CPD1578
| 中文名称 | CPD1578 |
|---|---|
| 中文同义词 | 7-(间甲苯基)吡唑并[1,5-A]嘧啶-3-甲酰胺;化合物CU-CPT-8M |
| 英文名称 | CU-CPT-8m |
| 英文同义词 | CPD1578;CU-CPT-8m;cas 125079-83-6;CU-CPT-8M;CAS 125079-83-6 ;TLR8 INHIBITOR;TLR8-specific antagonist;7-(m-tolyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide;Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 7-(3-methylphenyl)-;CU CPT 8m,inhibit,Toll-like Receptor (TLR),CUCPT8m,Inhibitor |
| CAS号 | 125079-83-6 |
| 分子式 | C14H12N4O |
| 分子量 | 252.27 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 125079-83-6.mol |
| 结构式 |  |
CPD1578 性质
| 密度 | 1.35±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Sealed in dry,Room Temperature |
| 溶解度 | 氯仿：5mg/mL； DMF：0.2mg/mL； DMSO：0.2mg/mL；乙醇：微溶 |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 12.41±0.50(Predicted) |
| InChI | InChI=1S/C14H12N4O/c1-9-3-2-4-10(7-9)12-5-6-16-14-11(13(15)19)8-17-18(12)14/h2-8H,1H3,(H2,15,19) |
| InChIKey | HNKGGVGQAVODNJ-UHFFFAOYSA-N |
| SMILES | C12=C(C(N)=O)C=NN1C(C1=CC=CC(C)=C1)=CC=N2 |
|
TLR8 67 nM (IC 50 ) |
CU-CPT-8m is a specific TLR8 antagonist, with an IC 50 of 67±10 nM and negligible cytotoxicity. The K d value of CU-CPT-8m is determined to be 220 nM. CU-CPT-8m only reduces the proinflammatory response in the TLR8-overexpressing cells strongly supports that CU-CPT-8m directly recognizes TLR8 in cells. It is particularly notable that TLR7 signaling is not affected at concentrations up to 75 μM. TLR7 and TLR8 are closely related and share many common ligands. Treatment of 1 μM CU-CPT-8m completely abolishes the elevation of TNF-α and IL-8 mRNA levels induced by R848. CU-CPT-8m inhibits R848-induced TNF-α production in the differentiated THP-1 monocytes cells in a dose-dependent manner with an IC 50 of 90±10 nM, which is in good agreement with its IC 50 value determined in HEK-Blue TLR8 cells.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-112050 | CU-CPT-8m | 1 mg | 502元 | |
| 2024/01/25 | HY-112050 | CPD1578 CU-CPT-8m | 125079-83-6 | 5mg | 1000元 |