Digeranyl-bisphosphonate-DGBP-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDigeranyl bisphosphonateCat. No.: HY-U00145CAS No.: 878143-03-4Synonyms: DGBP分式: CHNaOP分量: 536.4作靶点: Ras作通路: GPCR/G Protein储存式: -20C, protect from light, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (protect

2、 fromlight, stored under nitrogen)溶解性数据体外实验 DMSO : 2 mg/mL (3.73 mM; Need ultrasonic)H2O : 2 mg/mL (3.73 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8643 mL 9.3214 mL 18.6428 mL5 mM - - -10 mM - - -请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Digera

3、nyl bisphosphonate种有效的叶 焦磷酸叶酯 (GGPP) 合酶抑制剂，其抑制 Rac1 的叶酰叶酰化。IC50 & Target Rac1 1体外研究Digeranyl bisphosphonate (DGBP) impairs geranylgeranylation. To examine if Digeranyl bisphosphonate1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEmodulates Rac1 activity, cells are exposed to vehicle or Digeranyl bi

4、sphosphonate. Rac1 activationincreases significantly after chrysotile exposure, whereas the activity in Digeranyl bisphosphonate -treatedcells is reduced to control levels. Digeranyl bisphosphonate also decreases H2O2 generation in chrysotile-exposed macrophages 1.体内研究 To further evaluate the effect

5、 of Digeranyl bisphosphonate (0.2 mg/kg/day) in protecting mice from chrysotile-induced pulmonary fibrosis, the mice are administered vehicle or Digeranyl bisphosphonate subcutaneouslyin osmotic pumps, and exposed to saline or chrysotile the following day. Mice exposed to saline have normallung arch

6、itecture with vehicle and Digeranyl bisphosphonate treatment. Chrysotile-exposed mice that receivevehicle have significant architectural changes in their lung parenchyma and large amounts of collagendeposition, whereas the lungs of the Digeranyl bisphosphonate -treated mice are essentially normal. T

7、oinvestigate the effect of Digeranyl bisphosphonate in Bleomycin-induced fibrosis, osmotic pumps containingeither vehicle or Digeranyl bisphosphonate are implanted subcutaneously in WT mice. Mice are exposed tosaline or Bleomycin the following day. Digeranyl bisphophonate (0.2 mg/kg/day)-treated mic

8、e showsignificantly less hydroxyproline compared to vehicle-treated mice exposed to Bleomycin 1.PROTOCOLAnimal Mice 1Administration 1 Wild-type C57Bl/6 mice are used. After equilibration, osmotic pumps containing either vehicle (water) orDigeranyl bisphosphonate (0.2 mg/kg/day) are implanted subcuta

9、neously. Rac1 null and Rac2 knockout miceare used. Briefly, Rac1 null mice are conditional and are generated using LysMcre to selectively delete Rac1from cells of the granulocyte/monocyte lineage. The Rac2 knockout mice are generated using conventionalgene targeting to delete the Rac2 gene as Rac2 i

10、s only expressed in cells of the granulocyte/monocytelineage. Bleomycin (1.3-2.0 U/kg) or Chrysotile (100 g) is administered intratracheally. Mice are euthanizedand fibrosis determined.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Osborn-Heaford HL, et al. Targeting the isoprenoid pathway to abrogate progression of pulmonary fibrosis. Free Radic Biol Med. 2015Sep;86:47-56.McePdfHeightCaution: Product has not been ful