A TLR8 antagonist
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CU-CPT8m

Item No. 25349

Technical Information
Formal Name
7-(3-methylphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
CAS Number
125079-83-6
Molecular Formula
C14H12N4O
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
Chloroform: 5 mg/mlDMF: 0.2 mg/mlDMSO: 0.2 mg/mlEthanol: slightly soluble
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CU-CPT8m is an antagonist of toll-like receptor 8 (TLR8; Kd = 220 nM; IC50 = 67 nM in a reporter assay).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, S., Hu, Z., Tanji, H., et alSmall-molecule inhibition of TLR8 through stabilization of its resting state. Nat. Chem. Biol. 14(1), 58-64 (2018).