WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H525675
CAS#: 500355-52-2
Description: MK-0873 is a phosphodiesterase 4 (PDE4) inhibitor. Along with a minipig skin biopsy model, it has shown as an innovative tool to design topical formulation to achieve desired pharmacokinetics in humans.
Hodoodo Cat#: H525675
Name: MK-0873
CAS#: 500355-52-2
Chemical Formula: C25H18N4O3
Exact Mass: 422.14
Molecular Weight: 422.444
Elemental Analysis: C, 71.08; H, 4.30; N, 13.26; O, 11.36
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Synonym: MK0873; MK 0873; MK-0873
IUPAC/Chemical Name: 3-((3-(3-(cyclopropylcarbamoyl)-4-oxo-1,8-naphthyridin-1(4H)-yl)phenyl)ethynyl)pyridine 1-oxide
InChi Key: JJWKQXNHYDJXKF-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H18N4O3/c30-23-21-7-2-12-26-24(21)29(16-22(23)25(31)27-19-10-11-19)20-6-1-4-17(14-20)8-9-18-5-3-13-28(32)15-18/h1-7,12-16,19H,10-11H2,(H,27,31)
SMILES Code: O=C(C1=CN(C2=CC=CC(C#CC3=C[N+]([O-])=CC=C3)=C2)C4=NC=CC=C4C1=O)NC5CC5
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 422.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Mitra A, Leyes A, Manser K, Roadcap B, Mestre C, Tatosian D, Jin L, Uemura N. Use of minipig skin biopsy model as an innovative tool to design topical formulation to achieve desired pharmacokinetics in humans. J Pharm Sci. 2015 May;104(5):1701-8. doi: 10.1002/jps.24383. Epub 2015 Feb 17. PubMed PMID: 25691117.
2: Guay D, Boulet L, Friesen RW, Girard M, Hamel P, Huang Z, Laliberté F, Laliberté S, Mancini JA, Muise E, Pon D, Styhler A. 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. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5554-8. doi: 10.1016/j.bmcl.2008.09.009. Epub 2008 Sep 6. PubMed PMID: 18835163.
3: Boot JD, De Haas SL, Van Gerven JM, De Smet M, Leathem T, Wagner J, Denker A, Miller D, Van Doorn MB, Schoemaker RC, Cohen AF, Diamant Z. MK-0873, a PDE4 inhibitor, does not influence the pharmacokinetics of theophylline in healthy male volunteers. Pulm Pharmacol Ther. 2008;21(3):573-7. doi: 10.1016/j.pupt.2008.01.009. Epub 2008 Feb 3. PubMed PMID: 18321743.