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Submit ReviewRo 61-8048
说明： Potent kynurenine 3-monooxygenase (KMO) inhibitor
化学名： 3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]benzenesulfonamide
纯度： ≥99% (HPLC)
生物活性 for Ro 61-8048
Ro 61-8048 is a potent and competitive kynurenine 3-monooxygenase (kynurenine 3-hydroxylase; KMO) inhibitor (Ki = 4.8 nM, IC50 = 37 nM). Increases kynurenic acid levels to concentrations that antagonize the glycine site of NMDA receptors. Brain penetrant and exhibits antidystonic, anticonvulsant and neuroprotective activities. Ro 61-8048 decreases nicotine self-administration in vivo. Ro 61-8048 prevents post-operative brain edema and consequent neuronal apoptosis in a rat model of surgically induced brain injury.
化合物库 for Ro 61-8048
Ro 61-8048 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Ro 61-8048
| 分子量 | 421.45 |
| 公式 | C17H15N3O6S2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 199666-03-0 |
| PubChem ID | 5282337 |
| InChI Key | NDPBMCKQJOZAQX-UHFFFAOYSA-N |
| Smiles | O=S(NC1=NC(C2=CC=CC([N+]([O-])=O)=C2)=CS1)(C3=CC=C(OC)C(OC)=C3)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Ro 61-8048
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 42.15 | 100 | |
| ethanol | 4.21 | 10 |
制备储备液 for Ro 61-8048
以下数据基于产品分子量 421.45。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.37 mL | 11.86 mL | 23.73 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.75 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.37 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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产品说明书 for Ro 61-8048
参考文献 for Ro 61-8048
参考文献是支持产品生物活性的出版物。
Rover et al (1997) Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high affinity inhibitors of kynurenine 3-hydroxylase. J.Med.Chem. 40 4378 PMID: 9435907
Carpenedo et al (2002) Kynurenine 3-mono-oxygenase inhibitors attenuate post-ischaemic neuronal death in organotypic hippocampal slice cultures. J.Neurochem. 82 1465 PMID: 12354294
Hamann et al (2008) Effects of kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dtsz mutant. Eur.J.Pharmacol. 586 156 PMID: 18353306
Justinova et al (2013) Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid. Nat.Neurosci. 16 1652 PMID: 24121737
Secci et al (2017) Attenuating nicotine reinforcement and relapse by enhancing endogenous brain levels of kynurenic acid in rats and squirrel monkeys. Neuropsychopharmacology 42 1619 PMID: 28139681
Zakhary et al (2020) Modification of kynurenine pathway via inhibition of kynurenine hydroxylase attenuates surgical brain injury complications in a male rat model. J Neurosci Res 98 155 PMID: 31257634
If you know of a relevant reference for Ro 61-8048, please let us know.
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关键词: Ro 61-8048, Ro 61-8048 supplier, Potent, kynurenine, 3-hydroxylase, inhibitors, inhibits, NMDA, antagonists, increases, kynurenic, acid, levels, Tryptophan, Hydroxylase, 11-β, 11-beta, LTB-omega-Hydroxylase, Kynurenine, 3-Hydroxylase, Hydroxylases, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotr, 3-monooxygenase, 3254, Tocris Bioscience
2 篇 Ro 61-8048 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Ro 61-8048 的部分引用包括：
Mailankot (2010) Induction of indoleamine 2,3-dioxygenase by IF.-gamma in human lens epithelial cells: apoptosis through the formation of 3-hydroxykynurenine. Int J Biochem Cell Biol 42 1446 PMID: 20435158
Gimenez-Gomez et al (2018) Increasing kynurenine brain levels reduces ethanol consumption in mice by inhibiting dopamine release in nucleus accumbens. Neuropharmacology. 135 581 PMID: 29705534
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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