貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S82019-5mg	95.9%	￥590.00 S82019-5mg ￥590.00 現(xiàn)貨	8 8	-	-	-
S82019-10mg	95.9%	￥780.00 S82019-10mg ￥780.00 現(xiàn)貨	5 5	-	-	-
S82019-50mg	95.9%	￥2465.00 S82019-50mg ￥2465.00 現(xiàn)貨	3 3	-	-	-

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：

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

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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批號(hào)：JS298415 貨號(hào)：S20001-25g
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