Ro 61-8048

SKU: orb1225760

Description

Ro 61-8048 is a potent and selective inhibitors of kynurenine hydroxylase with IC50 of 37 nM.

Key Properties

• CAS Number: 199666-03-0
• MW: 421.45
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₅N₃O₆S₂
• SMILES: COC1=C(OC)C=C(C=C1)S(=O)(=O)NC1=NC(=CS1)C1=CC(=CC=C1)[N+]([O-])=O
• Target: Hydroxylase
• Solubility: DMSO: 59 mg/mL

Bioactivity

• In Vivo:
  Ro 61-8048 (50, 100 and 150 mg/kg i.p.) significantly reduces the severity of dystonia in dtsz hamsters without leading to marked central side effects. Ro 61-8048 (100 mg/kg i.p.) provokes a two-to threefold increase of the endogeneous broad spectrum glutamate receptor antagonist kynurenic acid in the striatum, cerebellum and brainstem of mutant hamsters. Animal model: Male and female dtsz mutant Syrian golden hamsters. Dosage: 50, 100 and 150 mg/kg. Administration: i.p. , one dose. Result: Significantly reduced the individual maximum severity of dystonia reached at the end of the observation period of 3 h at doses of 50, 100 and 150 mg/kg i.p.. 100 and 150 mg/kg significantly decreased the severity, indicating a fast onset of action. Adelayed onset of dystonic attacks was observed after treatment with 150 mg/kg but not after administration of 50 and 100 mg/kg. At lower doses of 10 and 25 mg/kg, the compound failed to exert any antidystonic effects. Caused a moderate sedation and hypolocomotion 5 to 70 min after administration of 100 and 150 mg/kg, while no central adverse effects were observable at a dose of 50 mg/kg or lower doses.
• In Vitro:
  In gerbils, a dose of 30 μmol/kg po (12.64 μg/kg Ro 61-8048, compound 16) leads to inhibition of the cerebral enzyme which peaked after 2h (~85% inhibition) and persisted for up to 8 h. Ro 61-8048 (0.1-100 μM) strongly reduces QUIN neo-formation, suggesting that, in vitro, kynurenine hydroxylase activity is required for QUIN neosynthesis.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Hydroxylase