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  2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Digeranyl bisphosphonate

Digeranyl bisphosphonate  (Synonyms: DGBP)

目錄號: HY-U00145 純度: 98.50%
COA 產(chǎn)品使用指南 技術支持

Digeranyl bisphosphonate (DGBP) 是一種有效的香葉基焦磷酸香葉酯 (GGPP) 合酶抑制劑，抑制 Rac1 的香葉基焦磷酸化。

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Digeranyl bisphosphonate Chemical Structure

Digeranyl bisphosphonate Chemical Structure

CAS No. : 878143-03-4

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1 mg ￥2475
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查看 Ras 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

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

IC50 & Target

Rac1[1]
體外研究
(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.
體內(nèi)研究
(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.
分子量

536.40

Formula

C21H34Na4O6P2
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 2 mg/mL (3.73 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

H2O 中的溶解度 : 2 mg/mL (3.73 mM; 超聲助溶)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.8643 mL 9.3214 mL 18.6428 mL
5 mM --- --- ---
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.50%

參考文獻
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.
參考文獻

Digeranyl bisphosphonate 相關分類

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.8643 mL 9.3214 mL 18.6428 mL 46.6070 mL

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Digeranyl bisphosphonate
目錄號：
HY-U00145
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