LP533401 hcl |
| Katalog-Nr.GC13293 |
LP533401 hcl ist ein Tryptophan-Hydroxylase-1-Inhibitor, der die Serotoninproduktion im Darm reguliert.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1040526-12-2
Sample solution is provided at 25 µL, 10mM.
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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.
Animal experiment: | Mice[1]Mice are treated from day 1 post-ovariectomy for 4 weeks with LP-533401 (1, 10, 100 or 250 mg per kg body weight per day) or vehicle. Next mice are treated for 4 weeks starting 2 weeks post-ovariectomy with LP-533401 (250 mg per kg body weight per day) or vehicle. lastly, mice are treated for 6 weeks starting 6 weeks post-ovariectomy with LP-533401 (25, 100 or 250 mg per kg body weight per day) or vehicle[1]. |
References: [1]. Yadav, V.K., et al. Inhibition of gut-derived serotonin synthesis: A potential bone anabolic treatment. Nat. Med. 16(3), 308-312 (2010). | |
| Cas No. | 1040526-12-2 | 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 |
| Löslichkeit | ≥ 56.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7764 mL | 8.8819 mL | 17.7639 mL |
| 5 mM | 0.3553 mL | 1.7764 mL | 3.5528 mL |
| 10 mM | 0.1776 mL | 0.8882 mL | 1.7764 mL |
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Quality Control & SDS
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- Purity: >98.50%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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