| 规格 | 价格 | 库存 | 数量 |
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| 10 mM * 1 mL in DMSO |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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纯度: ≥98%
| 靶点 |
ALK (IC50 = 14.3 nM)
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| 体外研究 (In Vitro) |
研究发现，SB525334 (1 μM) 可减少家族性特发性肺动脉高压 (iPAH) 肺动脉平滑肌细胞 (PASMC) 的增殖，IC50 为 295 nM。在用0.625ng/ml TGF-β1刺激前15分钟观察效果，并在6天后进行评估。
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| 体内研究 (In Vivo) |
在肺动脉高压 (PAH) 大鼠模型中，SB525334（3-30 mg/kg；口服；第 17 至 35 天每天一次）可显着逆转肺动脉压[2]。
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| 酶活实验 |
SB-525334（6-[2-叔丁基-5-（6-甲基-吡啶-2-基）-1H-咪唑-4-基]-喹喔啉）已被表征为转化生长因子-β1（TGF-β1）受体、激活素受体样激酶（ALK5）的强效和选择性抑制剂。该化合物以14.3nM的IC（50）抑制ALK5激酶活性，并且作为ALK4的抑制剂的效力低约4倍（IC（50＝58.5nM）。SB-525334作为ALK2、ALK3和ALK6的抑制剂是无活性的（IC（50）>10000 nM）[1]。
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| 细胞实验 |
细胞增殖测定[2]
细胞类型： PASMC 细胞 测试浓度： 1 μM 孵育时间： Pre - 孵育 15 分钟（然后用 0.625 ng/ml TGF-β1 刺激），6 天后评估 实验结果： 以 IC50 抑制 TGF-β1 介导的家族性 iPAH PASMC 增殖295纳米。 |
| 动物实验 |
Animal/Disease Models: Adult male SD (Sprague-Dawley) rats (MCT rat model of pulmonary hypertension)[2]
Doses: 3, 30 mg/kg Route of Administration: Oral administration; daily from days 17 to 35 Experimental Results: decreased the proportion of fully muscularized vessels to 28% at 3 mg/kg and returned fully muscularized vessel distribution beyond that seen at day 17 and approaching the phenotype observed in saline-exposed controls at 30 mg/kg. |
| 参考文献 |
[1]. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951.
[2]. Thomas M, et al. ALK5 mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline. [3]. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10), 3087-3899. |
| 分子式 |
C21H21N5
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|---|---|---|
| 分子量 |
343.42
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| 精确质量 |
343.179688
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| 元素分析 |
C, 73.44; H, 6.16; N, 20.39
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| CAS号 |
356559-20-1
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| 相关CAS号 |
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| 外观&性状 |
Yellow to orange solid
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| LogP |
4.05
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| tPSA |
67.350
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| SMILES |
CC1=CC=CC(C2=C(C3=CC=C4N=CC=NC4=C3)N=C(C(C)(C)C)N2)=N1
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| InChi Key |
DKPQHFZUICCZHF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)
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| 化学名 |
6-(2-(tert-butyl)-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)quinoxaline
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| 别名 |
SB 525334; SB-525334; SB525334
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 5% DMSO+corn oil:20 mg/mL 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9119 mL | 14.5594 mL | 29.1189 mL | |
| 5 mM | 0.5824 mL | 2.9119 mL | 5.8238 mL | |
| 10 mM | 0.2912 mL | 1.4559 mL | 2.9119 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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 PASMCs derived from iPAH patients were plated at equal cell densities in 96-well plates.
Echocardiographic measurement of pulmonary hypertensive parameters in animals.Am J Pathol.2009 Feb;174(2):380-9. |
RV systolic pressure levels (A) and Fulton index measures (RV/LV + S weight ratio) (B) in rats exposed to MCT or saline-negative control.Am J Pathol.20 |
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