產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
LP533401 hcl | 5mg 10mg 25mg 50mg 100mg | 1040526-12-2 | EY-Y0164380 |
Cas No.1040526-12-2
別名 N/A
化學名 (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
分子式 C27H23ClF4N4O3
分子量 562.94
溶解度 ≥ 56.3mg/mL in DMSO
儲存條件 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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
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.
關鍵字： 1040526-12-2;C27H23ClF4N4O3;LP533401 hcl;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務于科研工作者""的企業(yè)理念，立足生物科技領域，運用生物技術和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務生物科技領域的科學研究人員。
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