LP 533401
LP 533401 Basic information
- Product Name:
- LP 533401
- Synonyms:
-
- LP 533401
- 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]-
- LP 533401; LP533401
- (2S)-2-amino-3-[4-[2-amino-6-[2,2,2-trifluoro-1-[4-(3-fluorophenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoic acid
- CS-2152
- LP-533401 (free base)
- (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
- CAS:
- 945976-43-2
- MF:
- C27H22F4N4O3
- MW:
- 526.48
- Mol File:
- 945976-43-2.mol
LP 533401 Chemical Properties
- Boiling point:
- 699.0±65.0 °C(Predicted)
- Density
- 1.388±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 10 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml; DMSO: 5 mg/ml
- form
- A crystalline solid
- pka
- 2.04±0.10(Predicted)
- color
- Brown to breen
LP 533401 Usage And Synthesis
Uses
LP 533401 inhibits tryptophan hydroxylase 1 (Tph1) which is the rate-limiting enzyme responsible for serotonin production.
in vivo
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[1]. 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[2]. 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[3].
LP 533401Supplier
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- 18210857532; 18210857532
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