Cat. No.: HY-102040

Hispidol

Name: Hispidol
Brand: MedChemExpress
SKU: HY-102040
Price: 110.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: (Z)-Hispidol)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity : 98.30%
CAS No.: 5786-54-9
Formula: C₁₅H₁₀O₄
Molecular Weight:254.24

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Hispidol Chemical Structure

CAS No.: 5786-54-9

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Protocols (3)
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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.

All TNF Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	0.5 μM Compound: 55	Inhibition of TNF-alpha-induced adhesion of BCECF-labeled human U937 cells to human HT-29 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 3 hrs by fluorescence microscopic method Inhibition of TNF-alpha-induced adhesion of BCECF-labeled human U937 cells to human HT-29 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 3 hrs by fluorescence microscopic method	[PMID: 28646757]
RAW264.7	IC₅₀	1.06 μM Compound: 2c	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production treated 1 hr before LPS challenge measured after 24 hrs by EIA Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production treated 1 hr before LPS challenge measured after 24 hrs by EIA	[PMID: 21723122]
RAW264.7	IC₅₀	38.7 μM Compound: 2c	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess reaction Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess reaction	[PMID: 21723122]
RAW264.7	IC₅₀	99.79 μM Compound: 2c	Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay	[PMID: 21723122]

In Vitro

Hispidol shows 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). Hispidol shows strong inhibitory activities against TNF-α-induced monocytic-colonic epithelial cell adhesion as well as LPS-induced TNF-α expression, is as 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

The oral administration of hispidol suppresses significantly and dose-dependently TNBS-induced rat colitis. Oral administration of hispidol suppresses TNBS-induced colitis in a dose-dependent manner. There is a significant recovery in body weight decrease and colon tissue edematous inflammation. 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 5786-54-9
Appearance Solid
Molecular Weight 254.24
Formula C₁₅H₁₀O₄
Color Light yellow to yellow
SMILES

O=C1C2=CC=C(O)C=C2O/C1=C\C3=CC=C(O)C=C3
Synonyms

(Z)-Hispidol
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Bioorg Med Chem

Synthesis and biological evaluation of O4'-benzyl-hispidol derivatives and analogs as dual monoamine oxidase-B inhibitors and anti-neuroinflammatory agents. [Abstract]

2024 Aug 1:110:117826. PMID: 39004050

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (393.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.9333 mL

19.6665 mL

39.3329 mL

5 mM

0.7867 mL

3.9333 mL

7.8666 mL

10 mM

0.3933 mL

1.9666 mL

3.9333 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Protocols

All Cell Biology Animals and Diseases

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
DSS-Induced Colitis
Dextran sulfate sodium (DSS)-induced colitis is generated by administering DSS in mouse drinking water, producing epithelial injury, barrier disruption, weight loss, diarrhea, fecal blood, colon shortening, histologic mucosal damage, and inflammatory mediator changes; the model is mainly used to study acute or chronic intestinal inflammation resembling selected features of ulcerative colitis. DSS injury is interpreted through clinical and tissue readouts rather than a single molecular endpoint: daily body weight, stool consistency, and bleeding are combined into a disease activity index, while colon length, histology, cytokines, myeloperoxidase activity, intestinal permeability, and tight-junction markers provide complementary measures of inflammation and barrier damage.
TNBS-Induced Colitis
TNBS-induced colitis is produced by intrarectal delivery of 2,4,6-trinitrobenzene sulfonic acid in ethanol, where ethanol disrupts the mucosal barrier and TNBS haptenates colonic proteins, generating immune-mediated colonic inflammation with weight loss, diarrhea, ulceration, transmural injury, inflammatory-cell infiltration, and cytokine responses. The model is used as an experimental intestinal inflammation model with Crohn’s disease–like features, especially when Th1-type responses, IL-12–dependent inflammation, chronic relapsing inflammation, or fibrosis-related endpoints are studied.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.9333 mL	19.6665 mL	39.3329 mL	98.3323 mL
	5 mM	0.7867 mL	3.9333 mL	7.8666 mL	19.6665 mL
	10 mM	0.3933 mL	1.9666 mL	3.9333 mL	9.8332 mL
	15 mM	0.2622 mL	1.3111 mL	2.6222 mL	6.5555 mL
	20 mM	0.1967 mL	0.9833 mL	1.9666 mL	4.9166 mL
	25 mM	0.1573 mL	0.7867 mL	1.5733 mL	3.9333 mL
	30 mM	0.1311 mL	0.6555 mL	1.3111 mL	3.2777 mL
	40 mM	0.0983 mL	0.4917 mL	0.9833 mL	2.4583 mL
	50 mM	0.0787 mL	0.3933 mL	0.7867 mL	1.9666 mL
	60 mM	0.0656 mL	0.3278 mL	0.6555 mL	1.6389 mL
	80 mM	0.0492 mL	0.2458 mL	0.4917 mL	1.2292 mL
	100 mM	0.0393 mL	0.1967 mL	0.3933 mL	0.9833 mL

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Hispidol

Publications Citing Use of MedChemExpress (MCE) Hispidol

All TNF Receptor Isoforms