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RCGD423

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Chemical Structure| 108237-91-8 同义名 : -
CAS号 : 108237-91-8
货号 : A1006566
分子式 : C15H11BrN2S
纯度 : 97%
分子量 : 331.23
MDL号 : MFCD01123615
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(362.29 mM)，配合低频超声助溶，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 Signalling through glycoprotein 130 (gp130), the common receptor for IL-6 family cytokines, can have both context-specific and cytokine-specific effects on articular chondrocytes. RCGD423 is a small molecule gp130 modulator which can bias signalling towards anti-inflammatory and antidegenerative outputs. This small molecule increased proliferation while reducing apoptosis and hypertrophic responses in adult chondrocytes in vitro. In a rat partial meniscectomy model, RCGD423 greatly reduced chondrocyte hypertrophy, loss and degeneration while increasing chondrocyte proliferation beyond that observed in response to injury. Furthermore, RCGD423 improved cartilage healing in a rat full-thickness osteochondral defect model, increasing proliferation of mesenchymal cells in the defect and also inhibiting breakdown of cartilage matrix in de novo generated cartilage[2]. Treatment of mice skin with 2 topical doses of RCGD423 (50uM) for 48h induced levels of both c-Myc and n-Myc as well as Ldha[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.10mL

3.02mL

1.51mL

30.19mL

6.04mL

3.02mL
参考文献

[1]Shkhyan R, et al. Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repair. Ann Rheum Dis. 2018 May;77(5):760-769.

[2]Shkhyan R, Van Handel B, Bogdanov J, et al. Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repair. Ann Rheum Dis. 2018;77(5):760-769

[3]Flores A, Schell J, Krall AS, et al. Lactate dehydrogenase activity drives hair follicle stem cell activation. Nat Cell Biol. 2017;19(9):1017-1026