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RCGD423 {[allProObj[0].p_purity_real_show]}

货号:A1006566

RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.

RCGD423 化学结构 CAS号:108237-91-8
RCGD423 化学结构
CAS号:108237-91-8
RCGD423 3D分子结构
CAS号:108237-91-8
RCGD423 化学结构 CAS号:108237-91-8
RCGD423 3D分子结构 CAS号:108237-91-8
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RCGD423 纯度/质量文件 产品仅供科研

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产品名称 P-gp 其他靶点 纯度
Elacridar BCRP 99%+
Zosuquidar 3HCl ++

P-gp, Ki: 60 nM

99%+
SC144 99%+
Tariquidar +++

P-gp, Kd: 5.1 nM

98%
Schizandrin B 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

RCGD423 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].

RCGD423 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

RCGD423 实验方案

计算器
存储液制备 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

RCGD423 技术信息

CAS号108237-91-8
分子式C15H11BrN2S
分子量 331.23
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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