WAY-262611

製品コードS9828 バッチS982801

印刷

化学情報

Synonyms

BML-WN110

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₀H₂₂N₄

分子量

318.42

CAS No.

1123231-07-1

Solubility (25°C)*

体外

DMSO

64 mg/mL (200.99 mM)

Water

10 mg/mL (31.4 mM)

Ethanol

10 mg/mL (31.4 mM)

体内（毎回新しく調製した物を用意してください）

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.25mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.32mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 6.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1).
in vitro	WAY-262611, the DKK1 inhibitor, blocks DKK1 and restores the GDF5 reduced MMP13 gene expression.^[2]
in vivo	WAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Surplus human chondrocytes
	濃度	0.01 μM, 0.1 μM, 1 μM
	反応時間	21 days
	実験の流れ	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, whereafter the pellets are snap-frozen in liquid nitrogen and stored at -80°C.
動物実験	動物モデル	OVX rats
	投薬量	0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg; 2 mg/kg
	投与方法	Oral gavage; IV

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Decreased expression of GEM in osteoarthritis cartilage regulates chondrogenic differentiation via Wnt/β-catenin signaling [ J Orthop Surg Res, 2023, 18(1):751]	PubMed: 37794464
Osteoblast/osteocyte-derived interleukin-11 regulates osteogenesis and systemic adipogenesis [ Nat Commun, 2022, 13(1):7194]	PubMed: 36424386

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。