WAY-262611
(Synonyms: BML-WN110, Dickkopf-1 Inhibitor, Dkk1 Inhibitor) 目录号 : GC15753A Dkk1 inhibitor and Wnt signaling activator
Cas No.:1123231-07-1
Sample solution is provided at 25 µL, 10mM.
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.
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. |
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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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。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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