| Identification | Back Directory | [Name]
LP533401 hcl | [CAS]
1040526-12-2 | [Synonyms]
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 | [Molecular Formula]
C27H23ClF4N4O3 | [MDL Number]
MFCD18803629 | [MOL File]
1040526-12-2.mol | [Molecular Weight]
562.95 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
≥56.3 mg/mL in DMSO; insoluble in H2O; ≥19.4 mg/mL in EtOH | [form ]
solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Biological Activity]
lp533401 hcl is an inhibitor of tph-1 [1].tryptophan hydroxylase-1 (tph-1) is an isoenzyme of tryptophan hydroxylase and the initial enzyme in gut- and lung-derived serotonin biosynthesis. tph-1 is mainly expressed in the gut and lung [2].lp533401 hcl is a tph-1 inhibitor. in rat rbl2h3 cells expressing tph1, lp533401 (1 μm) completely inhibited serotonin production. lp533401 reduced the activity of recombinant wild-type tph-1 by 70% by interacting with residues tyr235 and phe241 [1].in rodents, lp533401 orally administration was incapable of crossing the blood-brain barrier. in mice, lp533401 (250 mg/kg) dose-dependently reduced serum serotonin concentration by 30%. in ovariectomized female c57bl6/j mice, lp533401 (10, 100, 250 mg/kg for 28 days) increased bone mass and bone-formation parameters such as osteocalcin serum concentration, osteoblast numbers and bone formation rate. also, lp533401 dose-dependently decreased serum serotonin concentration but didn’t affect brain serotonin content. in ovariectomized female rats, lp533401 completely rescued the ovariectomy-induced osteopenia [1]. in transgenic sm22-5-htt+ mice overexpressing 5-ht transporter (5-htt) in smooth muscle cells and spontaneously developing pulmonary hypertension (ph), lp533401 (250 mg/kg for 21 days) significantly reduced lung and blood 5-ht levels, vascular ki67-positive cells, distal pulmonary artery muscularization, right ventricular (rv) hypertrophy and rv systolic pressure [2]. | [References]
[1]. yadav vk, balaji s, suresh ps, et al. pharmacological inhibition of gut-derived serotonin synthesis is a potential bone anabolic treatment for osteoporosis. nat med, 2010, 16(3): 308-312.
[2]. abid s, houssaini a, chevarin c, et al. inhibition of gut- and lung-derived serotonin attenuates pulmonary hypertension in mice. am j physiol lung cell mol physiol, 2012, 303(6): l500-508. |
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Twochem Co.Ltd.
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021-58111628 15800915896 |
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cn.twochem.com |
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Cckinase, Inc.
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www.cckinase.com |
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