1. Anti-infection
  2. SARS-CoV Virus Protease
  3. ALG-097558

ALG-097558 is an orally active 3CLpro inhibitor. ALG-097558 demonstrates pan-coronavirus activity against various SARS-CoV-2 variants as well as other human coronaviruses (HCoVs) such as SARS-CoV-1, α-HCoV 229E, and β-HCoV OC43. ALG-097558 demonstrates potent inhibition with IC50s of 2 nM (SARS-CoV-2 3CLpro) and 6 nM (229E 3CLpro). ALG-097558 demonstrates antiviral activity in the SARS-CoV-2 hamster infection model. ALG-097558 can be used for the study of viral infections[1].

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ALG-097558 Chemical Structure

ALG-097558 Chemical Structure

CAS No. : 2892287-29-3

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Description

ALG-097558 is an orally active 3CLpro inhibitor. ALG-097558 demonstrates pan-coronavirus activity against various SARS-CoV-2 variants as well as other human coronaviruses (HCoVs) such as SARS-CoV-1, α-HCoV 229E, and β-HCoV OC43. ALG-097558 demonstrates potent inhibition with IC50s of 2 nM (SARS-CoV-2 3CLpro) and 6 nM (229E 3CLpro). ALG-097558 demonstrates antiviral activity in the SARS-CoV-2 hamster infection model. ALG-097558 can be used for the study of viral infections[1].

In Vitro

ALG-097558 (Compound 7) demonstrates potent inhibition with IC50s of 2 nM (SARS-CoV-2 3CLpro) and 6 nM (229E 3CLpro)[1].
ALG-097558 displays potent pan-coronavirus antiviral activity by strong inhibition of both the human β-CoV OC43 (EC50 = 8 nM), SARS-CoV-1 (EC50 = 22 nM) and B.1.1.7 AS49D (EC50 = 11 nM)[1].
ALG-097558 inhibits the 3CLpro activity of the β MERS-CoV (IC50 = 59 nM), hCoV OC43 (IC50 = 0.6 nM), α CoV 229E (IC50 = 2.8 nM), and γ Beluga whale CoV (IC50 = 1 nM)[1].
ALG-097558 (0-1 μM, 4 days) inhibits SARS-CoV-2 B.1.1.7 replication in primary human bronchial airway epithelial cells (HAEC) in an air-liquid interface culture[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[1]

Cell Line: Primary human bronchial airway epithelial cells
Concentration: 0-1 μM
Incubation Time: 4 days
Result: Inhibited SARS-CoV-2 replication with mean EC90, EC99, and EC99.9 values of 24, 36, and 43 nM respectively.
In Vivo

ALG-097558 (Compound 7) (2.5-150 mg/kg, p.o., twice a day, 3 days) demonstrates antiviral activity in the SARS-CoV-2 hamster infection model when co-administered with Ritonavir (HY-90001)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SARS-CoV-2 infected hamsters[1]
Dosage: 25, 50, 100, 150 mg/kg with Ritonavir (50 mg/kg) prophylactically (just before infection) or 2.5, 25, and 75 mg/kg with Ritonavir at 8 and 24 h postinfection (pi)
Administration: p.o. twice a day for 3 days
Result: Reduced lung infectious viral titer by more than four log10 TCID50/mg lung tissue when using a prophylactic dosing regimen.
Reduced the infectious virus loads in the lungs below or near the lower limit of quantification (10 TCID50mg lung tissue) in most animals when administered therapeutically starting from 8 h pi.
Reduced the infectious virus at doses of 25 and 75 mg/kg BID when administered therapeutically starting from 24 h pi.
Molecular Weight

540.00

Formula

C25H32ClF2N5O4

CAS No.
SMILES

[H][C@@]12[C@@H]3C=C[C@H]([C@@]1([C@H](N(C2)C([C@H](C(C)(C)C)NC(C(F)(Cl)F)=O)=O)C(N[C@@H](C[C@@H]4CCNC4=O)C#N)=O)[H])C3

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-175029
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