R1487 Hydrochloride 是一种高效的选择性 p38α 抑制剂，对 p38α 和 p38β 的 Kd 值分别为 0.2 nM 和 29 nM。
| Cas No. | 449808-64-4 |
| Canonical SMILES | O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC4CCOCC4)N=C3N1C.Cl |
| 分子式 | C19H19ClF2N4O3 |
| 分子量 | 424.83 |
| 溶解度 | DMSO : 20.83 mg/mL (49.03 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α.target: p38α;R1487 (Hydrochloride) potently inhibits cytokine production in a variety of in vitro and in vivo models.[1]R1487 (Hydrochloride) inhibits production of TNFR by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS.[1] References:
[1]. Goldstein DM et al. Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase. J Med Chem. 2011 Apr 14;54(7):2255-65. |
