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Submit ReviewAsunaprevir
说明： Potent hepatitis C virus (HCV) NS3 protease inihibitor
化学名： 1-[[N-tert-Butoxycarbonyl-L-tert-leucyl-trans-4-[(7-chloro-4-methoxyisoquinolin-1-yl)oxy]-L-prolyl]amino]-N-(cyclopropylsulfonyl)-(1R,2S)-2-vinylcyclopropane-1-carboxamide
纯度： ≥98% (HPLC)
生物活性 for Asunaprevir
Asunaprevir is a potent HCV NS3 protease inhibitor (IC50 = 0.2-3.5 nM). Asunaprevir can be used to control CRIPSR-Cas9 gene editing via the small molecule-assisted shut-off (SMASh) technique, which involves fusion of Cas9 to a peptide comprising a protease domain and a degron tag. Asuprenavir blocks the protease-mediated removal of the degron tag leading to degradation of Cas9 through proteasome and autophagolysosome pathways. It can also be used as a resversible switch to control CAR (chimeric antigen receptor)-T cells, where the CAR has been modified by insertion of a hepatitis C virus nonstructural protein 3 protease (HCV-NS3) between the scFv and the hinge domains. Also inhibits SARS-CoV-2 Mpro activity (IC50 = 15-48.4 μM).
技术数据 for Asunaprevir
| 分子量 | 748.29 |
| 公式 | C35H46ClN5O9S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 630420-16-5 |
| PubChem ID | 16076883 |
| InChI Key | XRWSZZJLZRKHHD-WVWIJVSJSA-N |
| Smiles | O=C([C@H]1N(C[C@@H](C1)OC2=NC=C(OC)C3=C2C=C(Cl)C=C3)C([C@H](C(C)(C)C)NC(OC(C)(C)C)=O)=O)N[C@]4([C@@H](C4)C=C)C(NS(=O)(C5CC5)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Asunaprevir
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 74.83 | 100 | |
| ethanol | 7.48 | 10 |
制备储备液 for Asunaprevir
以下数据基于产品分子量 748.29。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.34 mL | 6.68 mL | 13.36 mL |
| 5 mM | 0.27 mL | 1.34 mL | 2.67 mL |
| 10 mM | 0.13 mL | 0.67 mL | 1.34 mL |
| 50 mM | 0.03 mL | 0.13 mL | 0.27 mL |
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产品说明书 for Asunaprevir
参考文献 for Asunaprevir
参考文献是支持产品生物活性的出版物。
Chung et al (2015) Tunable and reversible drug control of protein production via a self-excising degron. Nat.Chem.Biol. 11 713 PMID: 26214256
Wu et al (2020) A small molecule-controlled Cas9 repressible system. Mol.Ther.Nucleic Acids 19 922 PMID: 32000033
Bafna et al (2021) Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture. Cell Rep. 35 109133 PMID: 33984267
Cao et al (2022) A reversible chemogenetic switch for chimeric antigen receptor T cells. Angew.Chem.Int.Ed.Engl. 61 e202109550 PMID: 34783141
If you know of a relevant reference for Asunaprevir, please let us know.
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关键词: Asunaprevir, Asunaprevir supplier, potent, protease, inhibitors, SARS-CoV-2, SARSCOV2, SMASh, Mpro, T-cells, Tcells, degron, chimeric, antigen, receptors, CART, protein, degradation, CAR-T, reversible, chemogenetic, switch, Hepatitis, Viruses, 3C, and, 3CL, Proteases, Coronavirus, CRISPR, Reagents, 7755, Tocris Bioscience
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