Hispidol

SKU: orb1302955

Description

Hispidol ((Z)-Hispidol) is a promising candidate for inflammatory bowel disease (IBD) research. It potently inhibits TNF-α-induced monocyte adhesion to colon epithelial cells with an IC50 of 0.50 μM. Studies suggest its anti-inflammatory effects are relevant for both in vitro mechanistic studies and in vivo models of intestinal inflammation.

Research Area

Cell Biology

Key Properties

• CAS Number: 5786-54-9
• MW: 254.24
• Purity: >99.99% (May vary between batches)
• Formula: C₁₅H₁₀O₄
• SMILES: Oc1ccc(\C=C2/Oc3cc(O)ccc3C2=O)cc1
• Target: TNF
• Solubility: DMSO:6.25 mg/mL (24.58 mM)

Bioactivity

• Target IC50:
  TNF-α:0.50 μM
• In Vivo:
  Oral administration of hispidol suppresses TNBS-induced colitis in a dose-dependent manner. Body weight loss and colon tissue edematous inflammation are recovered significantly. The oral administration of hispidol suppresses significantly and dose-dependently TNBS-induced rat colitis. A higher dose (30 mg/kg) of hispidol shows a similar recovery effect to that of 300 mg/kg sulfasalazine. In the colon tissues, TNBS induces a dramatic increase in the level of MPO, a biochemical marker of inflammation, which is suppressed significantly by hispidol in a dose-dependent manner.
• In Vitro:
  Hispidol demonstrates potent inhibitory effects on TNF-α-induced adhesion of monocytes to colonic epithelial cells and LPS-induced TNF-α expression, making it a promising candidate for inflammatory bowel disease (IBD) drug development. This compound not only inhibits TNF-α expression effectively (>70%)—a critical event in IBD progression—but also suppresses AP-1 transcriptional activity, which is essential for high levels of TNF-α expression.
• Animal Research:
  Hispidol is prepapred in corn oil.Rat: To study the effect of the drugs, hispidol (10 or 30 mg/Kg/day in corn oil) is administered orally once in a day, until 5 days after TNBS administration. The doses of 10 or 30 mg/kg are selected based on previous studies. The concentration of the compound inhibiting 70% and 90% (μM) cell-to-cell adhesion is selected and regarded as the in vivo test dose (mg/kg). Sulfasalazine (300 mg/Kg/day) is administered in corn oil as a positive control. On the 6th day, the rats are sacrificed and the severity of colitis and macroscopic ulceration are evaluated by two independent investigators who are blinded to the experiments. The colon tissues (5-7 cm proximal to rectum) are cut and used to measure the amount of myeloperoxidase and for the histological examinations.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Hispidol, (Z)-Hispidol, TNF Receptor, TNF-α

Compound Identifiers

PubChem CID

5281254