1. Metabolic Enzyme/Protease
    Cell Cycle/DNA Damage
    GPCR/G Protein
  2. Dihydroorotate Dehydrogenase
    DNA/RNA Synthesis
    Prostaglandin Receptor
  3. Laflunimus

Laflunimus (Synonyms: HR325)

Cat. No.: HY-101813
Handling Instructions

Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.

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

Laflunimus Chemical Structure

Laflunimus Chemical Structure

CAS No. : 147076-36-6

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Description

Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor[1][2].

In Vitro

Ig secretion from mouse splenocytes was induced by lipopolysaccharide (LPS) for 5 days. Laflunimus inhibited the secretion of IgM and IgG with IC50 values of 2.5 and 2 µM , respectively. Adding Uridine (50 µ M) increased these values to 70 and 60 µ M, respectively. Laflunimus inhibits LPS-induced kappa light-chain cell surface expression on 70Z/3 cells, a property also reversed by uridine[1].
Laflunimus (HR325) is more potent than A77 1726 as an inhibitor of PGHS in guinea pig polymorphonuclear leukocytes (IC50= 415 and 4400 nM, respectively) and on isolated ovine PGHS-1 (IC50=64 and 742 µM) and PGHS-2 (IC50=100 and 2766 µM)[2].

In Vivo

HR325 (50 mg/kg; p.o.; days 14-18 after being injected with SRBC) inhibits the secondary anti-sheep red blood cell (SRBC) antibody response with ID50 values of 38 mg/kg[1].

Animal Model: Male CD-1 mice (20-24 g)[1]
Dosage: 50 mg/kg
Administration: Oral; days 14-18 after being injected with SRBC
Result: The level of circulating anti-SRBC IgG in this model was inhibited dose relatedly by orally administered HR325.
Molecular Weight

310.27

Formula

C₁₅H₁₃F₃N₂O₂

CAS No.

147076-36-6

SMILES

O=C(NC1=CC=C(C(F)(F)F)C(C)=C1)/C(C#N)=C(C2CC2)\O

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

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Keywords:

LaflunimusHR325HR 325HR-325Dihydroorotate DehydrogenaseDNA/RNA SynthesisProstaglandin ReceptorDHODHimmunomodulatoranti-inflammatoryimmunoglobulinIgGLPSsheepredbloodcellsecretionInhibitorinhibitorinhibit

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Laflunimus
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