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  2. HCV
  3. L0909

L0909 is an HCV inhibitor with an EC50 of 0.022 μM. L0909 blocks HCV replication by inhibiting E1-mediated viral entry. L0909 exhibits sensitivity to clinical resistant HCV mutants. L0909 displays synergistic effects with clinical HCV drugs. L0909 can be used for the research of hepatitis c virus (HCV) infection.

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L0909

L0909 Chemical Structure

CAS No. : 2085271-43-6

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Description

L0909 is an HCV inhibitor with an EC50 of 0.022 μM. L0909 blocks HCV replication by inhibiting E1-mediated viral entry. L0909 exhibits sensitivity to clinical resistant HCV mutants. L0909 displays synergistic effects with clinical HCV drugs. L0909 can be used for the research of hepatitis c virus (HCV) infection[1].

In Vitro

L0909 (72 h) potently inhibits HCV RNA replication in Huh7.5 cells (CC50 = 14.77 μM) with an EC50 of 0.022 μM[1].
L0909 (-chloro) (72 h) potently inhibits HCV replication in Huh7.5 cells (CC50 = 12.761 μM) with an EC50 of 0.083 μM and a selectivity index of 154[1].
L0909 (0.1-5 μM; 3-14 days) does not inhibit HCV replication in replicon GS4.3 cells[1].
L0909 (0.3125-12.5 μM; 4-72 h) blocks HCV entry into Huh7.5 cells, exhibiting potent, rapid, and broad-spectrum activity against both genotype 1b and 2a HCV pseudoparticles and replicating virus[1].
L0909 inhibits HCV entry via targeting the HCV E1 glycoprotein, as evidenced by the F291V E1 mutation conferring ~20-fold resistance to the compound in Huh7.5 cells[1].
L0909 (serial dilutions; 72 h) retains potent, nanomolar activity against drug-resistant HCV variants (A156T, D168V, S282T) in Huh7.5 cells, similar to its activity against wild-type HCV[1].

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

Real Time qPCR[1]

Cell Line: Wild-type and drug-resistant HCV mutants (A156T NS3, D168V NS3, S282T NS5B)-infected Huh7.5 cells
Concentration: Serial dilutions
Incubation Time: 72 h
Result: Maintained potent activity against all tested drug-resistant mutants: EC50 = 0.0019 μM (A156T NS3), 0.03 μM (D168V NS3), 0.0044 μM (S282T NS5B), compared to an EC50 of 0.003 μM against wild-type HCV.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax Vz CL F
Rat[1] 5 mg/kg i.v. 14.34 h / 616.99 ng/mL 20057.05 mL/kg 1088.11 mL/h/kg /
Rat[1] 15 mg/kg p.o. 12.83 h 3.08 h 500.72 ng/mL 34834.07 mL/kg 2246.3 mL/h/kg 59 %
Dog[1] 5 mg/kg i.v. 7.28 h / 531.93 ng/mL 49181.42 mL/kg 4752.98 mL/h/kg /
Dog[1] 15 mg/kg p.o. 12.72 h 3 h 94.51 ng/mL 238116.97 mL/kg 12025.86 mL/h/kg 39 %
In Vivo

L0909 (250-1000 mg/kg; i.g.,; single dose) has an oral maximal tolerated dose above 1000 mg/kg in Kunming mice, with no observed mortality, body weight changes, or liver/kidney function abnormalities over 7 days[1].

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

Animal Model: Kunming mice (male and female, 3 each per group)[1]
Dosage: 250 mg/kg; 500 mg/kg; 1000 mg/kg
Administration: p.o.; single dose
Result: Showed no mortality across all treatment groups over 7 days.
Detected no significant changes in body weight compared to the control group.
Found no significant abnormalities in blood AST, ALT, UREA, or CRE levels at any tested dose, including 1000 mg/kg.
Molecular Weight

411.97

Formula

C23H30ClN5

CAS No.
SMILES

N#CC1=CC=C(N(CCN(C)C)C)C=C1CN2CCN(CC2)C3=CC=C(C=C3)Cl

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Storage

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

Purity & Documentation
References
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  • 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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L0909
Cat. No.:
HY-182679
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