TPT-004
Based on 1 Customer Validation
TPT-004 is a selective and oraly active tryptophan hydroxylases (TPH) inhibitor with IC50s of 77 nM and 16 nM for TPH1 and TPH2, repsectively. TPT-004 exhibits exceptional selectivity for TPH1 compared with other members of the AAAH family. TPT-004 shows efficacy peripheral serotonin attenuation and colorectal tumor growth in mice[1][2].
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- Pureté: 99.90%
- CAS No.: 3032648-15-7
- Formule: C18H20N6O3S
- Masse moléculaire:400.45
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Metabolism/Protease Compound Library
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
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Anti-Colorectal Cancer Compound Library
HY-L103
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
0.077 μM
Compound: 32; TPT-004
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Inhibition of recombinant MBP-tagged full length human THP1 using L-Trp as substrate assessed as formation of 5-HTP by measuring fluorescent property
Inhibition of recombinant MBP-tagged full length human THP1 using L-Trp as substrate assessed as formation of 5-HTP by measuring fluorescent property
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[PMID: 37905925] |
TPT-004 (72 h) reduces the intracellular serotonin levels, showing a dose-response curve with an IC50 of 0.952 μM, in serotonergic BON cells[1].
TPT-004 inhibits phenylalanine hydroxylase (PAH) and tyrosine hydroxylase (TH) with IC50 values of 403.5 nM and 1.359 μM, repsectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6N mice (aged 8 weeks) were subcutaneously transplanted with MC38 tumor fragments[1].
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Dosage:50 mg/kg
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Administration:Oral gavage; twice daily; for 20 days
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Result:Attenuated the tumor-growth, especially in the initial growth phase.
Chemical Information
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CAS No. 3032648-15-7
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Appearance Solid
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Masse moléculaire 400.45
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Formule C18H20N6O3S
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Color White to off-white
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SMILES
CCN1C2=C(C(NC1=O)=O)N(C(CC3=CN4C=C(SC4=N3)C)=N2)CC5COC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (312.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Specker E, et al. Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors. J Med Chem. 2023 Oct 31. [Content Brief]
[2]. Wesolowski R,et al. Selectivity and Safety Characterization of a Xanthine-Imidazothiazole Lead Structure: a Novel Tryptophan Hydroxylase Inhibitor of Peripheral Serotonin Synthesis. ACS Pharmacol Transl Sci. 2025 May 19;8(6):1678-1693. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4972 mL | 12.4860 mL | 24.9719 mL | 62.4298 mL |
| 5 mM | 0.4994 mL | 2.4972 mL | 4.9944 mL | 12.4860 mL | |
| 10 mM | 0.2497 mL | 1.2486 mL | 2.4972 mL | 6.2430 mL | |
| 15 mM | 0.1665 mL | 0.8324 mL | 1.6648 mL | 4.1620 mL | |
| 20 mM | 0.1249 mL | 0.6243 mL | 1.2486 mL | 3.1215 mL | |
| 25 mM | 0.0999 mL | 0.4994 mL | 0.9989 mL | 2.4972 mL | |
| 30 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0810 mL | |
| 40 mM | 0.0624 mL | 0.3121 mL | 0.6243 mL | 1.5607 mL | |
| 50 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2486 mL | |
| 60 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0405 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7804 mL | |
| 100 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL |
TPT-004 Related Classifications
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