CU-CPT8m 是一种特异性 TLR8 拮抗剂，IC50 为 67 nM。
| Cas No. | 125079-83-6 |
| 别名 | TLR8-specific antagonist |
| 化学名 | 7-(3-methylphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide |
| Canonical SMILES | CC1=CC(C2=CC=NC3=C(C(N)=O)C=NN32)=CC=C1 |
| 分子式 | C14H12N4O |
| 分子量 | 252.3 |
| 溶解度 | Chloroform: 5 mg/ml,DMF: 0.2 mg/ml,DMSO: 0.2 mg/ml,Ethanol: slightly soluble |
| 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 | CU-CPT8m is an antagonist of toll-like receptor 8 (TLR8; Kd = 220 nM; IC50 = 67 nM in a reporter assay). It is selective for TLR8 over a panel of all other human TLRs when used at a concentration of 1 μM. CU-CPT8m (1 μM) inhibits increases in TNF-α and IL-8 mRNA expression induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells. It also inhibits R-848-induced increases in TNF-α protein levels in differentiated THP-1 monocytes and human primary peripheral blood mononuclear cells (PBMCs) in a concentration-dependent manner. CU-CPT8m decreases TNF-α and IL-8 levels in synovial cells derived from patients with osteoarthritis and TNF-α levels in PBMCs derived from patients with rheumatoid arthritis. |
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