MHV370 | TLR7/8 inhibitor | Probechem Biochemicals

Chemical Structure : MHV370

CAS No.: 2205095-75-4

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MHV370 (MHV-370, MHV 370)

货号: PC-20815Not For Human Use, Lab Use Only.

MHV370 (MHV-370) is a potent, selective, orally bioavailable inhibitor of Toll-like receptors 7 and 8 (TLR7/8) with IC50 of 1.1 and 4.5 nM in cell-based assays.

规格	价格	库存
5 mg	￥3980	In stock
10 mg	￥5980	In stock
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

MHV370 (MHV-370) is a potent, selective, orally bioavailable inhibitor of Toll-like receptors 7 and 8 (TLR7/8) with IC50 of 1.1 and 4.5 nM in cell-based assays.
MHV370 potently inhibited CL307- and R848-driven reporter gene activity in cells with IC50 of 15 nM and 7 nM, respectively.
MHV370 displayed no activity against other TLRs (TLR1/2, TLR2/6), tumor necrosis factor (TNF) receptor, and NOD1 at 10 uM.
MHV370 did not lead to cell toxicity at 10 uM, did not block ODN2216/TLR9-dependent IFN-α secretion from isolated human pDCs.
MHV370 potently suppressed production of multiple cytokines following activation of isolated monocytes with the TLR8-specific agonist TL8-0506, i.e., TNF, interleukin-6 (IL-6), and IL-1β.
MHV370 inhibited ssRNA-induced IFN-α and TNF responses on PBMCs with IC50 of 4.1 and 70 nM, respectively.
MHV370 is a potent, selective, and reversible antagonist of TLR7 and TLR8 in humans, and a selective TLR7 antagonist in mice.
MHV370 blocks activation of cell types that drive lupus, including B cells and pDCs.
MHV370 (5 mg, oral) suppresses acute TLR7-dependent immune activation in mice.
MHV370 suppresses ISGs in the TMPD peritonitis model, protects from lupus-like disease in the NZB/W F1 mouse model.

物理化学性质&存储条件

分子量	532.69
分子式	C29H40N8O2
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 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-N-(4-((5-(1,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-4-yl)-3-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)bicyclo[2.2.2]octan-1-yl)morpholine-3-carboxamide

参考文献

1. Phil B Alper, et al. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127366.

2. Stuart Hawtin, et al. Cell Rep Med. 2023 May 16;4(5):101036.

MHV370 (MHV-370, MHV 370)

生物&药学活性

物理化学性质&存储条件

参考文献

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MHV370 (MHV-370, MHV 370)

生物&药学活性

物理化学性质&存储条件

参考文献

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