1. Anti-infection Cell Cycle/DNA Damage
  2. Influenza Virus DNA/RNA Synthesis
  3. KJ001-12a

KJ001-12a is an orally active anti-influenza agent with activity against influenza A and B strains. KJ001-12a acts as an RNA-dependent RNA polymerase inhibitor that reduces the expression levels of viral M2 mRNA and vRNA. KJ001-12a shows low sensitivity to the loss of inhibitory activity caused by the I38T mutation. KJ001-12a is applicable for influenza-related research.

For research use only. We do not sell to patients.

KJ001-12a

KJ001-12a Chemical Structure

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Description

KJ001-12a is an orally active anti-influenza agent with activity against influenza A and B strains. KJ001-12a acts as an RNA-dependent RNA polymerase inhibitor that reduces the expression levels of viral M2 mRNA and vRNA. KJ001-12a shows low sensitivity to the loss of inhibitory activity caused by the I38T mutation. KJ001-12a is applicable for influenza-related research[1].

IC50 & Target[1]

RNA Polymerase

 

In Vitro

KJ001-12a potently inhibits influenza A/PR/8/34 (H1N1) replication in MDCK cells with an IC50 of 1.9 nM and a high selectivity index of 6436.8[1].
KJ001-12a (72 h) inhibits replication of multiple influenza A and B strains in MDCK cells, with IC50 values ranging from 15.56 nM to 59.26 nM and a consistent TC50 of 12.23 μM[1].
KJ001-12a inhibits influenza A/PR/8/34 (WT) replication in MDCK cells with an IC50 of 25.72 nM, and its activity is reduced only 9.36-fold against the I38T mutant strain[1].
KJ001-12a (0.2 nM; 24 h) significantly inhibits influenza A/PR/8/34 (H1N1) M2 mRNA expression in MDCK cells, achieving a 76.72% inhibition rate[1].
KJ001-12a (1-10 nM) dose-dependently inhibits influenza A virus RdRp activity in 293T cells, achieving 45.6% inhibition at 10 nM[1].

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

Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t CL F
Rat[1] 1.00 mg/kg i.v. 1.90 h 0.08 h 291.94 ng/mL 359.16 ng·h/mL 369.73 ng·h/mL 1.41 h 2718.58 mL/h/kg /
Rat[1] 5.00 mg/kg p.o. 0.94 h 1.00 h 256.10 ng/mL 722.77 ng·h/mL 726.46 ng·h/mL 1.80 h / 40.25 %
In Vivo

KJ001-12a (1-5 mg/kg; i.v., p.o.; single dose) exhibits an absolute oral bioavailability of 40.25% in male Sprague-Dawley rats, with favorable pharmacokinetic parameters after single intravenous and oral doses[1].

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

Molecular Weight

463.43

Formula

C25H19F2N3O4

SMILES

O=C1N2[C@](COCC2)([H])N(C3C4=CC=C(F)C=C4C=CC5=CC(F)=CC=C35)N6C1=C(O)C(C=C6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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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Product Name:
KJ001-12a
Cat. No.:
HY-184289
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