TelotriSTAT ethyl 是一种口服具有活力的色氨酸羟化酶抑制剂,可抑制血清素的产生。
产品描述
Telotristat ethyl is a orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
体内活性
Telotristat ethyl (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation[1]. Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. However, Telotristat ethyl (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT) nor alter constitutive gastrointestinal motility in mice. Telotristat ethyl (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis[2]. Telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery but not in the brain of the mice. Telotristat ethyl (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease.
Cas No.
1033805-22-9
分子式
C27H26ClF3N6O3
分子量
574.98
别名
LX1606
储存和溶解度
DMSO:98.5 mg/mL (171.31mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years