生物活性
LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
体内研究
(In Vivo)
With oral administration of LX-1031 in mice, the average 5-HT reductions in the jejunum relative to control are appr 33, 51, and 66% with the 15, 45 and 135 mg/kg/day doses respectively. In a preliminary report, the effects of LX-1031, 100 mg/kg daily, on 5-HT levels in jejunal mucosa are reversible within 2 days of discontinuation in mice[1]. LX-1031 dose-dependently reduces expression of 5-HT in the duodenum, jejunum and ileum, but has no effect on brain 5-HT levels in preclinical assay[2].
分子量
538.52
性状
Solid
Formula
C28H25F3N4O4
CAS 号
945976-76-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : ≥ 34 mg/mL (63.14 mM)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 1.8569 mL 9.2847 mL 18.5694 mL
5 mM 0.3714 mL 1.8569 mL 3.7139 mL
10 mM 0.1857 mL 0.9285 mL 1.8569 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: