2. NF-κB
  3. NF-κB
  4. Geranylgeraniol

Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model.

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Geranylgeraniol Chemical Structure

Geranylgeraniol Chemical Structure

CAS No. : 24034-73-9

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Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Geranylgeraniol Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model[1][2][3][4].

IC50 & Target

NF-kB[1]
In Vitro

Geranylgeraniol (0-10 μM; 24 h) dose-dependently suppresses the LPS-induced increase in the mRNA levels of Il-1β, Tnf-α, Il-6, and Cox-2[1].
Geranylgeraniol (10 μM; 24 h) inhibits the phosphorylation of TAK1, IKKα/β, and NF-κB p65 proteins as well as NF-κB nuclear translocation induced by LPS while maintaining IκBα expression[1].
Geranylgeraniol, (50 μM; 24 h) eliminates cell damage caused by Simvastatin (HY-17502) (10 µM) and Mevalonat (10 mM), and reduces the inflammatory marker and the damage of the mitochondria, maintaining its shape and component[2].

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

Geranylgeraniol Related Antibodies

Western Blot Analysis[1]

Cell Line: MG6 cell
Concentration: 0, 1, 10 μM
Incubation Time: 24 hours
Result: Suppressed by TAK1, IKKα/β, and NF-κB p65 proteins level at 10 μM.

RT-PCR[1]

Cell Line: MG6 cell
Concentration: 10 μM
Incubation Time: 0, 6, 12, 24 hours
Result: Significantly inhibited pro-inflammatory cytokine Il-1β, Tnf-α, Il-6, and Cox-2 mRNA level.
In Vivo

Geranylgeraniol (725 mg/kg/d; p.o.; 90 d) is not toxicologically significant with a dose below 725 mg/kg/d in rats[3].
Geranylgeraniol (483 mg/kg/d; p.o.; 10 d) suppresses lipopolysaccharide-induced inflammation via inhibition of nuclear factor-κB activation in rats[4].

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

Animal Model: Han Wistar rats (169-192 g for male; 116-152 g for female)[3]
Dosage: 0, 725, 1450, and 2900 mg/kg
Administration: Oral gavage; once daily; 90 days
Result: Showed the lowest observed adverse effect level (LOAEL) for local effects and the no observed adverse effect level (NOAEL) for systemic effects as 725 mg/kg/d.
Reduced body weights by 12.9 and 21.6% in the intermediate- and high-dose group males, respectively, compared to controls.
Animal Model: Wistar rats (male, 8-week-old, 130-150 g)[4]
Dosage: 0, 48.3, 483, 4830 mg/kg
Administration: Oral gavage; once daily; 10 days; with or not LPS challenge (i.p.; 0.5 mg/kg)
Result: Suppressed LPS-induced inflammatory cytokines and mRNA expression of LPS-induced inflammatory genes in liver with doses of 483 mg/kg and 4830 mg/kg.
Suppressed protein levels of IRAK1, TRAF6, and TAK1, originating from transcriptional down-regulation with doses of 483 mg/kg and 4830 mg/kg.
Molecular Weight

290.48

Formula

C20H34O
CAS No.
Appearance

Liquid (Density: 0.8930 g/cm3)

Color

Colorless to light yellow

SMILES

C/C(C)=C\CC/C(C)=C/CC/C(C)=C/CC/C(C)=C/CO
Structure Classification
Initial Source

Halobacterium cutirubrum
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (344.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4426 mL 17.2129 mL 34.4258 mL
5 mM 0.6885 mL 3.4426 mL 6.8852 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.61 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.18%

SDS (393 KB)

COA (239 KB) HNMR (125 KB) GC (221 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4426 mL 17.2129 mL 34.4258 mL 86.0644 mL
5 mM 0.6885 mL 3.4426 mL 6.8852 mL 17.2129 mL
10 mM 0.3443 mL 1.7213 mL 3.4426 mL 8.6064 mL
15 mM 0.2295 mL 1.1475 mL 2.2951 mL 5.7376 mL
20 mM 0.1721 mL 0.8606 mL 1.7213 mL 4.3032 mL
25 mM 0.1377 mL 0.6885 mL 1.3770 mL 3.4426 mL
30 mM 0.1148 mL 0.5738 mL 1.1475 mL 2.8688 mL
40 mM 0.0861 mL 0.4303 mL 0.8606 mL 2.1516 mL
50 mM 0.0689 mL 0.3443 mL 0.6885 mL 1.7213 mL
60 mM 0.0574 mL 0.2869 mL 0.5738 mL 1.4344 mL
80 mM 0.0430 mL 0.2152 mL 0.4303 mL 1.0758 mL
100 mM 0.0344 mL 0.1721 mL 0.3443 mL 0.8606 mL
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Geranylgeraniol Related Classifications

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.

Keywords:

Geranylgeraniol24034-73-9NF-κBNuclear factor-κBNuclear factor-kappaBcholesterol pathwayapoptosisneuroinflammationmevalonatemitochondrianeuronal deathLPS-inducedmicroglial inflammationInhibitorinhibitorinhibit

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