PF-4191834 是 5-Lipoxygenase (5-LOX) 的非铁螯合和非氧化还原抑制剂,IC50 为 229 nM。 PF-4191834 对 5-LOX 的特异性比 12-LOX 和 15-LOX 高约 300 倍,并且对环氧合酶没有活性。 PF-4191834 可用于炎症和疼痛的研究。
产品描述
PF-4191834 is a noniron chelating and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) with an IC50 of 229 nM. PF-4191834 shows ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and displays no activity toward the cyclooxygenase enzymes. PF-4191834
体外活性
PF-4191834 exerts a concentration-dependent inhibition of human 5-LOX (IC50: 130 nM and an IC80: 370 nM). PF-4191834 inhibits the synthesis of the 5-LOX products 5-HETE, 5-oxo-ETE, LTB4, and LTE4 with estimated IC50 values between 100 and 190 nM. However, it does not inhibit significantly the COX-1/2 enzymes or the 12- or 15-LOX enzymes at concentrations up to 30 μM[1].
Cas No.
1029317-21-2
分子式
C22H23N3O2S
分子量
393.5
别名
PF-04191834
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years