CU-CPT-8m|cas 125079-83-6|DC Chemicals

Cas No.:	125079-83-6
Chemical Name:	Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 7-(3-methylphenyl)-
Synonyms:	Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 7-(3-methylphenyl)-;CU-CPT-8m;7-(m-tolyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide;CPD1578
SMILES:	O=C(C1=C2N=CC=C(C3=CC=CC(C)=C3)N2N=C1)N
Formula:	C₁₄H₁₂N₄O
M.Wt:	252.271
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.

In Vitro:

CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67±10 nM and negligible cytotoxicity. The Kd 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 IC50 of 90±10 nM, which is in good agreement with its IC50 value determined in HEK-Blue TLR8 cells[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC70332	CU-CPD107	CU-CPD107 is a TLR8-specific small molecule with unique synergistic agonist activities in the presence of ssRNA, but inactive without the aid of ssRNA.CU-CPD107 significantly inhibited of R848-induced signaling in HEK-Blue hTLR8 cells with an IC50 of 13.7 uM.CU-CPD107 only inhibited synthesized small-molecule agonist-induced TLR8 signaling without affecting other TLRs.CU-CPD107 synergistically increased IFN-β, TNF-α, IL-1β, IL-6, and IL-8 mRNA expression levels in the presence of 5 μg/ml ssRNA40 in HEK-Blue hTLR8 cells, whereas CU-CPD107 alone did not. CU-CPD107 only activated TLR8-mediated signaling in the presence of ssRNA.CU-CPD107 showed no pure agonistic activity, addressing a major challenge that has existed for previous TLR7 and TLR8 agonists as vaccine adjuvants or antiviral drugs.
DC10770	CU-CPT-9a	CU-CPT9a is an antagonist of toll-like receptor 8 (TLR8). It inhibits activation of NF-κB induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells (IC50 = 0.5 nM). CU-CPT9a reverses R-848-induced increases in NF-κB p65, IRAK-4, and TRAF3 protein levels in HEK-Blue cells.
DC10769	CU-CPT-9b	CU-CPT9b is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM).
DC10771	CU-CPT-8m	CU-CPT-8m is a nolve TLR8 inhibitor.
DC10276	C29	C29 is a potential TLR2 inhibitor.