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WAY-262611 Sale

(Synonyms: BML-WN110, Dickkopf-1 Inhibitor, Dkk1 Inhibitor) 目录号 : GC15753

A Dkk1 inhibitor and Wnt signaling activator

WAY-262611 Chemical Structure

Cas No.:1123231-07-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,029.00
现货
10mg
¥798.00
现货
50mg
¥3,077.00
现货

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Sample solution is provided at 25 µL, 10mM.

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

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.

化学性质

Cas No. 1123231-07-1 SDF
别名 BML-WN110, Dickkopf-1 Inhibitor, Dkk1 Inhibitor
化学名 [1-(4-naphthalen-2-ylpyrimidin-2-yl)piperidin-4-yl]methanamine
Canonical SMILES C1CN(CCC1CN)C2=NC=CC(=N2)C3=CC4=CC=CC=C4C=C3
分子式 C20H22N4 分子量 318.42
溶解度 ≥ 8.95mg/mL in DMSO 储存条件 Store at -20°C
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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。
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1 mg 5 mg 10 mg
1 mM 3.1405 mL 15.7025 mL 31.4051 mL
5 mM 0.6281 mL 3.1405 mL 6.281 mL
10 mM 0.3141 mL 1.5703 mL 3.1405 mL
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