貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S81380-1mg	≥98%	￥255.00 S81380-1mg ￥255.00 現(xiàn)貨	500 >10	-	-	-
S81380-2mg	≥98%	￥340.00 S81380-2mg ￥340.00 現(xiàn)貨	250 >10	-	-	-
S81380-5mg	≥98%	￥552.50 S81380-5mg ￥552.50 現(xiàn)貨	100 >10	-	-	-
S81380-10mg	≥98%	￥850.00 S81380-10mg ￥850.00 現(xiàn)貨	50 >10	-	-	-
S81380-25mg	≥98%	￥1930.00 S81380-25mg ￥1930.00 現(xiàn)貨	20 >10	-	-	-
S81380-50mg	≥98%	￥2900.00 S81380-50mg ￥2900.00 現(xiàn)貨	10 10	-	-	-
S81380-100mg	≥98%	￥4200.00 S81380-100mg ￥4200.00 現(xiàn)貨	5 5	-	-	-

產(chǎn)品介紹

PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0??nM and (S)-PFI-2 shows inhibiting activity with IC50 ?value of?1.0??μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis

產(chǎn)品描述：

靶點(diǎn)：

Histone Methyltransferase;HistoneMethyltransferase

體外研究：

(R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0??nM and (S)-PFI-2 shows inhibiting activity with IC50 ?value of?1.0??μM

體內(nèi)研究：

PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuates the progression of renal fibrosis and preserves renal function in FA nephropathy. PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced ECM accumulation and fibroblasts activation after FA injury[2]. PFI-2 hydrochloride (i.p., 200 μM, twice a week) impeded Th2 cytokine signaling activation and M2 macrophage polarization. PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys. PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuated macrophages M2 polarization and M2 macrophages-to-myofibroblasts transition in obstructed kidneys. PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed myeloid myofibroblast accumulation and renal fibrosis after UUO injury. PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced the infiltration of inflammatory cells, the production of inflammatory molecules, and NF-κB activation in FA nephropathy. Animal Model: Male C57BL/6 mice (8-10-week old, 20-25 g) Dosage: 200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL) Administration: intraperitoneal injection, twice a week Result: Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01).Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys

參考文獻(xiàn)：

1. Yuzhen Niu, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547. 2. Benquan Liu, et al. Pharmacological inhibition of SETD7 by PFI-2 attenuates renal fibrosis following folic acid and obstruction injury. Eur J Pharmacol. 2021 Jun 15;901:174097.

溶解性：

Soluble in DMSO、H2O

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.866 ml	9.329 ml	18.657 ml
5 mM	0.373 ml	1.866 ml	3.731 ml
10 mM	0.187 ml	0.933 ml	1.866 ml
50 mM	0.037 ml	0.187 ml	0.373 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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PFI-2 (hydrochloride)