IDX184
Based on 1 Customer Validation
IDX184 is a potent and orally bioavailable inhibitor of HCV replication. IDX184 potently inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.80%
- CAS 番号: 1036915-08-8
- 分子式: C25H35N6O9PS
- 分子量:626.62
-
保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
IC50 & Target
IC50: 0.31 μM (HCV polymerase)[2]
Ki: 52.3 nM (HCV polymerase)[2]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | CC50 |
>100 μM
Compound: 2; IDX-184
|
Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion assay
Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion assay
|
[PMID: 26819659] |
| Huh-7 | CC50 |
>100 μM
Compound: 2; IDX-184
|
Cytotoxicity against human HuH7 cells infected with HCV assessed as reduction in cellular rRNA level after 96 hrs by qRT-PCR analysis
Cytotoxicity against human HuH7 cells infected with HCV assessed as reduction in cellular rRNA level after 96 hrs by qRT-PCR analysis
|
[PMID: 26819659] |
| PBMC | CC50 |
>100 μM
Compound: 2; IDX-184
|
Cytotoxicity against human PBMC after 6 days by trypan blue exclusion assay
Cytotoxicity against human PBMC after 6 days by trypan blue exclusion assay
|
[PMID: 26819659] |
| Vero | CC50 |
>100 μM
Compound: 2; IDX-184
|
Cytotoxicity against African green monkey Vero cells after 3 days by hemocytometry
Cytotoxicity against African green monkey Vero cells after 3 days by hemocytometry
|
[PMID: 26819659] |
体外実験
IDX184 is a liver-targeted prodrug of the nucleotide 2′-MeG-MP. IDX184 is a liver-targeted nucleotide polymerase inhibitor of hepatitis C virus[1].
IDX184 is a second generation, orally bioavailable nucleotide prodrug designed to provide increased anti-HCV efficacy and safety versus the parent nucleoside. In HCV replicon testing, IDX184 is the most potent inhibitor (EC50=0.3-0.45 μM) compared to any of the 2’ or 4’ modified nucleosides (EC50=4-6 μM) and is also highly inhibitory in the JFH-1 infectious system (EC50=0.06-0.11 μM). IDX184 is not toxic (CC50>100μM) in any tested cell line[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 1036915-08-8
-
性状 Solid
-
分子量 626.62
-
分子式 C25H35N6O9PS
-
Color White to off-white
-
SMILES
C[C@]([C@](O[C@@H]1CO[P](NCC2=CC=CC=C2)(OCCSC(C(C)(C)CO)=O)=O)([H])N3C(NC(N)=NC4=O)=C4N=C3)([C@@H]1O)O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 250 mg/mL (398.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (274 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5959 mL | 7.9793 mL | 15.9586 mL | 39.8966 mL |
| 5 mM | 0.3192 mL | 1.5959 mL | 3.1917 mL | 7.9793 mL | |
| 10 mM | 0.1596 mL | 0.7979 mL | 1.5959 mL | 3.9897 mL | |
| 15 mM | 0.1064 mL | 0.5320 mL | 1.0639 mL | 2.6598 mL | |
| 20 mM | 0.0798 mL | 0.3990 mL | 0.7979 mL | 1.9948 mL | |
| 25 mM | 0.0638 mL | 0.3192 mL | 0.6383 mL | 1.5959 mL | |
| 30 mM | 0.0532 mL | 0.2660 mL | 0.5320 mL | 1.3299 mL | |
| 40 mM | 0.0399 mL | 0.1995 mL | 0.3990 mL | 0.9974 mL | |
| 50 mM | 0.0319 mL | 0.1596 mL | 0.3192 mL | 0.7979 mL | |
| 60 mM | 0.0266 mL | 0.1330 mL | 0.2660 mL | 0.6649 mL | |
| 80 mM | 0.0199 mL | 0.0997 mL | 0.1995 mL | 0.4987 mL | |
| 100 mM | 0.0160 mL | 0.0798 mL | 0.1596 mL | 0.3990 mL |