Isosorbide di-(methyl fumarate)
Based on 1 Customer Validation
Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 2013542-44-2
- Formula: C16H18O10
- Molecular Weight:370.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Isosorbide di-(methyl fumarate) (25-100 μg/mL; 1 h) does not exhibit phototoxicity in neonatal human dermal fibroblasts[1].
Isosorbide di-(methyl fumarate) (1-200 μg/mL) does not exhibit mutagenic effects in Salmonella typhimurium strains TA1535 and TA1537[1].
Isosorbide di-(methyl fumarate) (24 h) upregulates genes associated with oxidative stress response and xenobiotic metabolism, while downregulating genes associated with immune response and epithelial differentiation, in cytokine-stimulated human keratinocytes[1].
Isosorbide di-(methyl fumarate) (1-10 μg/mL; 24 h) activates the NRF2/ARE pathway in human embryonic kidney 293 cells, with significant increases in the expression of the luciferase re-
porter gene[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neonatal human dermal fibroblasts
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Concentration:25, 50, 100 μg/mL
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Incubation Time:1 h
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Result:Resulted in neutral red uptake of 97.1% in UVA(-) cells and 84.7% in UVA(+) cells at 25 μg/mL.
Resulted in neutral red uptake of 57.5% in UVA(-) cells and 53% in UVA(+) cells at 50 μg/mL.
Resulted in neutral red uptake of 1.3% in UVA(-) cells and 0.3% in UVA(+) cells at 100 μg/mL.
Showed UVA treatment significantly reduced viability at 0, 25, and 50 μg/mL, but the magnitude of reduction was similar between UVA(-) and UVA(+) cells at each concentration, indicating no phototoxic effect.
Isosorbide di-(methyl fumarate) (200-2000 mg/kg; topical; single dose) in female Wistar rats cause no acute dermal toxicity, skin irritation, or systemic adverse effects[1].
Isosorbide di-(methyl fumarate) (500 mg; topical; single dose; 4 h) in male New Zealand White rabbits causes only transient, very slight skin irritation that resolves rapidly[1].
Isosorbide di-(methyl fumarate) (100 mg; topical; 6 hours on days 0, 7, 14 (induction); 6 hours on day 28 (challenge)) in Hartley guinea pigs does not elicit skin sensitization or systemic adverse effects[1].
Isosorbide di-(methyl fumarate) (5% lotion; topical; once daily; 6 days) significantly reduces erythema, scaling, and skin thickness in Imiquimod (HY-B0180)-induced psoriasiform mouse lesions, while modulating gene expression to repress immune responses and support epidermal development[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 5-7 weeks old)[1]
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Dosage:100 mg of IDMF topical cream
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Administration:topical; once daily (5 days/week); 13 days
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Result:Did not cause erythema or increase skin scale.
Increased the granular layer by 28% and orthokeratosis by 34.5%.
No leukocytic infiltrate, parakeratosis, or hyperkeratosis was observed.
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Animal Model:BALB/c (male, 8-9 weeks old, psoriasiform lesions induced by daily topical 5% Imiquimod cream for 5 days)[1]
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Dosage:5% IDMF lotion
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Administration:topical; once daily; 6 days (1 hour after imiquimod on days 1-5, alone on day 6)
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Result:Significantly reduced skin erythema on days 5 and 6.
Reduced skin scaling/flaking and skin thickness on day 6.
Upregulated 68 genes associated with hair cycle and epidermis development.
Downregulated 98 genes associated with immune response activation, granulocyte migration, and immune effector process.
Chemical Information
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CAS No. 2013542-44-2
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Appearance Solid
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Molecular Weight 370.31
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Formula C16H18O10
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Color White to light yellow
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SMILES
COC(/C=C/C(O[C@H]1[C@]2([H])[C@@](OC1)([H])[C@H](CO2)OC(/C=C/C(OC)=O)=O)=O)=O
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Synonyms
IDMF
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 33.33 mg/mL (90.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7004 mL | 13.5022 mL | 27.0044 mL | 67.5110 mL |
| 5 mM | 0.5401 mL | 2.7004 mL | 5.4009 mL | 13.5022 mL | |
| 10 mM | 0.2700 mL | 1.3502 mL | 2.7004 mL | 6.7511 mL | |
| 15 mM | 0.1800 mL | 0.9001 mL | 1.8003 mL | 4.5007 mL | |
| 20 mM | 0.1350 mL | 0.6751 mL | 1.3502 mL | 3.3756 mL | |
| 25 mM | 0.1080 mL | 0.5401 mL | 1.0802 mL | 2.7004 mL | |
| 30 mM | 0.0900 mL | 0.4501 mL | 0.9001 mL | 2.2504 mL | |
| 40 mM | 0.0675 mL | 0.3376 mL | 0.6751 mL | 1.6878 mL | |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5401 mL | 1.3502 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4501 mL | 1.1252 mL | |
| 80 mM | 0.0338 mL | 0.1688 mL | 0.3376 mL | 0.8439 mL |
Isosorbide di-(methyl fumarate) Related Classifications
HY-183326 Related Classifications
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