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1040526-12-2 | LP-533401 hydrochloride

LP-533401 hydrochloride NLT 98%

SKU : MC503735

CAS Number : 1040526-12-2

Molecular Formula : C27H23ClF4N4O3 | Molecular Weight : 562.94

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name LP-533401 hydrochloride
CAS Number 1040526-12-2
MDL Number MFCD18803629
Molecular Formula C27H23ClF4N4O3
Molecular Weight 562.94
Introduction of 1040526-12-2 :

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut. IC50 & Target: Tryptophan hydroxylase 1[1] In Vitro: 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[1]. In Vivo: 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[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 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[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 LP-533401 to mice injected with EL4 cells inhibits the decrement in osteoblast numbers and trabecular bone volume, prolongs survial, and decreases leukemic infiltration[3].

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