| Company Name: |
Shanghai Balmxy Pharmaceutical Co., Ltd
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021-24206007 13764915196 |
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sales@balmxy.com |
| Products Intro: |
Product Name:LP-533401HCl
CAS:1040526-12-2
Purity:98%+ Package:5g;25g;100g;500g;1kg;5kg;25kg;100kg Remarks:BX60005
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| | LP533401 hcl Basic information |
| Product Name: | LP533401 hcl | | Synonyms: | 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;LP533401 hcl;LP-533401 hydrochloride;CS-1770;L-?Phenylalanine, 4-?[2-?amino-?6-?[2,?2,?2-?trifluoro-?1-?(3'-?fluoro[1,?1'-?biphenyl]?-?4-?yl)?ethoxy]?-?4-?pyrimidinyl]?-?, hydrochloride (1:1);LP 533401 hydrochloride,LP533401 hydrochloride;(2S)-2-Amino-3-(4-(2-amino-6-(2,2,2-trifluoro-1-(3'-fluoro-[1,1'-biphenyl]-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid hydrochloride | | CAS: | 1040526-12-2 | | MF: | C27H23ClF4N4O3 | | MW: | 562.95 | | EINECS: | | | Product Categories: | | | Mol File: | 1040526-12-2.mol |  |
| | LP533401 hcl Chemical Properties |
| storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | | solubility | ≥56.3 mg/mL in DMSO; insoluble in H2O; ≥19.4 mg/mL in EtOH | | form | solid |
| | LP533401 hcl Usage And Synthesis |
| 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. |
| | LP533401 hcl Preparation Products And Raw materials |
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