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Ro 61-8048 

Cat. No.: HY-12347 Purity: 99.90%
Handling Instructions

Ro 61-8048 is an orally active and selective inhibitor of kynurenine 3-hydroxylase, with an IC50 of 37 nM. Ro 61-8048 provokes a significant increase of extracellular kynurenic acid concentrations.

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

Ro 61-8048 Chemical Structure

Ro 61-8048 Chemical Structure

CAS No. : 199666-03-0

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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 73 In-stock
Estimated Time of Arrival: December 31
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5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 88 In-stock
Estimated Time of Arrival: December 31
50 mg USD 242 In-stock
Estimated Time of Arrival: December 31
100 mg USD 385 In-stock
Estimated Time of Arrival: December 31
200 mg USD 715 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Ro 61-8048

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  • Customer Review

Description

Ro 61-8048 is an orally active and selective inhibitor of kynurenine 3-hydroxylase, with an IC50 of 37 nM. Ro 61-8048 provokes a significant increase of extracellular kynurenic acid concentrations[1].

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[1].
Ro 61-8048 (0.1-100 μM) strongly reduces QUIN neo-formation, suggesting that, in vitro, kynurenine hydroxylase activity is required for QUIN neosynthesis[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[2].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female dtsz mutant Syrian golden hamsters[2].
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. A delayed 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.
Molecular Weight

421.45

Formula

C17H15N3O6S2

CAS No.
SMILES

O=S(C1=CC=C(OC)C(OC)=C1)(NC2=NC(C3=CC=CC([N+]([O-])=O)=C3)=CS2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 59 mg/mL (139.99 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3728 mL 11.8638 mL 23.7276 mL
5 mM 0.4746 mL 2.3728 mL 4.7455 mL
10 mM 0.2373 mL 1.1864 mL 2.3728 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  50% PEG300    50% saline

    Solubility: 20 mg/mL (47.46 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.93 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MCE.
References
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Product Name:
Ro 61-8048
Cat. No.:
HY-12347
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