产品属性:
产品名称 | 规格 | CAS号 | 型号 |
LX-1031 | 10mM (in 1mL DMSO) 5mg 25mg 100mg 250mg | 945976-76-1 | EY-Y0164383 |
Cas No.945976-76-1
别名 LX1031; LX 1031
化学名 (2S)-2-amino-3-[4-[2-amino-6-[(1R)-2,2,2-trifluoro-1-[4-(3-methoxyphenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoic acid
分子式 C28H25F3N4O4
分子量 538.52
溶解度 ≥ 26.9 mg/mL in DMSO
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. Serotonin plays important physiological roles both peripherally and centrally. LX-1031 is a heterocyclic substituted phenylalanine analog, an oral small molecule tryptophan hydroxylase (TPH) inhibitor that reduces synthesis of serotonin (5-HT) peripherally and is being developed for conditions characterized by excess 5-HT expression such as diarrhea-predominant irritable bowel syndrome (IBS-D) and, possibly, carcinoid diarrhea.
In vitro: LX-1031 inhibits TPH1 at its concentration of 10-8–10-7 mol L-1 range [1].
In vivo: With oral administration of LX-1031 in mice, the 5-HT reductions in the jejunum relative to control were ~33%, 51%, and 66% with the 15, 45 and 135 mg/kg/day doses, respectively; the effect of 5 mg/kg/day on GI 5-HT content was not significantly different from control [2].
Clinical trial: In double-blind studies (doses of LX-1031 ranging from 250 to 1000 mg q.i.d.), average 5HIAA reductions of 33% were noted. In phase I studies, 54 healthy volunteers received the drug for up to 14 days while the diet was strictly controlled to avoid 5-HT-rich foods. Twenty four hour urine collections were obtained. Significant reductions in urinary 5-HIAA persisted over the duration of exposure [3].
关键字: 945976-76-1;C28H25F3N4O4;LX-1031;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。
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