CU-CPT8m

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-alpha and IL-8 mRNA expression induced by the TLR8 agonist R-848 (Cay-14806) in TLR8-overexpressing HEK-Blue cells. It also inhibits R-848-induced increases in TNF-alpha protein levels in differentiated THP-1 monocytes and human primary peripheral blood mononuclear cells (PBMCs) in a concentration-dependent manner. CU-CPT8m decreases TNF-alpha and IL-8 levels in synovial cells derived from patients with osteoarthritis and TNF-alpha levels in PBMCs derived from patients with rheumatoid arthritis.Formal Name: 7-(3-methylphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide. CAS Number: 125079-83-6. Molecular Formula: C14H12N4O. Formula Weight: 252.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Chloroform: 5 mg/ml, DMF: 0.2 mg/ml, DMSO: 0.2 mg/ml, Ethanol: slightly soluble. lambdamax: 233, 346 nm. SMILES: CC1=CC(C2=CC=NC3=C(C(N)=O)C=NN32)=CC=C1. InChi Code: 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). InChi Key: HNKGGVGQAVODNJ-UHFFFAOYSA-N.