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首页 / 抑制剂/激动剂 / 免疫/炎症 / PG Synthase / HPGDS inhibitor 2

HPGDS inhibitor 2 {[allProObj[0].p_purity_real_show]}

货号：A1155033 同义名： MFCD32067944

GSK-2894631A is a highly potent and selective HPGDS inhibitor with IC50 value of 9.9nM.

HPGDS inhibitor 2 化学结构 CAS号：2101626-26-8
HPGDS inhibitor 2 化学结构
CAS号：2101626-26-8
HPGDS inhibitor 2 3D分子结构
CAS号：2101626-26-8
HPGDS inhibitor 2 化学结构 CAS号：2101626-26-8
HPGDS inhibitor 2 3D分子结构 CAS号：2101626-26-8
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HPGDS inhibitor 2 纯度/质量文件 产品仅供科研

货号：A1155033 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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HPGDS inhibitor 2 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]

HPGDS inhibitor 2 动物研究

Dose Mice: 0.03 mg/kg - 3 mg/kg[1] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Mice[1]
Dose 0.03 mg/kg - 3 mg/kg
Administration p.o.
F 0.61
Papp 240 nm/s
T1/2 3.8 h
CL 5.6 ml/min/kg
FaS-SIF 0.070 mg/ml
Vss 1.7 L/kg
DNAUC 1800 ng/h/ml

HPGDS inhibitor 2 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.

HPGDS inhibitor 2 实验方案

计算器
存储液制备 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

HPGDS inhibitor 2 技术信息

CAS号2101626-26-8
分子式C20H24F2N2O3
分子量 378.413
别名 MFCD32067944
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
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

Tags: HPGDS inhibitor 2 | 2101626-26-8 | HPGDS inhibitor2 | HPGDS inhibitor-2 | PGE synthase Inhibitor | Immunology/Inflammation | PGE synthase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | HPGDS inhibitor 2 纯度/质量文件 | HPGDS inhibitor 2 生物活性 | HPGDS inhibitor 2 动物研究 | HPGDS inhibitor 2 参考文献 | HPGDS inhibitor 2 实验方案 | HPGDS inhibitor 2 技术信息

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