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Hispidol

Catalog No. T4319   CAS 5786-54-9
Synonyms: (Z)-Hispidol

Hispidol ((Z)-Hispidol) ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 μM.

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Hispidol Chemical Structure
Hispidol, CAS 5786-54-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 54.00
5 mg In stock $ 89.00
10 mg In stock $ 147.00
25 mg In stock $ 223.00
50 mg In stock $ 289.00
100 mg In stock $ 455.00
200 mg In stock $ 622.00
500 mg In stock $ 1,060.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 100%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Hispidol ((Z)-Hispidol) ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 μM.
Targets&IC50 TNF-α:0.50 μM
In vitro Hispidol exhibits strong inhibitory activities against TNF-α-induced monocytic-colonic epithelial cell adhesion as well as LPS-induced TNF-α expression that is an excellent candidate for IBD drug development. This inhibition of TNF-α expression by hispidol corresponds to the additional inhibitory activity against AP-1 transcriptional activity, which is another transcription factor required for high level TNF-α expression. Hispidol exhibits potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to inflammatory bowel disease (IBD).
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.
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[1].
Synonyms (Z)-Hispidol
Molecular Weight 254.24
Formula C15H10O4
CAS No. 5786-54-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL

TargetMolReferences and Literature

1. Kadayat TM, et al. Discovery and structure-activity relationship studies of 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives as a novel class of potential therapeutics for inflammatory bowel disease. Eur J Med Chem. 2017 Sep 8;137:575-597.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Apoptosis Compound Library Angiogenesis related Compound Library HIF-1 Signaling Pathway Compound Library Anti-Cardiovascular Disease Compound Library Anti-Aging Compound Library Immuno-Oncology Compound Library Bioactive Compound Library Pyroptosis Compound Library NO PAINS Compound Library

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Keywords

Hispidol 5786-54-9 Apoptosis TNF inhibit (Z)-Hispidol TNF Receptor Tumor Necrosis Factor Receptor TNFR Inhibitor inhibitor

 

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