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Laflunimus

Catalog No. T11813   CAS 147076-36-6
Synonyms: HR325

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. Laflunimus is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH).

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Laflunimus Chemical Structure
Laflunimus, CAS 147076-36-6
Pack Size Availability Price/USD Quantity
5 mg 6-8 weeks $ 247.00
25 mg 6-8 weeks $ 766.00
50 mg 6-8 weeks $ 996.00
100 mg 6-8 weeks $ 1,490.00
1 mL * 10 mM (in DMSO) 6-8 weeks $ 272.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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. Laflunimus is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH).
In vitro Laflunimus inhibits LPS-induced kappa light-chain cell surface expression on 70Z/3 cells, a property also reversed by uridine. Laflunimus 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).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.
In vivo HR325?inhibits the secondary anti-sheep red blood cell (SRBC) antibody response with ID50 values of 38 mg/kg.
Synonyms HR325
Molecular Weight 310.27
Formula C15H13F3N2O2
CAS No. 147076-36-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Thomson TA, et al. In vitro and in Vivo inhibition of immunoglobulin secretion by the immunosuppressive compound HR325 is reversed by exogenous uridine. Scand J Immunol. 2002 Jul;56(1):35-42. 2. Curnock AP, et al. Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti-inflammatory drugs. J Pharmacol Exp Ther. 1997 Jul;282(1):339-47.

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Keywords

Laflunimus 147076-36-6 Others HR-325 HR 325 HR325 inhibitor inhibit

 

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