Osthole (Synonyms: Osthol; NSC 31868)

Name: Osthole
Brand: MedChemExpress
SKU: HY-N0054
Rating: 5.0 (23 reviews)

Cat. No.: HY-N0054 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 484-12-8

Size	Price	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 44	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 44	In-stock	Estimated Time of Arrival: December 31
Solid
250 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 71	In-stock	Estimated Time of Arrival: December 31
1 g	USD 121	In-stock	Estimated Time of Arrival: December 31
5 g	USD 330	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Osthole:

Osthole-d₃ Get quote
Osthole (Standard) Get quote

11 Publications Citing Use of MCE Osthole

RT-PCR

IHC

: 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]

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	23.2 μM Compound: 1	Cytotoxicity against human A431 cells after 24 hrs by MTT assay Cytotoxicity against human A431 cells after 24 hrs by MTT assay	[PMID: 25062005]
A549	IC₅₀	46.2 μM Compound: 1	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 25062005]
COLO 205	IC₅₀	> 60 μM Compound: 1	Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay	[PMID: 25062005]
HCT-116	IC₅₀	30.2 μM Compound: 1	Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay	[PMID: 25062005]
HeLa	IC₅₀	1.6 μM Compound: 1	Inhibition of CRM1-mediated hemagglutininin-tagged HIV1 Rev protein nuclear export in human HeLa cells assessed as nucleus localization after 12 hrs by indirect fluorescent antibody technique Inhibition of CRM1-mediated hemagglutininin-tagged HIV1 Rev protein nuclear export in human HeLa cells assessed as nucleus localization after 12 hrs by indirect fluorescent antibody technique	[PMID: 20493693]
HepG2	IC₅₀	161.4 μM Compound: Osthole I	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 25461322]
MCF7	IC₅₀	25.8 μM Compound: 5, Osthole	Anticancer activity against human MCF7 assessed as inhibition of cell growth by MTT assay Anticancer activity against human MCF7 assessed as inhibition of cell growth by MTT assay	[PMID: 21051232]
MDA-MB-231	IC₅₀	30.2 μM Compound: 5, Osthole	Anticancer activity against human MDA-MB-231 assessed as inhibition of cell growth by MTT assay Anticancer activity against human MDA-MB-231 assessed as inhibition of cell growth by MTT assay	[PMID: 21051232]
PC-3	IC₅₀	24.8 μM Compound: 1	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay Cytotoxicity against human PC3 cells after 24 hrs by MTT assay	[PMID: 25062005]
RAW264.7	IC₅₀	12.4 μM Compound: 15	Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced NO production after 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced NO production after 24 hrs	[PMID: 25621853]
SH-SY5Y	EC₅₀	26.45 μM Compound: Osthole	Neuroprotection against oxygen-glucose deprivation-induced toxicity in human SH-SY5Y cells assessed as cytoprotection by MTT assay Neuroprotection against oxygen-glucose deprivation-induced toxicity in human SH-SY5Y cells assessed as cytoprotection by MTT assay	[PMID: 33132198]
SH-SY5Y	EC₅₀	33.26 μM Compound: Osthole	Neuroprotection against H202-induced toxicity in human SH-SY5Y cells assessed as cytoprotection by MTT assay Neuroprotection against H202-induced toxicity in human SH-SY5Y cells assessed as cytoprotection by MTT assay	[PMID: 33132198]
T47D	IC₅₀	42.4 μM Compound: 1	Cytotoxicity against human T47D cells after 24 hrs by MTT assay Cytotoxicity against human T47D cells after 24 hrs by MTT assay	[PMID: 25062005]

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.

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.

484-12-8

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
10 mM	0.4093 mL	2.0467 mL	4.0935 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (250 KB) LCMS (111 KB)

Handling Instructions (2659 KB)

References

[1]. Kordulewska NK, et al. Changes in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H1 receptor, COX-2, NF-κB, CCR1, chemokine CCL5/RANTES and interleukin-1β in PBMC allergic and non-allergic patients. Immunobiology. [Content Brief]

[2]. Tang DZ, et al. Osthole stimulates osteoblast differentiation and bone formation by activation of beta-catenin-BMP signaling. J Bone Miner Res. 2010 Jun;25(6):1234-45. [Content Brief]

[3]. Sun W, et al. Osthole pretreatment alleviates TNBS-induced colitis in mice via both cAMP/PKA-dependent and independent pathways. Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128. [Content Brief]

[4]. Zhang ZR, et al. Osthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine. Evid Based Complement Alternat Med. 2015;2015:919616. [Content Brief]

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	[1]. Kordulewska NK, et al. Changes in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H1 receptor, COX-2, NF-κB, CCR1, chemokine CCL5/RANTES and interleukin-1β in PBMC allergic and non-allergic patients. Immunobiology. [Content Brief] [2]. Tang DZ, et al. Osthole stimulates osteoblast differentiation and bone formation by activation of beta-catenin-BMP signaling. J Bone Miner Res. 2010 Jun;25(6):1234-45. [Content Brief] [3]. Sun W, et al. Osthole pretreatment alleviates TNBS-induced colitis in mice via both cAMP/PKA-dependent and independent pathways. Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128. [Content Brief] [4]. Zhang ZR, et al. Osthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine. Evid Based Complement Alternat Med. 2015;2015:919616. [Content Brief]

Complete Stock Solution Preparation Table

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

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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Osthole (Synonyms: Osthol; NSC 31868)

Customer Review

Other Forms of Osthole:

Osthole Related Antibodies

11 Publications Citing Use of MCE Osthole

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View All Histamine Receptor Isoform Specific Products:

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Biological Activity

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References

Customer Review

Osthole Related Antibodies

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Complete Stock Solution Preparation Table

Osthole Related Classifications

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