LP533401 hcl

Product Name: LP533401 hcl
CAS No.: 1040526-12-2
Chemical Name: LP533401 hcl
Synonyms: CS-1770;LP533401 hcl;LP-533401 hydrochloride;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;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
CBNumber: CB82731287
Molecular Formula: C27H23ClF4N4O3
Formula Weight: 562.95
MOL File: 1040526-12-2.mol

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LP533401 hcl Property

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
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0028599
Product name: LP-533401hydrochloride
Purity: 98.09%
Packaging: 5mg
Price: $100
Updated: 2021/12/16

ChemScene

Product number: CS-0028599
Product name: LP-533401hydrochloride
Purity: 98.09%
Packaging: 10mg
Price: $150
Updated: 2021/12/16

ChemScene

Product number: CS-0028599
Product name: LP-533401hydrochloride
Purity: 98.09%
Packaging: 25mg
Price: $280
Updated: 2021/12/16

ApexBio Technology

Product number: B5823
Product name: LP533401hcl
Packaging: 25mg
Price: $280
Updated: 2021/12/16

ChemScene

Product number: CS-0028599
Product name: LP-533401hydrochloride
Purity: 98.09%
Packaging: 50mg
Price: $450
Updated: 2021/12/16

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LP533401 hcl Chemical Properties,Usage,Production

Uses

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

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].

in vivo

Oral administration once daily for up to 6 weeks of LP-533401 (25, 100 or 250 mg/kg) dose-dependently prevents the development of and fully rescues, osteoporosis in ovariectomized rodents because of an isolated increase in bone formation. Pharmacokinetic studies in rodents show that LP-533401 level in the brain is negligible following oral administration, indicating that it is virtually unable to cross the blood-brain barrier^[1]. Mice treated repeatedly with LP-533401 (30-250 mg/kg per day) exhibit marked 5-HT content reductions in the gut, lungs, and blood, but not in the brain. After a single LP-533401 dose (250 mg/kg), lung and gut 5-HT contents decrease by 50%, whereas blood 5-HT levels remain unchanged, suggesting gut and lung 5-HT synthesis^[2]. Adult, healthy mice treated with the Tph-1 inhibitor LP-533401 show 30% decrease in circulating serotonin levels, with a consequent 30% increase in osteoblast numbers. Administration of LP-533401 to mice injected with EL4 cells inhibits the decrement in osteoblast numbers and trabecular bone volume, prolongs survial, and decreases leukemic infiltration^[3].

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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Preparation Products

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LP533401 hcl Suppliers

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1040526-12-2, LP533401 hclRelated Search:

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

LP-533401 hydrochloride

LP533401 hcl

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

1040526-12-2

C27H23ClF4N4O3