Asunaprevir

Name: Asunaprevir
Brand: Tocris Bioscience
SKU: 7755

Tocris Bioscience, part of Bio-Techne | Catalog # 7755

COA / SDS

Potent hepatitis C virus (HCV) NS3 protease inihibitor

Key Product Details

Description:	Potent hepatitis C virus (HCV) NS3 protease inihibitor
Chemical Name:	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
Purity:	≥98% (HPLC)
Molecular Weight:	748.29

View Full Technical Details for Asunaprevir

Technical Data
Citations

Biological Activity 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 M^pro activity (IC₅₀ = 15-48.4 μM).

Technical Data for Asunaprevir

M. Wt	748.29
Formula	C₃₅H₄₆ClN₅O₉S
Storage	Store at -20°C
Purity	≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Asunaprevir

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	74.83	100
	ethanol	7.48	10

Preparing Stock Solutions for Asunaprevir

The following data is based on the product molecular weight 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.

Concentration / Solvent Volume / Mass	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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References for Asunaprevir

References are publications that support the biological activity of the product.

Cao A reversible chemogenetic switch for chimeric antigen receptor T cells. Angew.Chem.Int.Ed.Engl. 2022 PMID: 34783141
Wu A small molecule-controlled Cas9 repressible system. Mol.Ther.Nucleic Acids 2020 PMID: 32000033
Bafna Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture. Cell Rep. 2021 PMID: 33984267
Chung Tunable and reversible drug control of protein production via a self-excising degron. Nat.Chem.Biol. 2015 PMID: 26214256