| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B408984-1ml |
1ml |
现货  |
|
| 英文别名 | PS540446 | Pyrrolo[2,1-f][1,2,4]triazine-6-carboxamide, 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propyl- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | BMS-582949 |
| 生化机理 | BMS-582949 (PS540446) 是一种强效的选择性 p38 丝裂原活化蛋白激酶（p38 MAPK）抑制剂，IC50 为 13nM，可同时抑制 p38 激酶活性和 p38 的活化。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | MAP 激酶 p38 alpha 抑制剂 |
| 产品介绍 |
Information BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38. BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop. In vivo The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM•h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively. cell lines：Human colon carcinoma cell line HT-29 Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 3.269 |
|---|---|
| hba_count | 4 |
| HBD Count | 3 |
| Rotatable Bond | 7 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CCCNC(=O)C1=C[N]2N=CN=C(NC3=CC(=CC=C3C)C(=O)NC4CC4)C2=C1C |
| 分子量 | 406.48 |
| Reaxy-Rn | 11821218 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11821218&ln= |
| DMSO(mg / mL) Max Solubility | 81 |
|---|---|
| DMSO(mM) Max Solubility | 199.27 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 11821218 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11821218&ln= |
| Concentration(Compounding value) | 9-11(mmol/L) |
|---|---|
| Appearance(B408984) | Light-yellow Liquid |
| Record the entire process by video | Conform |
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