Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB-505124 hydrochloride 是TGF-βI 型受体(ALK4,ALK5,ALK7) 的选择性抑制剂,对 ALK4,ALK5 的IC50值分别为 129 nM 和 47 nM,对 ALK1,2,3 或 6 无作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 348 | 5日内发货 | ||
5 mg | ¥ 630 | 5日内发货 |
SB-505124 hydrochloride 的其他形式现货产品:
产品描述 | SB-505124 hydrochloride functions as a selective, concentration-dependent inhibitor targeting TGF-β Receptor type I (ALK4, ALK5, ALK7), exhibiting IC50 values of 129 nM for ALK4 and 47 nM for ALK5. Notably, it does not affect ALK1, 2, 3, or 6. |
体外活性 | SB-505124 shows no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC 50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells [1]. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro [2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC [3]. |
体内活性 | SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but SB-505124 administered with a single dose of Carboplatin (60 mg/kg) causes durable responses without the need for maintenance therapy in five animals [4]. Animal Model: C57Bl6 mice with A549 xenografts [4] Dosage: 5 mg/kg Administration: I.p.; daily Result: Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals. |
分子量 | 371.87 |
分子式 | C20H22ClN3O2 |
CAS No. | 356559-13-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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