WAY-262611 - β-catenin Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEWAY-262611Cat. No.: HY-11035CAS No.: 1123231-07-1分式: CHN分量: 318.42作靶點(diǎn): -catenin作通路: Stem Cell/Wnt儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 42 mg/mL (131.90 mM)* means soluble, but sat

2、uration unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.1405 mL 15.7025 mL 31.4051 mL5 mM 0.6281 mL 3.1405 mL 6.2810 mL10 mM 0.3141 mL 1.5703 mL 3.1405 mL請根據(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，并請注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 WAY-262611翼的-聯(lián)蛋激動(dòng)劑，可增加形成速率，在TCF-熒光素酶測定實(shí)驗(yàn)中的EC50值為0.63 M。IC50 & Targ

3、et EC50: 0.63 M (-Catenin) 1體外研究WAY-262611 has the most potent activity in the primary assay, low kinase inhibition potential, and high1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEsolubility 1.體內(nèi)研究 WAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in thetrab

4、ecular bone formation rate in ovariectomized rats following oral administration. Calvariae from wt micetreated with WAY-262611 shows statistically increased BFR, while similarly treated KO animals are nodifferent from control. This indicates that WAY-262611 is acting via the Wnt -catenin pathway and

5、 mostlikely through inhibition of Dkk-1 1.PROTOCOLAnimal Rats: WAY-262611 is dissolved in DMSO and diluted with saline for iv (Rats). WAY-262611 is prepared inAdministration 1 0.5% methylcellulose/2% Tween-80 for po OVX rats14 are treated orally with 5 (po, vehicle=0.5%methylcellulose/2% Tween-80, q

6、d, 28 days) at four doses. Trabecular bone formation rate (BFR) in the tibiais established in all dose groups at the end of the in-life portion of the study. A clear dose response andactivity as low as 0.3 mg/kg/day are observed 1.Mice: To confirm activity via the Wnt pathway, the calvariae of wild

7、type (wt) and Dkk-1 knockout (KO) miceare treated with 5 once a day for 7 days (DMSO solution, sc injection). The KO animals are not expected torespond because of the inherent inability to inhibit a missing target protein, while wild type animals with fullyexpressed Dkk-1 are expected to show a phar

8、macological response 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Cell Sci. 2019 Apr 26. pii: jcs.228478. Evid-Based Compl Alt. 2019 May. SSRN. 2019 Apr.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Pelletier JC, et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases boneformation rate. J Med Chem. 2009 Nov 26;52(22):6962-5.McePdfHeightCaution: Product has not been fully validated for medical app