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125079-83-6

中文名稱 CPD1578
英文名稱 CU-CPT-8m
CAS 125079-83-6
分子式 C14H12N4O
分子量 252.27
MOL 文件 125079-83-6.mol
更新日期 2024/10/24 11:25:05
125079-83-6 結(jié)構(gòu)式 125079-83-6 結(jié)構(gòu)式

基本信息

中文別名
化合物CU-CPT-8M
7-(間甲苯基)吡唑并[1,5-A]嘧啶-3-甲酰胺
英文別名
CPD1578
CU-CPT-8m
cas 125079-83-6
TLR8-specific antagonist
CU-CPT-8M
CAS 125079-83-6
TLR8 INHIBITOR
7-(m-tolyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 7-(3-methylphenyl)-
所屬類別
生物:拮抗劑

物理化學性質(zhì)

密度1.35±0.1 g/cm3(Predicted)
儲存條件Sealed in dry,Room Temperature
溶解度Chloroform: 5 mg/ml; DMF: 0.2 mg/ml; DMSO: 0.2 mg/ml; Ethanol: slightly soluble
酸度系數(shù)(pKa)12.41±0.50(Predicted)
形態(tài)A crystalline solid
顏色White to off-white
InChIInChI=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)
InChIKeyHNKGGVGQAVODNJ-UHFFFAOYSA-N
SMILESC12=C(C(N)=O)C=NN1C(C1=CC=CC(C)=C1)=CC=N2

常見問題列表

生物活性
CU-CPT-8m 是 TLR8 的特異性拮抗劑,其 IC50 值為 67 nM。
靶點

TLR8

67 nM (IC 50 )

體外研究

CU-CPT-8m is a specific TLR8 antagonist, with an IC 50 of 67±10 nM and negligible cytotoxicity. The K d 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 IC 50 of 90±10 nM, which is in good agreement with its IC 50 value determined in HEK-Blue TLR8 cells.

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