的 IC50 值分別為 4.5 nM 和 3.7 nM 1。有治療哮喘的潛能 2。IC50 & Target hCRTH2 mCRTH24.5 nM (IC50, in CRTH2 transfected cells) 3.7 nM (IC50, in CRTH2 transfected cells)體外研究 BI-671800 (compound A) exhibits low nM potency as an antagonist o

5、f human or mouse CRTH2 in transfectedcells 1.體內(nèi)研究 BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice 1.BI-671800 (compound A), effectively blocks edema formation and greatly reduces the inflammatory infiltrateand skin pathology observed in drug vehicle-treated ani

6、mals 3.Animal Model: 6-8-week-old age- and sex-matched BALB/c mice (mice were sensitized for 14 days,challenged intranasally) 1.Dosage: 10-0.1 mg/kgAdministration: Oral gavage for 4 weeksResult: Shows significant inhibition of AHR in mice.REFERENCES1. Boehme SA, et al. A small molecule CRTH2 antagon

7、ist inhibits FITC-induced allergic cutaneous inflammation. Int Immunol. 2009Jan;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 AsthmaProc. 2017 Mar 1;38(2):157-164.3. Lukacs NW, et al. CRTH2 antagonism significantly ameliorates airway hyperreactivity and downregulates inflammation-induced genes ina mouse model of airway inflammation. Am J Physiol Lung Cell Mol Physiol. 2008 Nov;295(5):L767-79.McePdfHeightCaution: Product has not been fully validated for medical applications.For