Size | Price | Stock | Qty |
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5mg |
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Other Sizes |
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Targets |
COX-2
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ln Vitro |
In MC3T3-E1 cells, humulone (0.1, 1, 10, 100, 1000, and 10,000 nM; for 12 hours) reduces the quantity of produced PGE2 with a dose-dependent manner, with an IC50 of roughly 30 nM. The TNFK-treated cells' cyclooxygenase activity is decreased by humulone[1]. For a duration of 12 hours, humulone (0.1–10,000 nM) inhibits the rise in cyclooxygenase-2 mRNA that is caused by TNFα[1]. In MC3T3-E1 cells, humulone suppresses cyclooxygenase-2 activity with an IC50 of around 1.6 μM, but it barely impacts cyclooxygenase-1 activity below 10 μM[1].
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ln Vivo |
At 10 or 20 mg/kg (IP; single dose), humulone reduces spontaneous movement in an open field and lengthens the time that pentobarbital-induced sleep lasts[2]. TPA (10 nmol)-induced COX-2 expression in the skin of female ICR mice (6-7 weeks old) was considerably reduced by humulone (10 μmol) administered topically to the dorsal shaved area prior to treatment[3]. Humulone (1, 10 μmol; topical; 30 min before to treatment) inhibits the NF-κB DNA binding that is triggered by TPA. The nuclear translocation of NF-κB's p65 and p50 subunit proteins is attenuated by humulone in response to TPA stimulation[3].
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Animal Protocol |
Animal/Disease Models: Male BALB/cAnNRj mice (9-11 weeks of age)[2]
Doses: 10 or 20 mg/kg Route of Administration: IP; pre-treatment before sodium pentobarbital (35 mg/kg; ip) and ethanol (3.5 g/kg) Experimental Results: Dramatically diminished 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. demonstrated no effect on the onset of sleep induced by ethanol, but Dramatically increased sleep duration dose-dependently. |
References |
[1]. K Yamamoto, et al. Suppression of cyclooxygenase-2 gene transcription by humulon of beer hop extract studied with reference to glucocorticoid. FEBS Lett. 2000 Jan 14;465(2-3):103-6.
[2]. Ali Y Benkherouf, et al. Humulone Modulation of GABA A Receptors and Its Role in Hops Sleep-Promoting Activity. Front Neurosci. 2020 Oct 14;14:594708. [3]. Jung-Chul Lee, et al. Humulone inhibits phorbol ester-induced COX-2 expression in mouse skin by blocking activation of NF-kappaB and AP-1: IkappaB kinase and c-Jun-N-terminal kinase as respective potential upstream targets. Carcinogenesis. 2007 Jul;28(7): |
Molecular Formula |
C21H30O5
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Molecular Weight |
362.46
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CAS # |
26472-41-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(=CCC1=C([C@](CC=C(C)C)(C(=O)C(=C1O)C(=O)CC(C)C)O)O)C
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 50 mg/mL (137.95 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 | |
10 mM | 0.2759 mL | 1.3795 mL | 2.7589 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.