An antagonist of TLR8 (Kd = 220 nM; IC50 = 67 nM in a reporter assay); is selective for TLR8 over a panel of all other human TLRs at 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 at 1 μM; inhibits R-848-induced increases in TNF-α protein levels in differentiated THP-1 monocytes and human PBMCs in a concentration-dependent manner; 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.

CU-CPT8m – 25 mg

Brand:
Cayman
CAS:
125079-83-6
Storage:
-20
UN-No:
Non-Hazardous - /

CU-CPT8m is an antagonist of toll-like receptor 8 (TLR8; Kd = 220 nM; IC50 = 67 nM in a reporter assay).{35162} 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 (Item No. 14806) 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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SKU: 25349 - 25 mg Category:

Description

An antagonist of TLR8 (Kd = 220 nM; IC50 = 67 nM in a reporter assay); is selective for TLR8 over a panel of all other human TLRs at 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 at 1 μM; inhibits R-848-induced increases in TNF-α protein levels in differentiated THP-1 monocytes and human PBMCs in a concentration-dependent manner; 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.

Formal name: 7-(3-methylphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide

Synonyms: 

Molecular weight: 252.3

CAS: 125079-83-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity|Pattern Recognition

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