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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Toll-like Receptor (TLR)-M5049
M5049

Chemical Structure : M5049

CAS No.: 2101938-42-3

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M5049 (Enpatoran, M-5049)

货号: PC-72049Not For Human Use, Lab Use Only.

M5049 (Enpatoran, M-5049) is a novel potent, selective TLR7/8 inhibitor with IC50 of 11.1/24.1 nM in HEK NF-kB-luciferase reporter cells assay, repectively

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10 mg ￥2980 In stock
25 mg ￥4580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

M5049 (Enpatoran, M-5049) is a novel potent, selective TLR7/8 inhibitor with IC50 of 11.1/24.1 nM in HEK NF-kB-luciferase reporter cells assay, repectively.
M5049 (Enpatoran) is potent against TLR7 and TLR8 in PBMCs (IL-6 IC50=68.3 and 620 nM) as well as whole blood (IL-6 IC50=2.2 nM).
M5049 (Enpatoran) showed good selectivity and were found to be inactive against TLR3,TLR4 and TLR9 in vitro and in vivo, as wll as against a panel of 389 kinases as off-target profiling and at 1 mM M5049 only inhibited the activity of one kinase more than 50% (CAMKK2)
M5049 (Enpatoran) blocks multiple TLR7/8 RNA ligands. Treatment of BXSB-Yaa mice with M5049 (Enpatoran) led to an improvement in survival and reduction in kidney disease as evidenced by lower proteinuria.

物理化学性质&存储条件

分子量 320.319
分子式 C16H15F3N4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 Month
Shipping
Solubility

50 mM in DMSO (16.1 mg/mL) (Ultrasonic needed)
Chemical Name/SMILES

8-Quinolinecarbonitrile, 5-[(3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl]-

参考文献

1. Vlach J, et al. J Pharmacol Exp Ther. 2021 Mar;376(3):397-409.

2. Port A, et al. Pharmacol Res Perspect. 2021 Oct;9(5):e00842.

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