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500mg |
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1g |
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2g |
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5g |
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10g |
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Purity: ≥98%
Osthol (Osthol; Ostol; NSC 31868) is an O-methylated coumarin analog and a natural product which is found in the plants such as Cnidium monnieri, Angelica archangelica and Angelica pubescens. Osthol prevents washed rabbit platelets from aggregating and releasing ATP when triggered by ADP, arachidonic acid, PAF, collagen, ionophore A23187, and thrombin.
Targets |
Histamine H1 receptor
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ln Vitro |
Osthol is an O-methylated coumarin present in plants, including Angelica pubescens, Cnidium monnieri, and Angelica archangelica. In rabbit platelets that have been cleaned, osthol prevents platelet aggregation and ATP release that is brought on by ADP, arachidonic acid, PAF, collagen, ionophore A23187, and thrombin. Through the extracellular signal-regulated kinase 1/2 and bone morphogenetic protein-2/p38 pathways, osteospot mediates cell differentiation in human osteoblast cells and holds promise as a treatment for osteoporosis. By making HBsAg more glycosylated, osteoporosis also inhibits the hepatitis B virus's secretion in cell culture. [3]
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ln Vivo |
Local bone formation was significantly stimulated by subcutaneous injection of osthole at a dose of 5 mg/kg per day into mouse skulls (histological analysis of skull tissue samples collected 2 weeks after the last injection and stained with H&E Orange G). Osthole significantly influenced bone formation, according to morphological analysis, and microtubule inhibition of TN-16 was just as successful as it was in the earlier investigation. However, when osthole was taken daily at a dose of 1 mg/kg, no such effect was observed. The bone loss of the castration stent can be considerably reversible with an 8-week intraperitoneal injection of osthole. Histological analysis of L4 samples stained with trinitrophenol poinsettia revealed that castrate stents treated with osthole had partially recovered their trabecular structure. Osthole treatment dramatically increased trabecular volume, thickness, and total BMD while decreasing trabecular separation, according to morphological analysis [2].
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Cell Assay |
On the first study day, participants' peripheral blood samples are drawn between 7 and 9 a.m. and transferred into grouping tubes containing K3EDTA. And then they make fresh PBMCs. A solution of 1% heat-inactivated human AB serum, 1% gentamicin, and 0.25% PHA is added to isolated cells that are seeded on 24-well plates at a density of 1×106 per well using RPMI-1640. A 24-hour period is given to each well before active reagents are added, with pure medium serving as the substance's control. After three additional days, cells are harvested[1].
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Animal Protocol |
Mice: Four-week-old ICR Swiss mice receive subcutaneous injections over the calvarial surface twice a day for five days straight, either with or without Osthole treatment. The doses are 1 and 5 mg/kg per day, with three mice per group. As a positive control, microtubule inhibitor TN-16 (5 mg/kg per day, subcutaneous injection, twice daily for 2 days; 3 mice per group) is used. Three weeks after the start of treatment, all the mice are put to sleep, and the calvariae are removed, preserved for two days in 10% phosphate-buffered formalin, decalcified for two weeks in 10% EDTA, and then embedded in paraffin. Hematoxylin and eosine orange G are used to cut and stain histologic sections. Using the OsteoMeasure System for histomorphometry, the amount of new bone over the calvarial surface is measured. In order to quantify the mineral appositional rate (MAR) and bone-formation rate (BFR), mice undergo intraperitoneal injections of 20 mg/kg of double calcein at days 7 and 14, following which they are put to death 7 days later. Plastic sections of the labeling are inspected. The calvarial samples that have been dissected are embedded in methyl methacrylate after being fixed in 75% ethanol. A fluorescent microscope is used to examine unstained transverse sections that have a thickness of 3 µm. With the OsteoMeasure System, MAR and BFR are measured.
Rats: The rats are thirty six-month-old female Sprague-Dawley rats. The rats are randomly assigned by body weight into three groups for the surgery (n=10): group 1 is a sham surgery followed by PBS vehicle treatment (sham+VEH); group 2 is an ovariectomy followed by vehicle treatment (OVX+VEH); and group 3 is an ovariectomy followed by Osthole treatment (OVX+OST). The rats are given an intraperitoneal nembutal injection (30 mg/kg) to induce anesthesia. The eight-week course of treatment is administered beginning one month following surgery. For eight weeks, either vehicle or Osthole (100 mg/kg daily) is taken orally once daily. Dual-energy X-ray absorptiometry is used to measure the total bone mineral density (BMD, g/m2) of the rats prior to their euthanasia at the end of the experiments. Then, the left femoral shafts are utilized for biomechanical testing, and the fourth lumbar vertebrae (L4) are dissected for histomorphometric and micro-computed tomographic (µCT) analysis. |
References |
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Molecular Formula |
C15H16O3
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Molecular Weight |
244.29
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Exact Mass |
244.11
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Elemental Analysis |
C, 73.75; H, 6.60; O, 19.65
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CAS # |
484-12-8
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Related CAS # |
Osthole-d3
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Appearance |
Solid powder
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SMILES |
CC(=CCC1=C(C=CC2=C1OC(=O)C=C2)OC)C
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InChi Key |
MBRLOUHOWLUMFF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H16O3/c1-10(2)4-7-12-13(17-3)8-5-11-6-9-14(16)18-15(11)12/h4-6,8-9H,7H2,1-3H3
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Chemical Name |
7-methoxy-8-(3-methylbut-2-enyl)chromen-2-one
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*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.
Possible interrelation between effect of osthole on intracellular ion channels, cyclic adenosine monophosphate (cAMP), and cyclic guanosine monophosphate (cGMP) levels with some of its pharmacological activities. Evid Based Complement Alternat Med . 2015:2015:919616. td> |
Chemical structure of osthole, the principle component of Cnidium monnieri. Evid Based Complement Alternat Med . 2015:2015:919616. td> |
Effects of osthole on the histological manifestations of TNBS-induced colitis. Acta Pharmacol Sin . 2017 Aug;38(8):1120-1128. td> |
The protective effects of osthole against TNBS-induced colitis were mainly mediated by the cAMP/PKA-independent pathway. Acta Pharmacol Sin . 2017 Aug;38(8):1120-1128. td> |
Osthole stimulates local bone formation in mouse calvaria. J Bone Miner Res . 2010 Jun;25(6):1234-45. td> |
Osthole reverses bone loss induced by ovariectomy in rats. J Bone Miner Res . 2010 Jun;25(6):1234-45. td> |