2. Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel Apoptosis
  3. COX GABA Receptor Apoptosis
  4. Humulone

Humulone  (Synonyms: α-Lupulic acid)

Cat. No.: HY-N6084 Purity: 99.33%
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Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.

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

Humulone Chemical Structure

Humulone Chemical Structure

CAS No. : 26472-41-3

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Based on 1 publication(s) in Google Scholar

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Description

Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties[1][2][3].

IC50 & Target[1][2][3]

COX-2

 

In Vitro

Humulone (0.1, 1, 10, 100, 1000, 10000 nM; for 12 h) with with 10 ng/ml TNFα dose-dependently decreases the amount of released PGE2 with an IC50 of about 30 nM in MC3T3-E1 cells. Humulone reduces cyclooxygenase activity of the TNFK-treated cells[1].
Humulone (0.1-10000 nM; for 12 h) suppresses the TNFα-induced increase of cyclooxygenase-2 mRNA[1].
Humulone hardly affects the cyclooxygenase-1 activity below 10 μM, whereas inhibits the cyclooxygenase-2 activity with an IC50 of about 1.6 μM in MC3T3-E1 cells[1].

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

Humulone Related Antibodies
In Vivo

Humulone (10 or 20 mg/kg; IP; single dose) shortens sleep onset and increases the duration of sleep induced by pentobarbital and decreases the spontaneous locomotion in open field at 20 mg/kg[2].
Humulone (10 μmol; applied topically to the dorsal shaved area) pre-treatment significantly inhibited TPA (10 nmol)-induced COX-2 expression in Female ICR mice (6-7 weeks of age) skin[3].
Humulone (1, 10 μmol; applied topical; pre-treatment 30 min) suppresses TPA-induced NF-κB DNA binding. Humulone attenuates TPA-stimulated nuclear translocation of p65 and p50 subunit proteins of NF-κB[3].

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

Animal Model: Male BALB/cAnNRj mice (9-11 weeks of age)[2]
Dosage: 10 or 20 mg/kg
Administration: IP; pre-treatment before sodium pentobarbital (35 mg/kg; i.p.) and ethanol (3.5 g/kg)
Result: Significantly decreased the latency and prolonged the duration of sleep induced by pentobarbital at 20 mg/kg dose. These effects were not observed at a lower dose of 10 mg/kg.
Showed no effect on the onset of sleep induced by ethanol, but significantly increased sleep duration dose-dependently.
Molecular Weight

362.46

Formula

C21H30O5
CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

C/C(C)=C/C[C@@]1(C(C(C(CC(C)C)=O)=C(O)C(C/C=C(C)\C)=C1O)=O)O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (137.95 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 2.7589 mL 13.7946 mL 27.5893 mL
5 mM 0.5518 mL 2.7589 mL 5.5179 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 (protect from light). 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 2.7589 mL 13.7946 mL 27.5893 mL 68.9731 mL
5 mM 0.5518 mL 2.7589 mL 5.5179 mL 13.7946 mL
10 mM 0.2759 mL 1.3795 mL 2.7589 mL 6.8973 mL
15 mM 0.1839 mL 0.9196 mL 1.8393 mL 4.5982 mL
20 mM 0.1379 mL 0.6897 mL 1.3795 mL 3.4487 mL
25 mM 0.1104 mL 0.5518 mL 1.1036 mL 2.7589 mL
30 mM 0.0920 mL 0.4598 mL 0.9196 mL 2.2991 mL
40 mM 0.0690 mL 0.3449 mL 0.6897 mL 1.7243 mL
50 mM 0.0552 mL 0.2759 mL 0.5518 mL 1.3795 mL
60 mM 0.0460 mL 0.2299 mL 0.4598 mL 1.1496 mL
80 mM 0.0345 mL 0.1724 mL 0.3449 mL 0.8622 mL
100 mM 0.0276 mL 0.1379 mL 0.2759 mL 0.6897 mL
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Humulone Related Classifications

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  • 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:

Humulone26472-41-3α-Lupulic acidCOXGABA ReceptorApoptosisCyclooxygenaseGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorprenylatedphloroglucinolboneresorptionantioxidantanti-angiogenicInhibitorinhibitorinhibit

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