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LDN-193189 HCl

LDN-193189 HCl

产品编号 T6158   CAS 1062368-62-0
别名: LDN193189 Hydrochloride

LDN-193189 HCl (LDN193189 Hydrochloride) 是一种选择性 BMP I 型受体激酶抑制剂。

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LDN-193189 HCl Chemical Structure
LDN-193189 HCl, CAS 1062368-62-0
规格 价格/CNY 货期 数量
1 mg ¥ 447 现货
2 mg ¥ 645 现货
5 mg ¥ 858 现货
10 mg ¥ 1,390 现货
25 mg ¥ 2,530 现货
50 mg ¥ 3,530 现货
100 mg ¥ 4,970 现货
1 mL * 10 mM (in DMSO) ¥ 996 现货
其他形式的 LDN-193189 HCl:
产品目录号及名称: LDN-193189 HCl (T6158)
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选择批次  
纯度: 100%
纯度: 99.49%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 LDN-193189 HCl (LDN193189 Hydrochloride) is a selective BMP type I receptor kinases inhibitor.
靶点活性 ALK6:16.7 nM, ALK1:0.8 nM, ALK3:5.3nM, ALK2:0.8nM
体外活性 LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. [1] A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. [4]
体内活性 In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities. [1] LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. [2] In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors. [3] In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. [4]
激酶实验 C2C12 cells are seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. The wells are treated in quadruplicate with BMP ligands and LDN-193189 or vehicle. The cells are collected after 6 d in culture in 50 μL Tris-buffered saline and 1% Triton X-100. The lysates are added to p-nitro-phenylphosphate reagent in 96-well plates for 1 h and then evaluated alkaline phosphatase activity (absorbance at 405 nm). Cell viability are measured and quantity by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements[1].
细胞实验 Concentrations: 3 μM
别名 LDN193189 Hydrochloride
分子量 442.94
分子式 C25H22N6·HCl
CAS No. 1062368-62-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10 mg/mL (22.58 mM), Sonification is recommended

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2576 mL 11.2882 mL 22.5764 mL 56.4411 mL
5 mM 0.4515 mL 2.2576 mL 4.5153 mL 11.2882 mL
10 mM 0.2258 mL 1.1288 mL 2.2576 mL 5.6441 mL
20 mM 0.1129 mL 0.5644 mL 1.1288 mL 2.8221 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Yu PB, et al. Nat Med, 2008, 14(12), 1363-1369. 2. Cannon JE, et al. Br J Pharmacol, 2010, 161(1), 140-149. 3. Lee YC, et al. Cancer Res, 2011, 71(15), 5194-5203. 4. Derwall M, et al. Arterioscler Thromb Vasc Biol, 2012, 32(3), 613-622.
SB 525334 EW-7195 Belizatinib CH5424802 analog ASP3026 AZ7550 ALK inhibitor 1 Ceritinib

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 经典已知活性库 激酶抑制剂库 抗癌化合物库 血管生成库 成骨分子库 抗肺癌化合物库 已知活性化合物库 抑制剂库 NO PAINS 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

LDN-193189 HCl 1062368-62-0 Angiogenesis Tyrosine Kinase/Adaptors ALK LDN 193189 Hydrochloride LDN 193189 HCl LDN-193189 Hydrochloride LDN193189 HCl LDN193189 Hydrochloride Inhibitor inhibitor inhibit

 

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