Hispidulin A potent benzodiazepine (BZD) receptor ligand

Hispidulin (CAS 1447-88-7)

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Synonym: Dinatin; Scutellarein 6-methyl ether
Application: A potent benzodiazepine (BZD) receptor ligand
CAS Number: 1447-88-7
Molecular Weight: 300.27
Molecular Formula: C16H12O6
* Refer to Certificate of Analysis for lot specific data (including water content).
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Hispidulin is a natural flavanoid which acts as a potent benzodiazepine (BZD) receptor ligand. In addition, hispidulin competitively binds to the benzodiazepine receptor, thus inhibiting 3H-Flumazenil from binding to the receptor. Furthermore, it has been observed that hispidulin has antioxidant, antithrombotic, antifungal, and antiproliferative properties. Alternate studies indicate that hispidulin can inhibit the PI3K/Akt/mTOR signaling pathway in endothelial cells by targeting VEGF receptor 2. Inhibition of this receptor by hispidulin suppressed cell migration, invasion, and capillary-like structure formation of HU-VE-Cs in vascular endothelial cells. Hispidulin also aactivates AMPK.


References

1. Bourdillat, B., et al. 1988. Eur. J. Pharmacol. 147: 1-6. PMID: 2836213
2. Kavvadias, D., et al. 2003. Planta Med. 69: 113-117. PMID: 12624814
3. Kavvadias, D., et al. 2004. Br. J. Pharmacol. 142: 811-820. PMID: 15231642
4. He, L., et al. 2011. Cancer Sci. 102: 219-225. PMID: 21087351

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mM), and ethanol (10 mM).
Storage :
Desiccate at -20° C
Melting Point :
207.00° C (Predicted)
Boiling Point :
~601.51° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.70
IC50 :
Cell division protein kinase 5: EC5050 = 19100 nM (Rattus norvegicus); Influenza A virus: IC50 = 24700 nM (Influenza A virus); Neuraminidase: IC50 = 13.9 ug.mL-1 (Influenza A virus (A/Puerto Rico/8/1934(H1N1)))
Ki Data :
Adenosine A2a receptor: Ki= 6480 nM (Rattus norvegicus); Adenosine A1 receptor: Ki= 1610 nM (Rattus norvegicus)
pK Values :
pKa: 6.51
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5281628
SMILES :
COC1=C(C=C2C(=C1O)C(=O)C=C(O2)C3=CC=C(C=C3)O)O

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Certificate of Analysis

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Hispidulin  Product Citations

See how others have used Hispidulin. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 26914711  Kwak, JY. et al. 2016. Br. J. Dermatol. 175: 501-11.

Citations 1 to 1 of 1 total
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