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LP533401 hcl

Tph-1 inhibitor CAS# 1040526-12-2

LP533401 hcl

Catalog No. BCC6377----Order now to get a substantial discount!

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LP533401 hcl: 5mg $403 In Stock
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Chemical structure

LP533401 hcl

3D structure

Chemical Properties of LP533401 hcl

Cas No. 1040526-12-2 SDF Download SDF
PubChem ID 102602704 Appearance Powder
Formula C27H23ClF4N4O3 M.Wt 562.94
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 25 mg/mL (44.41 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name (2S)-2-amino-3-[4-[2-amino-6-[2,2,2-trifluoro-1-[4-(3-fluorophenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoic acid;hydrochloride
SMILES C1=CC(=CC(=C1)F)C2=CC=C(C=C2)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N.Cl
Standard InChIKey BHBWZCUMIXCDPM-CHXZROHQSA-N
Standard InChI InChI=1S/C27H22F4N4O3.ClH/c28-20-3-1-2-19(13-20)16-8-10-18(11-9-16)24(27(29,30)31)38-23-14-22(34-26(33)35-23)17-6-4-15(5-7-17)12-21(32)25(36)37;/h1-11,13-14,21,24H,12,32H2,(H,36,37)(H2,33,34,35);1H/t21-,24?;/m0./s1
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

LP533401 hcl Dilution Calculator

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LP533401 hcl Molarity Calculator

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Preparing Stock Solutions of LP533401 hcl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7764 mL 8.8819 mL 17.7639 mL 35.5278 mL 44.4097 mL
5 mM 0.3553 mL 1.7764 mL 3.5528 mL 7.1056 mL 8.8819 mL
10 mM 0.1776 mL 0.8882 mL 1.7764 mL 3.5528 mL 4.441 mL
50 mM 0.0355 mL 0.1776 mL 0.3553 mL 0.7106 mL 0.8882 mL
100 mM 0.0178 mL 0.0888 mL 0.1776 mL 0.3553 mL 0.4441 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on LP533401 hcl

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.

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Description

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

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