1. Metabolic Enzyme/Protease
  2. Tryptophan Hydroxylase

LP-533401 hydrochloride 

Cat. No.: HY-15849A
Handling Instructions

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

For research use only. We do not sell to patients.

LP-533401 hydrochloride Chemical Structure

LP-533401 hydrochloride Chemical Structure

CAS No. : 1040526-12-2

Size Price Stock
1 mg USD 72 Get quote
5 mg USD 300 Get quote
10 mg USD 528 Get quote
25 mg USD 1152 Get quote

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Other In-stock Forms of LP-533401 hydrochloride:

Other Forms of LP-533401 hydrochloride:

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  • Biological Activity

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Description

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

IC50 & Target

Tryptophan hydroxylase 1[1]

In Vitro

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor. LP-533401 (1 μM) completely inhibits serotonin production in Tph1-expressing cells (RBL2H3 cells) after treatment for 3 days[1].

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7764 mL 8.8819 mL 17.7639 mL
5 mM 0.3553 mL 1.7764 mL 3.5528 mL
10 mM 0.1776 mL 0.8882 mL 1.7764 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Mice are treated from day 1 post-ovariectomy for 4 weeks with LP-533401 (1, 10, 100 or 250 mg per kg body weight per day) or vehicle. Next mice are treated for 4 weeks starting 2 weeks post-ovariectomy with LP-533401 (250 mg per kg body weight per day) or vehicle. lastly, mice are treated for 6 weeks starting 6 weeks post-ovariectomy with LP-533401 (25, 100 or 250 mg per kg body weight per day) or vehicle[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

562.94

Formula

C₂₇H₂₃ClF₄N₄O₃

CAS No.

1040526-12-2

SMILES

N[[email protected]@H](CC1=CC=C(C2=NC(N)=NC(OC(C3=CC=C(C4=CC=CC(F)=C4)C=C3)C(F)(F)F)=C2)C=C1)C(O)=O.[H]Cl

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
LP-533401 hydrochloride
Cat. No.:
HY-15849A
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LP-533401 hydrochloride

Cat. No.: HY-15849A