1. GPCR/G Protein
  2. Ras
  3. Digeranyl bisphosphonate

Digeranyl bisphosphonate (Synonyms: DGBP)

Cat. No.: HY-U00145 Purity: >98.0%
Handling Instructions

Digeranyl bisphosphonate (DGBP) is a potent geranylgeranylpyrophosphate (GGPP) synthase inhibitor, which inhibits geranylgeranylation of Rac1.

For research use only. We do not sell to patients.

Digeranyl bisphosphonate Chemical Structure

Digeranyl bisphosphonate Chemical Structure

CAS No. : 878143-03-4

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1 mg USD 360 In-stock
Estimated Time of Arrival: December 31
5 mg USD 720 In-stock
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10 mg USD 1224 In-stock
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50 mg USD 3500 In-stock
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Description

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 H2O2 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.

Molecular Weight

536.40

Formula

C₂₁H₃₄Na₄O₆P₂

CAS No.

878143-03-4

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

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
In Vitro: 

H2O : 2 mg/mL (3.73 mM; Need ultrasonic)

DMSO : 2 mg/mL (3.73 mM; Need ultrasonic)

Preparing
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 --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Wild-type C57Bl/6 mice are used. After equilibration, osmotic pumps containing either vehicle (water) or Digeranyl bisphosphonate (0.2 mg/kg/day) are implanted subcutaneously. Rac1 null and Rac2 knockout mice are used. Briefly, Rac1 null mice are conditional and are generated using LysMcre to selectively delete Rac1 from cells of the granulocyte/monocyte lineage. The Rac2 knockout mice are generated using conventional gene targeting to delete the Rac2 gene as Rac2 is only expressed in cells of the granulocyte/monocyte lineage. Bleomycin (1.3-2.0 U/kg) or Chrysotile (100 μg) is administered intratracheally. Mice are euthanized and fibrosis determined.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: >98.0%

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Keywords:

Digeranyl bisphosphonateDGBPRasInhibitorinhibitorinhibit

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Digeranyl bisphosphonate
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