TMC310911
Based on 1 publication(s) in Google Scholar
TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity.
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- 純度: 99.85%
- CAS 番号: 1000287-05-7
- 分子式: C38H53N5O7S2
- 分子量:755.99
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Anti-Infection Compound Library
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MedChemExpress（MCE）の使用を引用している文献 TMC310911
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生物活性
EC50: 2.2-14.2 nM (Wild-type HIV-1)[1]
For a panel of 2,011 recombinant isolates with decreased susceptibility to at least one of the currently approved protease inhibitors (PIs), the FC in TMC310911 EC50 is ≤4 for 82% of isolates and ≤10 for 96% of isolates. The fold change (FC) in TMC310911 EC50 is ≤4 and ≤10 for 72% and 94% of isolates with decreased susceptibility to Darunavir, respectively. In vitro resistance selection (IVRS) performed with r13025, a multiple-PI-resistant recombinant isolate, and TMC310911 selected for mutations L10F, I47V, and L90M (FC in TMC310911 EC50 = 16)[1].
The TMC310911 EC50 values against HIV-1/LAI and HIV-2/ROD in MT4 cells with EC50 values of 14.2 nM and 2 nM, respectively, and HIV-1/LAI and HIV-1/SF2 in PBMCs with EC50 values of 2.2 nM and 2.3 nM, respectively, and HIV-1/BaL in M/M cells with an EC50 value of 13.9 nM. And the corresponding EC90 values ranged from 5.0 to 94.7 nM. The TMC310911 CC50 for MT4 cells is 9.9 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1000287-05-7
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性状 Solid
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分子量 755.99
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分子式 C38H53N5O7S2
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Color White to off-white
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SMILES
O=C(O[C@@H]1[C@@]2([H])[C@@](OCC2)([H])OC1)N[C@@H](CC3=CC=CC=C3)[C@H](O)CN(S(=O)(C4=CC=C5N=C(NC6CCN(C7CCCC7)CC6)SC5=C4)=O)CC(C)C
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別名
ASC-09
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Darunavir inhibits dengue virus replication by targeting the hydrophobic pocket of the envelope protein. [Abstract]2025 May:235:116839. PMID: 40024350
溶剤 & 溶解度
DMSO : 100 mg/mL (132.28 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
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データシート (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Dierynck I, et al. TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors. Antimicrob Agents Chemother. 2011 Dec;55(12):5723-31. [Content Brief]
[2]. Stellbrink HJ, et al. Antiviral activity, pharmacokinetics, and safety of the HIV-1 protease inhibitor TMC310911, coadministered with ritonavir, in treatment-naive HIV-1-infected patients. J Acquir Immune Defic Syndr. 2014 Mar 1;65(3):283-9. [Content Brief]
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 | 1.3228 mL | 6.6138 mL | 13.2277 mL | 33.0692 mL |
| 5 mM | 0.2646 mL | 1.3228 mL | 2.6455 mL | 6.6138 mL | |
| 10 mM | 0.1323 mL | 0.6614 mL | 1.3228 mL | 3.3069 mL | |
| 15 mM | 0.0882 mL | 0.4409 mL | 0.8818 mL | 2.2046 mL | |
| 20 mM | 0.0661 mL | 0.3307 mL | 0.6614 mL | 1.6535 mL | |
| 25 mM | 0.0529 mL | 0.2646 mL | 0.5291 mL | 1.3228 mL | |
| 30 mM | 0.0441 mL | 0.2205 mL | 0.4409 mL | 1.1023 mL | |
| 40 mM | 0.0331 mL | 0.1653 mL | 0.3307 mL | 0.8267 mL | |
| 50 mM | 0.0265 mL | 0.1323 mL | 0.2646 mL | 0.6614 mL | |
| 60 mM | 0.0220 mL | 0.1102 mL | 0.2205 mL | 0.5512 mL | |
| 80 mM | 0.0165 mL | 0.0827 mL | 0.1653 mL | 0.4134 mL | |
| 100 mM | 0.0132 mL | 0.0661 mL | 0.1323 mL | 0.3307 mL |
TMC310911 関連分類
HY-107123 関連分類
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