2. NF-κB
  3. Keap1-Nrf2
  4. Isosorbide di-(methyl fumarate)

Isosorbide di-(methyl fumarate)  (Synonyms: IDMF)

Cat. No.: HY-183326 Pureza: 99.87%
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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.

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Isosorbide di-(methyl fumarate)

Isosorbide di-(methyl fumarate) Estructura química

No. CAS : 2013542-44-2

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Isosorbide di-(methyl fumarate) Related Antibodies

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Descripciòn

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[1].

In Vitro

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.

Isosorbide di-(methyl fumarate) Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: Neonatal human dermal fibroblasts
Concentration: 25, 50, 100 μg/mL
Incubation Time: 1 h
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.
In Vivo

Isosorbide di-(methyl fumarate) (100 mg of topical cream; topical; 5 days/week; 13 days) applied to normal mouse tail skin increases granular layer thickness and orthokeratosis without inducing skin irritation or pathological changes[1].
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.

Animal Model: BALB/c (male, 5-7 weeks old)[1]
Dosage: 100 mg of IDMF topical cream
Administration: topical; once daily (5 days/week); 13 days
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.
Animal Model: BALB/c (male, 8-9 weeks old, psoriasiform lesions induced by daily topical 5% Imiquimod cream for 5 days)[1]
Dosage: 5% IDMF lotion
Administration: topical; once daily; 6 days (1 hour after imiquimod on days 1-5, alone on day 6)
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.
Peso molecular

370.31

Fòrmula

C16H18O10
No. CAS
Appearance

Solid

Color

White to light yellow

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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Isosorbide di-(methyl fumarate)2013542-44-2IDMFKeap1-Nrf2human embryonic kidney 293 cellsANCRIL-17Apsoriasis vulgariskeratinocytesSalmonella typhimuriumTNFcarboxylesterase 2NRF2/ARE pathwayNF-κBInhibitorinhibitorinhibit

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