1. GPCR/G Protein
  2. Histamine Receptor

Osthole (Synonyms: NSC 31868; Osthol; Ostol)

Cat. No.: HY-N0054 Purity: 99.81%
Data Sheet SDS Handling Instructions

Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
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1 g USD 132 In-stock
5 g USD 360 In-stock
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    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2017 Oct 12.

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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.

    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].

    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].

    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.4093 mL 2.0467 mL 4.0935 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay

    Osthole is dissolved in 96% ethyl alcohol and then sterilized through a 0.22 μg/mL filter and stored at 4°C as stock solutions for later dilution[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

    Osthole is prepared in PBS[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.
    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.

    Molecular Weight




    CAS No.


    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    Osthole is dissolved in a 1:9 (v/v) mixture of Tween 80 and 0.9% sodium chloride solution[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


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