1. Metabolic Enzyme/Protease
  2. Dihydroorotate Dehydrogenase
  3. CHIKV-IN-2

CHIKV-IN-2 

Cat. No.: HY-132174
Handling Instructions

CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools.

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

CHIKV-IN-2 Chemical Structure

CHIKV-IN-2 Chemical Structure

CAS No. : 2361289-44-1

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Description

CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools[1].

IC50 & Target

EC90: 270 nM (Chikungunya virus)[1]
Dihydroorotate Dehydrogenase[1]

In Vitro

CHIKV-IN-2 (compound 8q) is a potent pan-alphavirus inhibitor, with EC90s of 0.85-2.5 μM for CHIKV clinical isolates and attenuated vaccine strains[1].
CHIKV-IN-2 is active against alphavirus VEEV (EC90=0.40 μM) as well as flaviviruses such as West Nile Virus (WNV, EC90=0.20 μM) and Dengue Virus Strain-2 (DENV-2, EC90=0.60 μM)[1].

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

In Vivo

CHIKV-IN-2 (compound 8q) (80 mg/kg; i.p. twice a day for 3 days) significantly decreases infectious CHIKV dissemination to other tissues of mice[1].
CHIKV-IN-2 (40 mg/kg; p.o., i.p., s.c.) exhibits moderate bioavailability (F=41%, 43%, 4%), terminal elimination half-life (t1/2=9.9, 18.5, 18.6 h) and Cmax (642, 858, 90 ng/mL) in mice[1].
CHIKV-IN-2 (1 mg/kg; i.v.) exhibits terminal elimination half-life (t1/2= 2.02 h) and AUC (497 h•ng/mL) in mice[1].

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

Animal Model: Female and male C57BL/6 mice[1]
Dosage: 80 mg/kg
Administration: I.p. twice a day for 3 days
Result: Failed to inhibit virus loads at the site of infection.
Decreased virus dissemination to other tissues.
Animal Model: Male C57BL/6 mice were challenged with CHIKV in the right footpad[1]
Dosage: 1 mg/kg for i.v. and 40 mg/kg for p.o., i.p., s.c. (Pharmacokinetic Analysis)
Administration: I.v., p.o., i.p., s.c.
Result: I.v.: t1/2= 2.02 h; AUC=497 h•ng/mL.
P.o.: F=41%; t1/2=9.9 h; Cmax=642 ng/mL.
I.p.: F=43%; t1/2=18.5 h; Cmax=858 ng/mL.
S.c.: F=4%; t1/2=18.6 h; Cmax=90 ng/mL.
Molecular Weight

362.46

Formula

C₂₃H₂₆N₂O₂

CAS No.
SMILES

O=C(NC1=CC=C(C(C)(C)C#N)C=C1)C2=CC3=C(CCCCC3)C=C2OC

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

CHIKV-IN-2Dihydroorotate DehydrogenaseDHODHChikungunyavirusCHIKVInhibitorinhibitorinhibit

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CHIKV-IN-2
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HY-132174
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