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.
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- Pureté: 95.0%
- CAS No.: 500355-52-2
- Formule: C25H18N4O3
- Masse moléculaire:422.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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PDE4 ＜38 nM (IC50) |
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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] |
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.
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.
| 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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Masse moléculaire 422.44
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (277 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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Instruction de manipulation (2659 KB)
Références
[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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