WAY-262611

目录号: GC15753纯度: >98.00%同义词: BML-WN110, Dickkopf-1 Inhibitor, Dkk1 Inhibitor
A Dkk1 inhibitor and Wnt signaling activator

WAY-262611
Cas No.: 1123231-07-1
规格价格库存数量操作
1mg¥204.00现货
1
5mg¥511.00现货
1
10mg¥665.00现货
1
50mg¥2,520.00现货
1
10mM (in 1mL DMSO)¥562.00现货
1

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产品描述 Description

WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay.

WAY-262611 has the most potent activity in the primary assay, low kinase inhibition potential, and high solubility[1].

WAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration. Calvariae from wt mice treated with WAY-262611 shows statistically increased BFR, while similarly treated KO animals are no different from control. This indicates that WAY-262611 is acting via the Wnt β-catenin pathway and most likely through inhibition of Dkk-1[1].

References:
[1]. Pelletier JC, 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.

实验参考方法 Experimental Reference Method

Animal experiment:

Rats: WAY-262611 is dissolved in DMSO and diluted with saline for iv (Rats). WAY-262611 is prepared in 0.5% methylcellulose/2% Tween-80 for po OVX rats14 are treated orally with 5 (po, vehicle=0.5% methylcellulose/2% Tween-80, qd, 28 days) at four doses. Trabecular bone formation rate (BFR) in the tibia is established in all dose groups at the end of the in-life portion of the study. A clear dose response and activity as low as 0.3 mg/kg/day are observed[1]. Mice: To confirm activity via the Wnt pathway, the calvariae of wild type (wt) and Dkk-1 knockout (KO) mice are treated with 5 once a day for 7 days (DMSO solution, sc injection). The KO animals are not expected to respond because of the inherent inability to inhibit a missing target protein, while wild type animals with fully expressed Dkk-1 are expected to show a pharmacological response [1].

References:

[1]. Pelletier JC, 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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1123231-07-1
同义词
BML-WN110, Dickkopf-1 Inhibitor, Dkk1 Inhibitor
化学名
[1-(4-naphthalen-2-ylpyrimidin-2-yl)piperidin-4-yl]methanamine
SMILES
C1CN(CCC1CN)C2=NC=CC(=N2)C3=CC4=CC=CC=C4C=C3
分子式
C20H22N4
分子量
318.42 g/mol
溶解性
≥ 8.95mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

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