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
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
Preparing Stock Solutions
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 |
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.
