Adavivint

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Chemical Structure| 1467093-03-3 同义名 : SM04690;Lorecivivint
CAS号 : 1467093-03-3
货号 : A591020
分子式 : C29H24FN7O
纯度 : 99%+
分子量 : 505.546
MDL号 : MFCD30489411
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(49.45 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The Wnt pathway plays an important role in cell differentiation, organogenesis, morphogenesis, and tissue remodeling. Adavivint is a small-molecule Wnt pathway inhibitor with an EC50 value of 19.5nM for the TCF/LEF reporter but had no effect on the SV40 luciferase reporter. Treatment of bone-marrow-derived human mesenchymal stem cells (hMSCs; CD29+, CD44+, CD166+, CD105+, CD45−) with 30nM adavivint resulted in a concentration-dependent decrease in the expression of Wnt pathway genes (ASCL1, LEF1, TCF7L2, TCF7, C-MYC, and AXIN2). Adavivint also dose-dependently promoted the aggregation of hMSCs with an EC50 value of 10nM. Compared to DMSO-treated controls, hMSCs treated with adavivint (30nM) for 3 days showed significantly increased expression of Sox9. Adavivint treatment also downregulated the genes associated with tendon or ligament differentiation (COL1A1) and osteoblast differentiation (osteocalcin, alkaline phosphatase, BMP4, RUNX2) in hMSCs. Treatment of adavivint (30nM) for 21 days induced chondrocyte differentiation in mouse chondrogenic ATDC5 cells. Primary mouse embryo calvarial cells exposed to 100 nM of adavivint for 21 days showed increased number and size of Alcian Blue stained chondrocytes compared with DMSO-treated controls. A single IA injection of adavivint (0.3 μg) promoted cartilage growth, improved joint health, decreased cartilage breakdown, and inhibited the Wnt pathway in a rat model of knee osteoarthritis[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.78mL

3.96mL

1.98mL
参考文献

[1]Deshmukh V, Hu H, Barroga C, Bossard C, Kc S, Dellamary L, Stewart J, Chiu K, Ibanez M, Pedraza M, Seo T, Do L, Cho S, Cahiwat J, Tam B, Tambiah JRS, Hood J, Lane NE, Yazici Y. A small-molecule inhibitor of the Wnt pathway (SM04690) as a potential disease modifying agent for the treatment of osteoarthritis of the knee. Osteoarthritis Cartilage. 2018 Jan;26(1):18-27.