中文名称: | L-苯丙氨酸,4 [ 2-AMINO-6 -(3 - [ 2,2,2 -三氟-1 -氟[ 1,1'-联苯-4-乙氧基])] - 4-PYRIMIDINYL ]— | ||||
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英文名称: | LP 533401 | ||||
别名: | L-苯丙氨酸,4[2-AMINO-6-(3-[2,2,2-三氟-1-氟[1,1'-联苯-4-乙氧基])]-4-PYRIMIDINYL]—;色氨酸羟化酶1抑制剂(LP-533401);化合物T15778;(2S)-2-氨基-3-(4-(2-氨基-6-(2,2,2-三氟-1-(3'-氟-[1,1'-二苯基]-4-基)乙氧基)嘧啶-4-基)苯基)丙酸 LP-533401/L-Phenylalanine,4-[2-amino-6-[2,2,2-trifluoro-1-(3'-fluoro[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-;L-Phenylalanine,4-[2-amino-6-[2,2,2-trifluoro-1-(3\'-fluoro[1,1\'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-;LP533401;LP533401;(2S)-2-amino-3-[4-[2-amino-6-[2,2,2-trifluoro-1-[4-(3-fluorophenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoicacid | ||||
CAS No: | 945976-43-2 | 分子式: | C27H22F4N4O3 | 分子量: | 526.48 |
CAS No: | 945976-43-2 | ||||
分子式: | C27H22F4N4O3 | ||||
分子量: | 526.48 |
沸点:
699.0±65.0 °C(Predicted)
密度:
1.388±0.06 g/cm3(Predicted)
包装规格:
1mg 5mg 25mg in glass bottle
产品简介:
LP-533401是调节肠道内5-羟色胺产生的色氨酸羟化酶1抑制剂。
储备液保存:
-80°C 2 years
-20°C 1 year
-20°C 1 year
靶点:
Tryptophan hydroxylase
体外研究:
LP-533401 completely inhibits serotonin production in Tph1–expressing cells (RBL2H3 cells) at a dose of 1 μM.
体内研究:
Oral administration once daily for up to 6 weeks of this small molecule prevents the development of and fully rescues, in a dose-dependent manner, 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 LP533401 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 LP533401 to mice injected with EL4 cells inhibits the decrement in osteoblast numbers and trabecular bone volume, prolongs survial, and decreases leukemic infiltration.
保存条件:
2-8°C
注意事项:
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2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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