Introduction：Basic information about CAS 147076-36-6|Laflunimus, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Laflunimus |
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| CAS Number | 147076-36-6 | Molecular Weight | 310.27100 |
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| Density | 1.441g/cm3 | Boiling Point | 408.7ºC at 760mmHg |
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| Molecular Formula | C15H13F3N2O2 | Melting Point | / |
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| MSDS | / | Flash Point | 201ºC |
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Names
| Name | (Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[3-methyl-4-(trifluoromethyl)phenyl]prop-2-enamide |
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| Synonym | More Synonyms |
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Laflunimus BiologicalActivity
| 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]. |
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| Related Catalog | Signaling Pathways >>Cell Cycle/DNA Damage >>DNA/RNA SynthesisSignaling Pathways >>GPCR/G Protein >>Prostaglandin ReceptorResearch Areas >>Inflammation/Immunology |
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| 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]. |
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| 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. |
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| References | [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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Chemical & Physical Properties
| Density | 1.441g/cm3 |
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| Boiling Point | 408.7ºC at 760mmHg |
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| Molecular Formula | C15H13F3N2O2 |
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| Molecular Weight | 310.27100 |
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| Flash Point | 201ºC |
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| Exact Mass | 310.09300 |
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| PSA | 73.12000 |
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| LogP | 3.77098 |
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| Vapour Pressure | 2.06E-07mmHg at 25°C |
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| Index of Refraction | 1.588 |
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Safety Information
Synonyms
