An SPR inhibitor (IC50s = 62 and 14 nM for the recombinant human and rat enzymes

SPRi 3 – 5 mg

Brand:
Cayman
CAS:
1292285-54-1
Storage:
-20
UN-No:
Non-Hazardous - /

SPRi 3 is an inhibitor of sepiapterin reductase (SPR), an enzyme that catalyzes the formation of tetrahydrobiopterin (BH4), with IC50 values of 62 and 14 nM for the recombinant human and rat enzymes, respectively.{57061} It is selective for SPR over GTP cyclohydroxylase 1 (GCH1) in primary mouse dorsal root ganglia sensory neurons at 10 µM.{57062} SPRi 3 (50 µM) inhibits proliferation of anti-CD3 and anti-CD28 antibody-stimulated isolated human peripheral blood mononuclear cells (PBMCs) or CD4+ T cells.{57063} Intraperitoneal administration of SPRi 3 (300 mg/kg) decreases brain BH4 levels and reduces mechanical allodynia in mouse models of peripheral neuropathy induced by spared nerve injury (SNI) or chronic constriction injury (CCI).{57062} It also decreases macrophage infiltration and thermal hyperalgesia in the inflamed joints of a mouse model of rheumatoid arthritis induced by complete Freund’s adjuvant (CFA) at the same dose.  

 

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Description

An SPR inhibitor (IC50s = 62 and 14 nM for the recombinant human and rat enzymes, respectively); is selective for SPR over GCH1 in primary mouse dorsal root ganglia sensory neurons at 10 µM; inhibits proliferation of anti-CD3 and anti-CD28 antibody-stimulated isolated human PBMCs or CD4+ T cells at 50 µM; decreases brain BH4 levels and reduces mechanical allodynia in mouse models of peripheral neuropathy induced by SNI or CCI at 300 mg/kg; decreases macrophage infiltration and thermal hyperalgesia in the inflamed joints of a mouse model of rheumatoid arthritis induced by CFA at 300 mg/kg

Formal name: N-[2-(5-hydroxy-2-methyl-1H-indol-3-yl)ethyl]-2-methoxy-acetamide

Synonyms: 

Molecular weight: 262.3

CAS: 1292285-54-1

Purity: ≥98%

Formulation: A solid

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