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MK-608

Names

[ CAS No. ]:
443642-29-3

[ Name ]:
MK-608

[Synonym ]:
MK-608
Lamevudine
(2R,3R,4R,5R)-2-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(hydroxymethyl)-3-methyltetrahydrofuran-3,4-diol
7-deaza-2’-C-methyladenosine
7-Deaza-2'-C-methyladenosine
7DMA
7-(2-C-Methyl-β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-(2-C-methyl-β-D-ribofuranosyl)-

Biological Activity

[Description]:

MK-0608 is a potent and orally bioavailable inhibitor of HCV replication in vitro with an EC50 of 0.3 μM (EC90=1.3 μM) in the subgenomic-replicon assay[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HCV
Research Areas >> Infection

[Target]

EC50: 0.3 μM (HCV replication)[1]


[In Vivo]

Oral dosing of MK-0608 results in a potent antiviral effect. In preclinical pharmacokinetic experiments with rats, dogs, and rhesus monkeys, MK-0608 demonstrates good to excellent oral bioavailability (50 to 100%) and long plasma half-lives in dogs and rhesus macaques (9 and 14 h, respectively)[1]. Animal Model: The HCV-infected chimpanzees[1] Dosage: 1 mg/kg Administration: Administered orally; once daily for 37 days Result: Chimpanzee X6 had a baseline viral load that varied from 1,110 to 12,900 IU/mL, and chimpanzee X4 had a baseline viral load of 3×106 to 9×106 IU/mL.

[References]

[1]. Carroll SS, et al. Robust antiviral efficacy upon administration of a nucleoside analog to hepatitis C virus-infected chimpanzees. Antimicrob Agents Chemother. 2009 Mar;53(3):926-34.

Chemical & Physical Properties

[ Density]:
1.8±0.1 g/cm3

[ Boiling Point ]:
620.7±55.0 °C at 760 mmHg

[ Melting Point ]:
222 °C(Solv: methanol (67-56-1)

[ Molecular Formula ]:
C12H16N4O4

[ Molecular Weight ]:
280.280

[ Flash Point ]:
329.2±31.5 °C

[ Exact Mass ]:
280.117157

[ PSA ]:
126.65000

[ LogP ]:
0.22

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.769

[ Storage condition ]:
2-8°C

Related Compounds