2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis Anti-infection
  3. Histamine Receptor Apoptosis Parasite HBV
  4. Osthole

Osthole  (Synonyms: Osthol; NSC 31868)

Cat. No.: HY-N0054 Purity: 99.95%
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Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity. Osthole also suppresses the secretion of HBV in cells.

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

Osthole Chemical Structure

Osthole Chemical Structure

CAS No. : 484-12-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 44 In-stock
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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Osthole:

Osthole Related Antibodies

Top Publications Citing Use of Products

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Mice are intraperitoneally injected with Osthole (100 mg/kg). After 24h, TMX (90mg/kg) is administered to mice. Mice are sacrificed 8 h after the TMX injections. Western blot analyses of the liver homogenates are performed.

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole reduces TMX-induced oxidative stress.

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole reduces the TMX-induced inflammatory response. Mice are intraperitoneally injected with Osthole (100 mg/kg).

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole significantly suppresses the expression of pro-oxidant genes (NOX2 and ACOX). Mice are intraperitoneally injected with osthole (100 mg/kg).

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole reduces the TMX-induced inflammatory response. Mice are intraperitoneally injected with Osthole (100 mg/kg)

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole significantly increases the expression of antioxidant genes (GPX1, SOD2). Mice are intraperitoneally injected with osthole (100 mg/kg).

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole significantly increases the expression of antioxidant genes (GCL-c, and G6pdh. Mice are intraperitoneally injected with osthole (100 mg/kg).

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2018 Jan;39(1):74-84.  [Abstract]

    Osthole inhibits the metabolic activation of APAP and promotes APAP clearance. Hepatic SULT2A1 and UGT1A1 levels are determined by Western blotting.

    Osthole purchased from MedChemExpress. Usage Cited in: Front Physiol. 2018 Nov 21;9:1650.  [Abstract]

    OST suppress activation of NRK-49F cells. NRK-49F are preincubated with OST for 30 min before TGFβ1 (5 ng/ml) and are harvested 24 h after TGFb1 stimulation. Western blot analyses of a-SMA, Col I (collagen I) and FN (fibronectin) are showed.

    Osthole purchased from MedChemExpress. Usage Cited in: Front Physiol. 2018 Nov 21;9:1650.  [Abstract]

    Western blot analyses (E) of PCNA, cyclin D1 and p21 cip1 in the treatment of FBS and OST.

    Osthole purchased from MedChemExpress. Usage Cited in: Front Physiol. 2018 Nov 21;9:1650.  [Abstract]

    Representative micrographs of immunofluorescent staining of FN (red) and a-SMA (green) with the treatment of TGFβ1 and OST.

    Osthole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128.  [Abstract]

    Osthole attenuates the phosphorylation of p38 in TNBS-induced colitis. Mice receive Osthole intraperitoneally at 100 mg/kg once daily starting at three days before being exposed to TNBS treatments and until the end of the experiments. Colitis is induced by infusing a 100 μL enema of TNBS (2.8 mg) in 50% ethanol into the colonic lumen. Western blot analysis of the colonic mucosa homogenates is performed 2 d after the initial rectal TNBS administration.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity. Osthole also suppresses the secretion of HBV in cells.

    IC50 & Target

    Histamine H1 receptor[1]
    In Vitro

    Osthole (p<0.0001) and Fexofenadine (p<0.001) inhibit increased HRH-1 mRNA expression induced by histamine in the study group. This result is also observed in cells cultured with histamine/Osthole; where combined substances decreased HRH-1 mRNA expression compared to histamine (p<0.0001)[1]. Assessment of cell viability does not detect obvious toxicity when Osthole is used at a dose up to 100 μM. However, when the dose reached 500 μM, Osthole started to show toxic effect. Based on these observations, Osthole is used in all in vitro studies at the dose range of 10 to 100 μM. Osthole dose-dependently promotes osteoblast differentiation, as shown by the upregulation of osteoblast differentiation marker genes such as type I collagen (col1), bone sialoprotein (BSP) and osteocalcin (OC) (2 days of culture). Osthole promotes ALP activity in mouse primary osteoblasts in a dose-dependent manner[2].

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

    Osthole Related Antibodies
    In Vivo

    Subcutaneous injection of Osthole at a dose of 5 mg/kg per day onto mouse calvariae significantly stimulates local bone formation, as shown by histologic analysis of calvarial samples harvested 2 weeks after the last injection and stained with H&E orange G. Histomorphometric analysis reveals that Osthole has a significant effect on bone formation as potent as the positive control, the microtubule inhibitor TN-16. This effect, however, is not seen when Osthole is used at a dose of 1 mg/kg per day. Intraperitoneal injection of Osthole for 8 weeks significantly reverses bone loss in the ovariectomized rats. Histologic examination of the L4samples stained with trinitrophenol poinsettia demonstrates a partial recovery of the trabecular structure in ovariectomized rats treated with Osthole. Histomorphometric analysis shows that treatment with Osthole significantly increases total BMD, trabecular bone volume, and trabecular thickness and decreases trabecular separation[2].

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

    244.29

    Formula

    C15H16O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C=CC2=CC=C(OC)C(C/C=C(C)\C)=C2O1
    Structure Classification
    Initial Source
    Shipping

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

    DMSO : ≥ 100 mg/mL (409.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.0935 mL 20.4675 mL 40.9350 mL
    5 mM 0.8187 mL 4.0935 mL 8.1870 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

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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:

    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 (10.23 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 (10.23 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 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:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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: 99.95%

    COA (250 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Peripheral blood samples are collected from participants between 7.00 and 9.00 a.m. on the first study day and these are concentrated in grouping tubes with K3EDTA. Fresh PBMCs are then prepared. Isolated cells are seeded on 24-well plates at 1×106 per well with RPMI-1640 and supplemented with 1% heat inactivated human AB serum, 1% gentamicin and 0.25% PHA. Active reagents are added to each well after 24 h and pure medium formed the control for each substance. Cells are then harvested after a further three days[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Four-week-old ICR Swiss mice are injected subcutaneously over the calvarial surface with or without the treatment of Osthole twice a day for 5 consecutive days at the doses of 1 and 5 mg/kg per day (3 mice per group). Microtubule inhibitor TN-16 is used as a positive control (5 mg/kg per day, by subcutaneous injection, twice a day for 2 days; 3 mice per group). All mice are euthanized 3 weeks after treatment, and calvariae are dissected, fixed in 10% phosphate-buffered formalin for 2 days, decalcified in 10% EDTA for 2 weeks, and embedded in paraffin. Histologic sections are cut and stained with hematoxylin and eosine orange G. New bone area over the calvarial surface is quantified by histomorphometry using the OsteoMeasure System. To measure mineral appositional rate (MAR) and bone-formation rate (BFR), double calcein labeling is performed at days 7 and 14 by intraperitoneal injection (20 mg/kg), and mice are euthanized 7 days after the second labeling. The labeling is examined in plastic sections. The dissected calvarial samples are fixed in 75% ethanol and embedded in methyl methacrylate. Unstained transverse sections (3 µm thick) are examined with a fluorescent microscope. MAR and BFR are measured using the OsteoMeasure System.
    Rats[2]
    Thirty 6-month-old female Sprague-Dawley rats are used. After anesthesia with intraperitoneal nembutal injection (30 mg/kg), the rats are randomized by body weight into three groups for the surgery (n=10/group): group 1: sham surgery followed by PBS vehicle treatment (sham+VEH); group 2: ovariectomy followed by vehicle treatment (OVX+VEH); and group 3: ovariectomy followed by Osthole treatment (OVX+OST). The treatment is started 1 month after surgery and continued for 8 weeks. Vehicle or Osthole (100 mg/kg per day) is administered orally once a day for 8 weeks. Before rats are euthanized at the end of the experiments, the total bone mineral density (BMD, g/m2) is measured using dual-energy X-ray absorptiometry. The fourth lumbar vertebrae (L4) then are dissected for histomorphometric and micro-computed tomographic (µCT) analysis, and the left femoral shafts are used for biomechanical testing.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.0935 mL 20.4675 mL 40.9350 mL 102.3374 mL
    5 mM 0.8187 mL 4.0935 mL 8.1870 mL 20.4675 mL
    10 mM 0.4093 mL 2.0467 mL 4.0935 mL 10.2337 mL
    15 mM 0.2729 mL 1.3645 mL 2.7290 mL 6.8225 mL
    20 mM 0.2047 mL 1.0234 mL 2.0467 mL 5.1169 mL
    25 mM 0.1637 mL 0.8187 mL 1.6374 mL 4.0935 mL
    30 mM 0.1364 mL 0.6822 mL 1.3645 mL 3.4112 mL
    40 mM 0.1023 mL 0.5117 mL 1.0234 mL 2.5584 mL
    50 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0467 mL
    60 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7056 mL
    80 mM 0.0512 mL 0.2558 mL 0.5117 mL 1.2792 mL
    100 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0234 mL
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    Osthole 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:

    Osthole484-12-8Osthol NSC 31868NSC31868NSC 31868NSC-31868Histamine ReceptorApoptosisParasiteHBVHepatitis B virusInhibitorinhibitorinhibit

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