Acebilustat

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Chemical Structure| 943764-99-6 同义名 : CTX-4430
CAS号 : 943764-99-6
货号 : A639379
分子式 : C29H27N3O4
纯度 : 99%+
分子量 : 481.542
MDL号 : MFCD30496703
存储条件:

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 16 mg/mL(33.23 mM),配合低频超声助溶,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 Leukotriene B4 (LTB4) is a potent chemoattractant of neutrophil migration and activation. Leukotriene A4 hydrolase (LTA4H) is the rate‐limiting enzyme for LTB4 synthesis. Reducing the production of LTB4 via inhibiting LTA4H may be a potential therapeutic approach for anti-inflammatory treatment. Acebilustat is a potent inhibitor of LTA4H. The IC50 value of acebilustat for the inhibition of LTB4 production in human whole blood is 31ng/mL (~0.064μM)[3]. Acebilustat at a concentration of 0.1μM decreased the count of apical polymorphonuclear neutrophils at 2-, 10- and 18-hour post-transmigration without affecting primary granule exocytosis in these cells[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.38mL

2.08mL

1.04mL

20.77mL

4.15mL

2.08mL

参考文献

[1]Elborn JS, Horsley A, et al. Phase I Studies of Acebilustat: Biomarker Response and Safety in Patients with Cystic Fibrosis. Clin Transl Sci. 2017 Jan;10(1):28-34.

[2]Elborn JS, Bhatt L, et al. Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction. Clin Transl Sci. 2017 Jan;10(1):20-27.

[3]Elborn JS, Bhatt L, Grosswald R, Ahuja S, Springman EB. Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction. Clin Transl Sci. 2017 Jan;10(1):20-27.

[4]Forrest OA, Ingersoll SA, Preininger MK, Laval J, Limoli DH, Brown MR, Lee FE, Bedi B, Sadikot RT, Goldberg JB, Tangpricha V, Gaggar A, Tirouvanziam R. Frontline Science: Pathological conditioning of human neutrophils recruited to the airway milieu in cystic fibrosis. J Leukoc Biol. 2018 Oct;104(4):665-675.