CU-CPT9b

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CU-CPT9b 是 Toll 样受体 8 (TLR8；Kd = 21 nM) 的拮抗剂。它抑制 TLR8 激动剂 R-848 在 TLR8 过表达 HEK-Blue 细胞中诱导的 NF-?B 激活，IC50 值为 0.7 nM。

CU-CPT9b is an antagonist of toll-like receptor 8 (TLR8;?Kd = 21 nM).?It inhibits activation of NF-?B induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.

CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7±0.2 nM. ITC experiments have confirmed the strong binding of CU-CPT9b with a Kd of 21 nM. It is shown that CU-CPT-9b binds to the inactive TLR8 dimer in a similar way to CU-CPT8m. CU-CPT9b utilizes hydrogen bonds with G351 and V520*, which are conserved among TLR8/antagonist structures. Additionally, CU-CPT9b forms water-mediated contacts with S516* and Q519*, which are not observed in TLR8/CU-CPT8m structure, suggesting that the enhanced potency of CU-CPT9b derives from the new interactions with these polar residues. The orientation of Y567* also changes to facilitate van der Waals interactions with CU-CPT9b as compared to TLR8/CU-CPT8m.

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CU-CPT-9b | TLR8-specific antagonist 1

Immunology/Inflammation

TLR

TLR8

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2162962-69-6

251.28

C16H13NO2

>98% (HPLC)

DMSO:100 mg/mL (397.96 mM)

Cc1cc(ccc1O)-c1ccnc2cc(O)ccc12

4-(4-Hydroxy-3-methylphenyl)quinolin-7-ol

(-20℃)

With Ice Pack

≥ 2 years