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1040526-12-2

中文名称 CS-1770
英文名称 LP533401 hcl
CAS 1040526-12-2
分子式 C27H23ClF4N4O3
分子量 562.95
MOL 文件 1040526-12-2.mol
1040526-12-2 结构式 1040526-12-2 结构式

基本信息

中文别名
LP-533401盐酸盐
英文别名
CS-1770
LP533401 hcl
LP-533401 hydrochloride
L-?Phenylalanine, 4-?[2-?amino-?6-?[2,?2,?2-?trifluoro-?1-?(3'-?fluoro[1,?1'-?biphenyl]?-?4-?yl)?ethoxy]?-?4-?pyrimidinyl]?-?, hydrochloride (1:1)
L-phenylalanine, 4-[2-amino-6-[2,2,2-trifluoro-1-(3'-fluoro[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-, Hydrochloride (1:1) LP533401 hcl
所属类别
生物化工:激动剂抑制剂

物理化学性质

储存条件Inert atmosphere,2-8°C
溶解度≥56.3 mg/mL in DMSO; insoluble in H2O; ≥19.4 mg/mL in EtOH
形态固体

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335
CS-1770价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-15849ACS-1770
LP-533401 hydrochloride
1040526-12-21 mg400元
2024/04/30HY-15849ACS-1770
LP-533401 hydrochloride
1040526-12-25mg1000元
2024/04/30HY-15849ACS-1770
LP-533401 hydrochloride
1040526-12-210mM * 1mLin DMSO1238元

常见问题列表

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.

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