MK-0668 is an extremely potent and orally active antagonist of very late antigen-4 with picomolar, whole blood activity and slow dissociation rates were discovered by incorporating an amino substituent on the proline fragment of the initial lead structure. This level of potency against the unactivated form of VLA-4 was shown to be sufficient to overcome the poor pharmacokinetic profiles typical of this class of VLA-4 antagonists, and sustained activity as measured by receptor occupancy was achieved in preclinical species after oral dosing.
MedKoo Cat#: 525667
Name: MK-0668 Mesylate
CAS#: 865111-04-2 (mesylate)
Chemical Formula: C32H34Cl2N6O9S2
Exact Mass: 780.1206
Molecular Weight: 781.68
Elemental Analysis: C, 49.17; H, 4.38; Cl, 9.07; N, 10.75; O, 18.42; S, 8.20
The following data is based on the product molecular weight 781.68 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 |
