MK-0873
Based on 1 Customer Validation
MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of < 38 nM. MK-0873 inhibits LPS-induced TNF-α production. MK-0873 suppresses bronchoconstriction. MK-0873 is applicable to research related to chronic obstructive pulmonary disease, plaque psoriasis and asthma.
For research use only. We do not sell to patients.
- Purity : 95.0%
- CAS No.: 500355-52-2
- Formula: C25H18N4O3
- Molecular Weight:422.44
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PDE4 ＜38 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
65.7 μM
Compound: 20, MK-0873
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Displacement of [35S]MK-499 from human ERG expressed in HEK293 cells
Displacement of [35S]MK-499 from human ERG expressed in HEK293 cells
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[PMID: 18835163] |
| Sf9 | IC50 |
6.7 nM
Compound: 20, MK-0873
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Intrinsic inhibition of GST-fused human PDE4A expressed in SF9 cells
Intrinsic inhibition of GST-fused human PDE4A expressed in SF9 cells
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[PMID: 18835163] |
In Vitro
MK-0873 is a selective PDE4 inhibitor that potently inhibits PDE-4 isoforms with IC50 values <38 nM and shows negligible activity against other PDE enzymes (IC50 >6 μM)[1].
MK-0873 potently inhibits human GST-PDE4A248 with an IC50 of 6.7 nM[3].
MK-0873 inhibits LPS-induced TNF-α production in human whole blood with an IC50 of 178 nM[3].
MK-0873 inhibits LPS-induced TNF-α production in squirrel monkey whole blood with an IC50 of 23 nM[3].
MK-0873 binds to hERG potassium channels from stably transfected HEK293 cells with an IC50 of 66 μM, showing low affinity[3].
MK-0873 weakly inhibits cytochrome P450 2C9 with an IC50 of 41 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MK-0873 (0.03 mg/kg; i.p.; single dose) produces 65% inhibition of Ovalbumin (HY-W250978)-induced bronchoconstriction in sensitized guinea pigs[3].
MK-0873 (0.5 mg/kg/day; i.v.; daily; 4 days) produces 84% inhibition of late-phase Ascaris-induced bronchoconstriction in sensitized sheep[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:unspecified strain (conscious, sensitized, n > 5)[3]
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Dosage:0.03 mg/kg
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Administration:i.p.; single dose
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Result:Produced 65% mean inhibition of ovalbumin-induced bronchoconstriction.
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Animal Model:unspecified strain (Ascaris-sensitive)[3]
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Dosage:0.5 mg/kg/day
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Administration:i.v.; daily; 4 days
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Result:Produced 84% mean inhibition of late-phase Ascaris-induced bronchoconstriction.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 500355-52-2
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Appearance Solid
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Molecular Weight 422.44
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Formula C25H18N4O3
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Color Off-white to light yellow
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SMILES
O=C(C1=CN(C2=CC(C#CC3=C[N+]([O-])=CC=C3)=CC=C2)C4=NC=CC=C4C1=O)NC5CC5
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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
Protocols
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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.
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Imiquimod-Induced Psoriasiform Dermatitis
Imiquimod (IMQ)-induced psoriasiform dermatitis is a widely used murine model in which topical application of IMQ, a Toll-like receptor 7 (TLR7) agonist, triggers innate immune activation in the skin and induces a psoriasis-like inflammatory cascade characterized by epidermal hyperplasia, immune cell infiltration, and cytokine production dominated by the IL-23/IL-17 axis. This inflammatory response is mediated through activation of dendritic cells and downstream induction of IL-23, IL-17A, IL-22, and related pro-inflammatory mediators, recapitulating key features of human plaque psoriasis and enabling mechanistic and therapeutic studies. The model is commonly induced using Aldara (5% IMQ cream) applied topically to murine skin, resulting in rapid onset of erythema, scaling, and thickening that can be quantified as disease severity indices and validated histologically.
Purity & Documentation
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Data Sheet (289 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
[1]. Boot JD, et al. MK-0873, a PDE4 inhibitor, does not influence the pharmacokinetics of theophylline in healthy male volunteers. Pulmonary pharmacology & therapeutics. 2008;21(3):573-7. [Content Brief]
[2]. Rafael A, et al. Topical therapy for psoriasis: a promising future. Focus on JAK and phosphodiesterase-4 inhibitors. Eur J Dermatol. 2016 Jan-Feb;26(1):3-8. [Content Brief]
[3]. Guay D, et al. Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. Bioorganic & medicinal chemistry letters. 2008 Oct 15;18(20):5554-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-0873 Related Classifications
HY-108047 Related Classifications
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