WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522360
CAS#: 199666-03-0
Description: Ro61-8048 is a potent Kynurenine hydroxylase inhibitor (Ki = 4.8 nM, IC50 = 37 nM). Ro 61-8048 improves dystonia in a genetic model of paroxysmal dyskinesia. Ro 61-8048 may be potentially useful for the treatment of dyskinesias. Ro 61-8048 could be a new avenue to reduce neuronal loss in brain ischemia.
MedKoo Cat#: 522360
Name: Ro61-8048
CAS#: 199666-03-0
Chemical Formula: C17H15N3O6S2
Exact Mass: 421.04023
Molecular Weight: 421.44
Elemental Analysis: C, 48.45; H, 3.59; N, 9.97; O, 22.78; S, 15.21
Synonym: Ro61-8048; Ro 61-8048; Ro-61-8048; Ro618048; Ro 618048; Ro-618048
IUPAC/Chemical Name: 3,4-dimethoxy-N-(4-(3-nitrophenyl)thiazol-2-yl)benzenesulfonamide
InChi Key: NDPBMCKQJOZAQX-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H15N3O6S2/c1-25-15-7-6-13(9-16(15)26-2)28(23,24)19-17-18-14(10-27-17)11-4-3-5-12(8-11)20(21)22/h3-10H,1-2H3,(H,18,19)
SMILES Code: O=S(C1=CC=C(OC)C(OC)=C1)(NC2=NC(C3=CC=CC([N+]([O-])=O)=C3)=CS2)=O
Appearance: Light yellow solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 421.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Beconi MG, Yates D, Lyons K, Matthews K, Clifton S, Mead T, Prime M, Winkler D, O'Connell C, Walter D, Toledo-Sherman L, Munoz-Sanjuan I, Dominguez C. Metabolism and pharmacokinetics of JM6 in mice: JM6 is not a prodrug for Ro-61-8048. Drug Metab Dispos. 2012 Dec;40(12):2297-306. doi: 10.1124/dmd.112.046532. Epub 2012 Aug 31. PubMed PMID: 22942319.
2: Yang J, Li W, Zhou Z, Yang C. Is Ro 61-8048 a potential fast-acting antidepressant? J Neurol Sci. 2012 Apr 15;315(1-2):180; author reply 181-2. doi: 10.1016/j.jns.2011.11.037. Epub 2011 Dec 12. PubMed PMID: 22169632.
3: Ouattara B, Belkhir S, Morissette M, Dridi M, Samadi P, Grégoire L, Meltzer LT, Di Paolo T. Implication of NMDA receptors in the antidyskinetic activity of cabergoline, CI-1041, and Ro 61-8048 in MPTP monkeys with levodopa-induced dyskinesias. J Mol Neurosci. 2009 Jun;38(2):128-42. doi: 10.1007/s12031-008-9137-8. Epub 2008 Aug 14. PubMed PMID: 18704766.
4: Hamann M, Sander SE, Richter A. Effects of the kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt sz mutant. Eur J Pharmacol. 2008 May 31;586(1-3):156-9. doi: 10.1016/j.ejphar.2008.02.052. Epub 2008 Feb 29. PubMed PMID: 18353306.
5: Richter A, Hamann M. The kynurenine 3-hydroxylase inhibitor Ro 61-8048 improves dystonia in a genetic model of paroxysmal dyskinesia. Eur J Pharmacol. 2003 Sep 30;478(1):47-52. PubMed PMID: 14555184.
6: Chiarugi A, Moroni F. Quinolinic acid formation in immune-activated mice: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[-N-4-(-3-nitrophenyl)thiazol-2yl]-benzenesul fonamide (Ro 61-8048), two potent and selective inhibitors of kynurenine hydroxylase. Neuropharmacology. 1999 Aug;38(8):1225-33. PubMed PMID: 10462134.
7: Cozzi A, Carpenedo R, Moroni F. Kynurenine hydroxylase inhibitors reduce ischemic brain damage: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[-N-4-(nitrophenyl)thiazol-2yl]-benzenesulfonamide (Ro 61-8048) in models of focal or global brain ischemia. J Cereb Blood Flow Metab. 1999 Jul;19(7):771-7. PubMed PMID: 10413032.
