Synonym
Osthole; Osthol; Ostole; Ostol;
IUPAC/Chemical Name
7-methoxy-8-(3-methylbut-2-en-1-yl)-2H-chromen-2-one
InChi Key
MBRLOUHOWLUMFF-UHFFFAOYSA-N
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
SMILES Code
O=C1C=CC2=C(O1)C(C/C=C(C)\C)=C(OC)C=C2
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.
In vitro activity:
The cultures were treated 72h with FXF and osthole. The present study suggests that osthole may be a potential inhibitor of histamine H1 receptor activity. This study also demonstrated that cells cultured with histamine increase COX-2 mRNA expression and osthole reduce it.
Reference: Immunobiology. 2017 Mar;222(3):571-581. https://pubmed.ncbi.nlm.nih.gov/27843000/
In vivo activity:
This study found that local injection of Osthole significantly increased new bone formation on the surface of mouse calvaria. Ovariectomy caused evident bone loss in rats, whereas Osthole largely prevented such loss, as shown by improved bone microarchitecture, histomorphometric parameters, and biomechanical properties.
Reference: J Bone Miner Res. 2010 Jun;25(6):1234-45. https://pubmed.ncbi.nlm.nih.gov/20200936/
|
Solvent |
mg/mL |
mM |
| Solubility |
| Ethanol |
34.5 |
141.23 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
244.29
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Kordulewska NK, Kostyra E, Cieślińska A, Matysiewicz M, Fiedorowicz E, Sienkiewicz-Szłapka E. 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. 2017 Mar;222(3):571-581. doi: 10.1016/j.imbio.2016.11.004. Epub 2016 Nov 10. PMID: 27843000.
2. Ko FN, Wu TS, Liou MJ, Huang TF, Teng CM. Inhibition of platelet thromboxane formation and phosphoinositides breakdown by osthole from Angelica pubescens. Thromb Haemost. 1989 Nov 24;62(3):996-9. PMID: 2556815.
3. Sun W, Cai Y, Zhang XX, Chen H, Lin YD, Li H. 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. doi: 10.1038/aps.2017.71. Epub 2017 Jun 12. PMID: 28603288; PMCID: PMC5547558.
4. Tang DZ, Hou W, Zhou Q, Zhang M, Holz J, Sheu TJ, Li TF, Cheng SD, Shi Q, Harris SE, Chen D, Wang YJ. Osthole stimulates osteoblast differentiation and bone formation by activation of beta-catenin-BMP signaling. J Bone Miner Res. 2010 Jun;25(6):1234-45. doi: 10.1002/jbmr.21. PMID: 20200936; PMCID: PMC3153131.
In vitro protocol:
1. Kordulewska NK, Kostyra E, Cieślińska A, Matysiewicz M, Fiedorowicz E, Sienkiewicz-Szłapka E. 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. 2017 Mar;222(3):571-581. doi: 10.1016/j.imbio.2016.11.004. Epub 2016 Nov 10. PMID: 27843000.
2. Ko FN, Wu TS, Liou MJ, Huang TF, Teng CM. Inhibition of platelet thromboxane formation and phosphoinositides breakdown by osthole from Angelica pubescens. Thromb Haemost. 1989 Nov 24;62(3):996-9. PMID: 2556815.
In vivo protocol:
1. Sun W, Cai Y, Zhang XX, Chen H, Lin YD, Li H. 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. doi: 10.1038/aps.2017.71. Epub 2017 Jun 12. PMID: 28603288; PMCID: PMC5547558.
2. Tang DZ, Hou W, Zhou Q, Zhang M, Holz J, Sheu TJ, Li TF, Cheng SD, Shi Q, Harris SE, Chen D, Wang YJ. Osthole stimulates osteoblast differentiation and bone formation by activation of beta-catenin-BMP signaling. J Bone Miner Res. 2010 Jun;25(6):1234-45. doi: 10.1002/jbmr.21. PMID: 20200936; PMCID: PMC3153131.
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