1. Materials information
Names
| Name |
4-amino-1-[(2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidin-2-one
|
| Synonym |
More Synonyms
|
PSI-6130 Biological Activity
| Description |
PSI-6130 is a potent and selective inhibitor of HCV NS5B
polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM. |
| Related Catalog |
Signaling Pathways >>
Metabolic Enzyme/Protease >>
HCV Protease
Signaling Pathways >>
Anti-infection >>
HCV
Research Areas >>
Infection
|
| Target |
IC50: 0.6 μM (HCV replication)[2]
|
| In Vitro |
PSI-6130 exhibits potent and specific inhibitory activity against
HCV RNA replication mediated by the NS5B polymerase. Both PSI-6130
inhibit HCV GT-1b (Con1 strain) and GT-1a (H77 strain) subgenomic RNA
replication, with mean EC50 values of 0.51 and 0.30 μM, respectively.
PSI-6130 inhibits 40% human serum with EC50 of 0.51 μM[1]. PSI-6130
inhibits HCV replication with a mean IC50 of 0.6 μM, PSI-6130-TP
inhibits HCV replicase with a mean IC50 of 0.34 μM. PSI-6130-TP inhibits
recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived
from the 3′-end of the negative strand of the HCV genome with an IC50 of
0.13 μM and Ki of 0.023 μM[2].
|
| Kinase Assay |
The inhibition potency of compounds with respect to the RdRp
activity of recombinant NS5B570-BK, NS5B570-Con1, and NS5B570-H77
proteins is determined by measuring the incorporation of radiolabeled
NMP into acid-insoluble RNA products by use of a complement strand of
internal ribosomal entry site (cIRES) RNA template. Briefly, 50%
inhibitory concentration (IC50) determinations are carried out using 200
nM in vitro-transcribed cIRES RNA template, 1 μCi of tritiated UTP (42
Ci/mmol), 500 μM ATP, 500 μM GTP, 1 μM CTP, 1× TMDN buffer (40 mM
Tris-HCl [pH 8.0], 4 mM MgCl2, 4 mM dithiothreitol, 40 mM NaCl), and 200
nM enzyme. The inhibition potency of compounds with respect to the RdRp
activity of NS5B570-S282T-Con1 is determined under GT-1b assay
conditions as. NS5B570-BK and NS5B570-Con1 enzymes are used as controls.
The final reaction volume is 50 μL under all assay conditions. All
reactions contain a final 10% dimethyl sulfoxide. Km and Ki values are
measured.
|
| References |
[1]. Ali
S, et al. Selected replicon variants with low-level in vitro resistance
to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack
cross-resistance with R1479. Antimicrob Agents Chemother. 2008
Dec;52(12):4356-69. [2]. Ma
H, et al. Characterization of the metabolic activation of hepatitis C
virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine
(PSI-6130) and identification of a novel active 5'-triphosphate
species. J Biol Chem. 2007 Oct 12;282(41):29812-20. Epub 2007 Aug 13.
|
Chemical & Physical Properties
| Density |
1.7±0.1 g/cm3 |
| Boiling Point |
482.4±55.0 °C at 760 mmHg |
| Molecular Formula |
C10H14FN3O4 |
| Molecular Weight |
259.234 |
| Flash Point |
245.5±31.5 °C |
| Exact Mass |
259.096832 |
| PSA |
110.60000 |
| LogP |
-0.72 |
| Vapour Pressure |
0.0±2.7 mmHg at 25°C |
| Index of Refraction |
1.653 |
2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
Provide door to door service
Suitable for goods under 50kg
Delivery: 3-7 days
Cost: low cost
Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
Provide seaport to seaport service
Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
4. Contact information
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