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WAY-262611 95%

WAY-262611

源葉(MedMol)
S82019
1123231-07-1
C20H22N4
318.4155
品牌 貨號(hào) 產(chǎn)品規(guī)格 價(jià)格(RMB) 庫(kù)存（上海） 北京 武漢 南京 購(gòu)買(mǎi)數(shù)量
源葉(MedMol) S82019-5mg 95% ￥590.00元 8 - - -
源葉(MedMol) S82019-10mg 95% ￥780.00元 5 - - -
源葉(MedMol) S82019-50mg 95% ￥2465.00元 3 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(shū)(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

WAY-262611 (BML-WN110, Compound 5) 是一種 beta-catenin (β-Catenin) 的激動(dòng)劑，可增加骨形成速率，在TCF-熒光素酶測(cè)定中的EC50值為0.63 μM。WAY-262611 也是一種 dickkopf 1 (DKK1) 的抑制劑
產(chǎn)品描述： WAY-262611 (BML-WN110, Compound 5) 是一種 beta-catenin (β-Catenin) 的激動(dòng)劑，可增加骨形成速率，在TCF-熒光素酶測(cè)定中的EC50值為0.63 μM。WAY-262611 也是一種 dickkopf 1 (DKK1) 的抑制劑
靶點(diǎn)： DKK1;β-Catenin(TCF-Luciferase assay):0.63 μM(EC50);Wnt/beta-catenin
體外研究：
WAY-262611, the DKK1 inhibitor, blocks DKK1 and restores the GDF5 reduced MMP13 gene expression
體內(nèi)研究：
WAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration
細(xì)胞實(shí)驗(yàn)： Cell lines: Surplus human chondrocytes Concentrations: 0.01 μM, 0.1 μM, 1 μM Incubation Time: 21 days Method: Chondrocytes are resuspended at 1.25×106 cells/ml in basic differentiation media (BDM) consisting of DMEM high glucose supplemented with 100 nM dexamethasone, 1× insulin-transferrin-selenous acid premix (ITS), 1.0 mg/ml human serum albumin supplemented with 5.0 μg/ml linoleic acid, 14 μg/ml L-ascorbic acid 2-phosphate and 1× Penicilline-Streptomycin. The cell suspension is divided into aliquots of 200 μl to each well of an uncoated flat bottom 96-well plate. The plate is centrifuged at 1,500 rpm for 5 min and incubated for 48 h at 37°C in 5% CO2 and 90% relative humidity to allow for pellet formation. After 48 h the culture medium is changed to BDM supplemented with appropriate growth factors (GFs); 2, 10, 100 or 200 ng/ml recombinant GDF5, 50 ng/ml recombinant Wnt3a, 0.5 μM GSK3b inhibitor CHIR-99021, 0.01, 0.1 or 1 μM DKK1 inhibitor WAY-262611. Medium is changed three times per week for 21 days,
動(dòng)物實(shí)驗(yàn)： Animal Models: OVX rats Dosages: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg; 2 mg/kg Administration: Oral gavage; IV
參考文獻(xiàn)：
1. Jeffrey C Pelletier, et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate. J Med Chem. 2009 Nov 26;52(22):6962-5. 2. L Enochson, et al. GDF5 reduces MMP13 expression in human chondrocytes via DKK1 mediated canonical Wnt signaling inhibition. Osteoarthritis Cartilage. 2014 Apr;22(4):566-77.
溶解性： Soluble  in  DMSO、Ethanol、H2O
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 3.141 ml 15.703 ml 31.406 ml
5 mM 0.628 ml 3.141 ml 6.281 ml
10 mM 0.314 ml 1.57 ml 3.141 ml
50 mM 0.063 ml 0.314 ml 0.628 ml
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參考文獻(xiàn)

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