| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
PSI-6206 (also known as GS331007 and RO-2433), a deaminated derivative of PSI-6130, is a novel, potent and selective HCV NS5B polymerase inhibitor. In a subgenomic HCV replicon assay system, PSI-6206 and 2'-C-methylcytidine were shown to be strong and specific inhibitors of HCV replication. Comparing PSI-6206 to 2'-C-methylcytidine in the HCV replicon assay, it demonstrates lower cellular toxicity and more inhibitory activity.
| Targets |
HCV (EC90 >100 μM)
|
|---|---|
| ln Vitro |
PSI-6206 (RO 2433) is subjected to surrogate bovine viral diarrhea virus (BVDV) assays as well as a cell-based quantitative real-time RT-PCR assay to assess its anti-HCV activity. No assay shows any activity or cytotoxicity from PSI-6206[1]. PSI-6130 (PSI-6130-TP) and RO2433 (RO2433-TP) both form 5′-triphosphate (TP) that steadily increases over time, reaching steady state levels after 48 hours. Additionally, RO2433-TP prevents both the recombinant HCV polymerase NS5B and the native HCV replicase that is separated from HCV replicon cells from synthesizing RNA[2]. A strong and specific inhibitor of HCV NS5B polymerase, PSI-6206 (RO2433) is the deaminated derivative of PSI-6130[3].
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| References |
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| Molecular Formula |
C10H13FN2O5
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|---|---|
| Molecular Weight |
260.2190
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| Exact Mass |
260.08
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| Elemental Analysis |
C, 46.16; H, 5.04; F, 7.30; N, 10.77; O, 30.74
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| CAS # |
863329-66-2
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| Related CAS # |
PSI-6206-13C,d3;1256490-42-2
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| PubChem CID |
11311503
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Melting Point |
237-238℃
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| Index of Refraction |
1.596
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| LogP |
-0.77
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
415
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
C[C@]1([C@H](O)[C@@H](CO)O[C@H]1N1C=CC(=O)NC1=O)F
|
| InChi Key |
ARKKGZQTGXJVKW-VPCXQMTMSA-N
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| InChi Code |
InChI=1S/C10H13FN2O5/c1-10(11)7(16)5(4-14)18-8(10)13-3-2-6(15)12-9(13)17/h2-3,5,7-8,14,16H,4H2,1H3,(H,12,15,17)/t5-,7-,8-,10-/m1/s1
|
| Chemical Name |
1-[(2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidine-2,4-dione
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| Synonyms |
RO-2433; RO2433; RO 2433; PSI6206; PSI 6206; PSI-6206; GS-331007; GS 331007; GS331007
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~52 mg/mL (~199.8 mM)
Ethanol: ~24 mg/mL (~92.2 mM) Water: ~52 mg/mL (~199.8 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8429 mL | 19.2145 mL | 38.4290 mL | |
| 5 mM | 0.7686 mL | 3.8429 mL | 7.6858 mL | |
| 10 mM | 0.3843 mL | 1.9215 mL | 3.8429 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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