| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
LP533401 targets tryptophan hydroxylase 1 (Tph1). Tph1 is the rate-limiting enzyme in serotonin biosynthesis in the gut. By inhibiting Tph1, LP533401 reduces gut serotonin production. This has downstream effects on bone metabolism, as gut serotonin regulates bone formation, providing a potential anabolic treatment for osteoporosis.
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| ln Vitro |
At a dosage of 1 μM, LP-533401 totally suppresses the synthesis of serotonin in Tph1-expressing cells (RBL2H3 cells)[1].
LP533401 completely inhibits serotonin production in Tph1-expressing cells (RBL2H3 cells) at a dose of 1 μM. It is a potent inhibitor of Tph1. In vitro activity is confirmed through measurement of serotonin levels in Tph1-expressing cell lines treated with the compound. |
| ln Vivo |
Due to a distinct increase in bone production, oral administration of this small molecule once daily for up to 6 weeks completely rescues and prevents the onset of osteoporosis in ovariectomized rodents in a dose-dependent way. After oral treatment, LP-533401 levels in the brain are insignificant, according to pharmacokinetic tests conducted on mice, suggesting that it is essentially unable to penetrate the blood-brain barrier[1]. Repeated administration of LP-533401 (30–250 mg/kg per day) to mice results in significant decreases in 5-HT levels in the blood, lungs, and stomach but not in the brain. Lung and gut 5-HT contents drop by 50% following a single LP533401 dose (250 mg/kg), while blood 5-HT levels stay constant, indicating gut and lung 5-HT synthesis[2]. When administered with the Tph-1 inhibitor LP-533401, adult, healthy mice exhibit a 30% drop in serotonin levels in the blood, which is followed by a 30% increase in osteoblast counts. Giving LP533401 to mice that have received an EL4 cell injection prevents the loss in trabecular bone volume and osteoblast counts, prolongs survival, and lowers leukemic infiltration[3].
LP533401 has anabolic effects in bone in vivo. By inhibiting gut serotonin production, it promotes bone formation. The compound has potential for the treatment of osteoporosis. In vivo efficacy has been demonstrated in animal models of bone metabolism. |
| Enzyme Assay |
Non-cell-based enzyme assays for LP533401 use purified tryptophan hydroxylase 1 (Tph1) enzyme. The compound is incubated with the enzyme and substrate (tryptophan) at varying concentrations. Tph1 activity is measured by quantifying serotonin production using HPLC or fluorescence-based methods. IC50 values for enzyme inhibition are determined.
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| Cell Assay |
Cellular assays for LP533401 utilize Tph1-expressing cells such as RBL2H3 cells. Cells are treated with the compound at various concentrations (e.g., 1 μM). Serotonin levels in cell lysates or supernatants are measured by ELISA or HPLC. Complete inhibition of serotonin production at 1 μM confirms potent cellular activity.
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| Animal Protocol |
In vivo animal models for LP533401 include models of osteoporosis and bone metabolism. The compound is administered orally or via other routes. Efficacy is assessed by measuring bone mineral density, bone formation markers, and gut serotonin levels. The compound's anabolic effects on bone are evaluated. Detailed protocols are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LP533401 include molecular weight of 526.48 g/mol and molecular formula C27H22F4N4O3. CAS number is 945976-43-2. Storage: -20°C. Detailed PK parameters such as half-life and bioavailability are not extensively reported. The compound is a small molecule Tph1 inhibitor.
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| Toxicity/Toxicokinetics |
LP533401 has potential for the treatment of osteoporosis. By inhibiting gut serotonin production, it promotes bone formation. Detailed toxicity data are not extensively reported. The compound is a research tool for studying the role of gut serotonin in bone metabolism and for developing osteoporosis therapies.
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| References |
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| Additional Infomation |
LP533401 is a tryptophan hydroxylase 1 inhibitor. It has CAS number 945976-43-2. The compound regulates serotonin production in the gut. It completely inhibits serotonin production in Tph1-expressing cells at 1 μM. It has anabolic effects in bone and potential for osteoporosis treatment.
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| Molecular Formula |
C27H22F4N4O3
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| Molecular Weight |
526.4916
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| Exact Mass |
526.162
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| CAS # |
945976-43-2
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| Related CAS # |
LP-533401 hydrochloride;1040526-12-2
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| PubChem CID |
44560455
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| Appearance |
Brown to breen solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
699.0±65.0 °C at 760 mmHg
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| Flash Point |
376.5±34.3 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.609
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| LogP |
5.62
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
38
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| Complexity |
759
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| Defined Atom Stereocenter Count |
1
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| 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
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| InChi Key |
JZWUKILTKYJLCN-XEGCMXMBSA-N
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| InChi Code |
InChI=1S/C27H22F4N4O3/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)/t21-,24?/m0/s1
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| 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
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| Synonyms |
LP-533401 LP 533401 LP533401
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8994 mL | 9.4969 mL | 18.9937 mL | |
| 5 mM | 0.3799 mL | 1.8994 mL | 3.7987 mL | |
| 10 mM | 0.1899 mL | 0.9497 mL | 1.8994 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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