产品说明书

HPGDS inhibitor 2

Print
Chemical Structure| 2101626-26-8 同义名 : MFCD32067944
CAS号 : 2101626-26-8
货号 : A1155033
分子式 : C20H24F2N2O3
纯度 : 99%
分子量 : 378.413
MDL号 : MFCD32067944
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(383.18 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 H-PGDS (hematopoietic prostaglandin D synthase) is a member of the σ-class of glutathione-S-transferases, expressed in dendritic cells and Langerhans cells of skin, Kupffer cells in the liver, dendritic cells in the thymus, microglia in the brain, the oviduct, and megakaryocytes in the bone marrow, as well as in mast cells, eosinophils, and activated Th2 cells in many tissues. It has been implicated in asthma, allergic rhinitis, Krabbe disease, Duchenne muscular dystrophy and lupus. GSK-2894631A is a selective and potent H-PGDS inhibitor with IC50 value of 9.9nM. It exhibited good murine pharmacokinetics, dose-dependently attenuated PGD2 production in a mast cell degranulation assay. GSK-2894631A attenuated PGD2 release to baseline levels in a dose-dependent manner with an ED50 of 0.032mg/kg a murine mast cell degranulation model of inflammation orally dosed of GSK-2894631A at 0.03mg/kg to 3mg/kg[2].
作用机制 GSK-2894631A binds to the ligand binding site of hH-PGDS.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.21mL

2.64mL

1.32mL

26.43mL

5.29mL

2.64mL
参考文献

[1]Deaton DN, Do Y, et al. The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478.

[2]Deaton DN, Do Y, Holt J, Jeune MR, Kramer HF, Larkin AL, Orband-Miller LA, Peckham GE, Poole C, Price DJ, Schaller LT, Shen Y, Shewchuk LM, Stewart EL, Stuart JD, Thomson SA, Ward P, Wilson JW, Xu T, Guss JH, Musetti C, Rendina AR, Affleck K, Anders D, Hancock AP, Hobbs H, Hodgson ST, Hutchinson J, Leveridge MV, Nicholls H, Smith IED, Somers DO, Sneddon HF, Uddin S, Cleasby A, Mortenson PN, Richardson C, Saxty G. The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478. doi: 10.1016/j.bmc.2019.02.017. Epub 2019 Feb 11. PMID: 30858025.