CS-1770
中文名称 | CS-1770 |
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中文同义词 | LP-533401盐酸盐;化合物 T15779 |
英文名称 | LP533401 hcl |
英文同义词 | 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;LP533401 hcl;LP-533401 hydrochloride;CS-1770;L-?Phenylalanine, 4-?[2-?amino-?6-?[2,?2,?2-?trifluoro-?1-?(3'-?fluoro[1,?1'-?biphenyl]?-?4-?yl)?ethoxy]?-?4-?pyrimidinyl]?-?, hydrochloride (1:1);LP 533401 hydrochloride,LP533401 hydrochloride;(2S)-2-Amino-3-(4-(2-amino-6-(2,2,2-trifluoro-1-(3'-fluoro-[1,1'-biphenyl]-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid hydrochloride |
CAS号 | 1040526-12-2 |
分子式 | C27H23ClF4N4O3 |
分子量 | 562.95 |
EINECS号 | |
相关类别 | 抑制剂 |
Mol文件 | 1040526-12-2.mol |
结构式 |
CS-1770 性质
储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
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溶解度 | DMSO 中≥56.3 mg/mL;不溶于水;乙醇中≥19.4 mg/mL |
形态 | 固体 |
颜色 | 浅黄至黄色 |
Tryptophan hydroxylase 1
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-15849A | CS-1770 LP-533401 hydrochloride | 1040526-12-2 | 1 mg | 400元 |
2024/08/19 | HY-15849A | CS-1770 LP-533401 hydrochloride | 1040526-12-2 | 5mg | 1000元 |