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LP533401 hclTph-1 inhibitor

LP533401 hcl

Catalog No. B5823
Size Price Stock
5mg $350.00 Please Inquire
25mg $900.00 Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

LP533401 hcl

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Chemical Properties

Cas No. 1040526-12-2 SDF Download SDF
Chemical Name (2S)-2-amino-3-(4-(2-imino-6-(2,2,2-trifluoro-1-(3'-fluoro-[1,1'-biphenyl]-4-yl)ethoxy)-2,3-dihydropyrimidin-4-yl)phenyl)propanoic acid hydrochloride
Canonical SMILES FC1=CC=CC(C2=CC=C(C(OC(C=C(N3)C4=CC=C(C[C@@](N)([H])C(O)=O)C=C4)=NC3=N)([H])C(F)(F)F)C=C2)=C1.Cl
Formula C27H23ClF4N4O3 M.Wt 562.94
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.