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LP-533401 HCl

Alias: LP-533401 HCl LP 533401 HCl LP533401 HCl LP-533401 Hydrochloride LP 533401 Hydrochloride LP533401 Hydrochloride
Cat No.:V18911 Purity: ≥98%
LP-533401 HCl is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the intestine.
LP-533401 HCl
LP-533401 HCl Chemical Structure CAS No.: 1040526-12-2
Product category: Tryptophan Hydroxylase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of LP-533401 HCl:

  • LP533401
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description
LP-533401 HCl is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the intestine.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
LP-533401 Hydrochronide is a tryptophan platformase1. LP-533401 (1 μM) totally suppresses plasmatonin synthesis in Tph1-expressing cells (RBL2H3 cells) after 3 days of treatment [1].
ln Vivo
Because of a distinct rise in bone mass, LP-533401 (25, 100, or 250 mg/kg) increased intensity once daily for six weeks boosted attempts to avoid and totally rescue osteoporosis in animals in late pregnancy. According to pharmacokinetic studies, LP-533401 is essentially impossible to pass the blood-brain barrier since it reaches very low concentrations in the brain of animals after the epidermis [1]. The 5-HT content of lesions, lungs, and blood significantly decreased in mice given LP-533401 (30–250 mg/kg daily), but not in the brain. Lung and damaged 5-HT levels were lowered by 50% following a single dosage of LP-533401 (250 mg/kg), although blood 5-HT levels did not change, suggesting disruption and lung 5-HT production [2]. Tph-1 LP-533401 treatment of glandular healthy cells resulted in a 30% decrease in circulating hematin levels and a 30% increase in incoming osteoblast counts. When LP-533401 is administered to mice that have had an EL4 cell injection, it can decrease venous circulation, prolong survival, and prevent the decrease of osteoblast quantity and trabecular bone volume [3].
References

[1]. Inhibition of gut-derived serotonin synthesis: A potential bone anabolic treatment. Nat. Med. 16(3), 308-312 (2010).

[2]. Inhibition of gut- and lung-derived serotonin attenuates pulmonary hypertension in mice. Am J Physiol Lung Cell Mol Physiol. 2012 Sep 15;303(6):L500-8.

[3]. Inhibition of leukemia cell engraftment and disease progression in mice by osteoblasts. Blood. 2014 Oct 30;124(18):2834-46.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H23CLF4N4O3
Molecular Weight
562.94 Exact Mass
Exact Mass
562.139
CAS #
1040526-12-2
Related CAS #
LP-533401;945976-43-2
PubChem CID
102602704
Appearance
Light yellow to yellow solid powder
LogP
7.252
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
11
Rotatable Bond Count
8
Heavy Atom Count
39
Complexity
759
Defined Atom Stereocenter Count
1
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)C[C@@H](C(=O)O)N)N.Cl
InChi Key
BHBWZCUMIXCDPM-CHXZROHQSA-N
InChi Code
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
Chemical Name
2(S)-Amino-3-(4-{2-amino-6-[2,2,2-trifluoro-1-(3'-fluoro-biphenyl-4-yl)-ethoxy]-pyrimidin-4-yl}-phenyl)-propionic acid Hydrochloride
Synonyms
LP-533401 HCl LP 533401 HCl LP533401 HCl LP-533401 Hydrochloride LP 533401 Hydrochloride LP533401 Hydrochloride
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~25 mg/mL (~44.41 mM)
H2O : ≥ mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 2.5 mg/mL (4.44 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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