[CAS NO. 878143-03-4] Digeranyl bisphosphonate
PRODUCTS SPECIFICATIONS [878143-03-4]
DESCRIPTION [878143-03-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 536.40 |
| Molecular Formula | C21H34Na4O6P2 |
| SMILES | C/C(C)=C\CC/C(C)=C/CC(P(O[Na])(O[Na])=O)(P(O[Na])(O[Na])=O)C/C=C(C)/CC/C=C(C)\C |
Summary
Digeranyl bisphosphonate (DGBP) is a potent geranylgeranylpyrophosphate (GGPP) synthase inhibitor, which inhibits geranylgeranylation of Rac1.
IC50 & Target
Rac1 [1]
In Vitro
Digeranyl bisphosphonate (DGBP) impairs geranylgeranylation. To examine if Digeranyl bisphosphonate modulates Rac1 activity, cells are exposed to vehicle or Digeranyl bisphosphonate. Rac1 activation increases significantly after chrysotile exposure, whereas the activity in Digeranyl bisphosphonate -treated cells is reduced to control levels. Digeranyl bisphosphonate also decreases H 2 O 2 generation in chrysotile-exposed macrophages [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
To further evaluate the effect of Digeranyl bisphosphonate (DGBP; 0.2 mg/kg/day) in protecting mice from chrysotile-induced pulmonary fibrosis, the mice are administered vehicle or Digeranyl bisphosphonate subcutaneously in osmotic pumps, and exposed to saline or chrysotile the following day. Mice exposed to saline have normal lung architecture with vehicle and Digeranyl bisphosphonate treatment. Chrysotile-exposed mice that receive vehicle have significant architectural changes in their lung parenchyma and large amounts of collagen deposition, whereas the lungs of the Digeranyl bisphosphonate -treated mice are essentially normal. To investigate the effect of Digeranyl bisphosphonate in Bleomycin-induced fibrosis, osmotic pumps containing either vehicle or Digeranyl bisphosphonate are implanted subcutaneously in WT mice. Mice are exposed to saline or Bleomycin the following day. Digeranyl bisphophonate (0.2 mg/kg/day)-treated mice show significantly less hydroxyproline compared to vehicle-treated mice exposed to Bleomycin [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
H 2 O : 2 mg/mL ( 3.73 mM ; Need ultrasonic)
DMSO : 2 mg/mL ( 3.73 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8643 mL | 9.3214 mL | 18.6428 mL |
| 5 mM | --- | --- | --- |
| 10 mM | --- | --- | --- |
