Rodatristat (Synonyms: KAR5417)
目录号: PL12483
CAS No. :1673568-73-4
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中文名称
Rodatristat
英文名称
Rodatristat
英文别名
Rodatristat;KAR5417;Rodatristat (USAN);Rodatristat [USAN];91D8378G2V;(3~{s})-8-[2-Azanyl-6-[(1~{r})-1-(4-Chloranyl-2-Phenyl-Phenyl)-2,2,2-Tris(Fluoranyl)ethoxy]pyrimidin-4-Yl]-2,8-Diazaspiro[4.5]decane-3-Carboxylic Acid;(S)-8-(2-amino-6-((R)-1-(5-chloro-[1,1'-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylic acid;GTPL10647;BDBM50233990;compound 15a [PMID: 28041831]
Cas No.
1673568-73-4
分子式
C27H27ClF3N5O3
分子量
561.98
包装储存
Please store the product under the recommended conditions in the Certificate of Analysis.
产品详情
Rodatristat (KAR5417) 是一种有效的 tryptophan hydroxylase 1 (TPH1) 和 TPH2 抑制剂,其 IC50 值分别为 33 nM 和 7 nM,并显著降低小鼠肠道中的血清素 (5-HT) 水平。
生物活性
Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) and TPH2 inhibitor with IC 50 s value of 33 nM and 7 nM, respectively, and shows robust reduction of intestinal serotonin (5-HT) levels in mice.
IC50 & Target[1][2]
serotonin TPH1 33 nM (IC50)
体内研究(In Vivo)
Rodatristat (10-50 mg/kg; oral administration; mice) treatment decreases intestinal 5-HT concentrations at 50 mg/kg, their efficacy drop off significantly at the lower 10 mg/kg dose. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
ClinicalTrial
参考文献
[1]. Goldberg DR, et al. Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors. Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419.
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