CS-1770

生物活性靶点体外研究体内研究 CS-1770 试剂级价格

CS-1770

CAS号:1040526-12-2
英文名:LP533401 hcl
中文名:CS-1770
CBNumber:CB82731287
分子式:C27H23ClF4N4O3
分子量:562.95
MOL File:1040526-12-2.mol

CS-1770化学性质

储存条件 :under inert gas (nitrogen or Argon) at 2-8°C
溶解度 :≥56.3 mg/mL in DMSO; insoluble in H2O; ≥19.4 mg/mL in EtOH
形态 :solid
颜色 :Light yellow to yellow

CS-1770性质、用途与生产工艺

生物活性 LP-533401 hydrochloride 是色氨酸羟化酶 1 (tryptophan hydroxylase 1) 抑制剂，可以调节肠道中血清素的产生。
靶点

Tryptophan hydroxylase 1
体外研究

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor. LP-533401 (1 μM) completely inhibits serotonin production in Tph1-expressing cells (RBL2H3 cells) after treatment for 3 days.
体内研究

Oral administration once daily for up to 6 weeks of LP-533401 (25, 100 or 250 mg/kg) dose-dependently prevents the development of and fully rescues, osteoporosis in ovariectomized rodents because of an isolated increase in bone formation. Pharmacokinetic studies in rodents show that LP-533401 level in the brain is negligible following oral administration, indicating that it is virtually unable to cross the blood-brain barrier. Mice treated repeatedly with LP-533401 (30-250 mg/kg per day) exhibit marked 5-HT content reductions in the gut, lungs, and blood, but not in the brain. After a single LP-533401 dose (250 mg/kg), lung and gut 5-HT contents decrease by 50%, whereas blood 5-HT levels remain unchanged, suggesting gut and lung 5-HT synthesis. Adult, healthy mice treated with the Tph-1 inhibitor LP-533401 show 30% decrease in circulating serotonin levels, with a consequent 30% increase in osteoblast numbers. Administration of LP-533401 to mice injected with EL4 cells inhibits the decrement in osteoblast numbers and trabecular bone volume, prolongs survial, and decreases leukemic infiltration.