TC-MCH 7c
Based on 1 Customer Validation
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
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- Reinheit: 99.79%
- CAS. Nr.: 864756-35-4
- Formel: C24H25FN2O3
- Molecular Weight:408.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
IC50: 5.6 nM (hMCH1R)[1]
Ki: 3.4 nM (hMCH1R) and 3.0 nM (mouse MCH1R)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
23 nM
Compound: 7c
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Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
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[PMID: 21190859] |
| CHO | IC50 |
5.6 nM
Compound: 7c
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Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
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[PMID: 21190859] |
| CHO-K1 | IC50 |
5.6 nM
Compound: 1
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Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
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[PMID: 19632840] |
| CHO-K1 | IC50 |
5.6 nM
Compound: 1
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Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
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[PMID: 19632840] |
| HEK293 | IC50 |
9 nM
Compound: 7c
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Displacement of [35S]N-[(4R)-10-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,40-piperidin]-6-yl]methanesulfonamide from human ERG expressed in HEK293 cells
Displacement of [35S]N-[(4R)-10-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,40-piperidin]-6-yl]methanesulfonamide from human ERG expressed in HEK293 cells
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[PMID: 21190859] |
TC-MCH 7c (oral; 3-30 mg/kg) with 30 mg/kg has plasma concentrations of 5.1, 1.8, and 0.7 μM at 2, 15, and 24 hours, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J DIO mice[1]
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Dosage:3, 10 and 30 mg/kg
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Administration:Oral; once-daily for 1.5 months
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Result:Exhibited excellent body weight reduction in a dose-dependent manner.
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Animal Model:Diet-induced obesity mice[2]
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Dosage:3, 10 and 30 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral
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Result:Plasma concentrations at 2, 15, and 24 hours were 5.1, 1.8, and 0.7 μM, respectively.
Chemical Information
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CAS. Nr. 864756-35-4
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Appearance Solid
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Molecular Weight 408.47
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Formel C24H25FN2O3
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Color Light yellow to yellow
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SMILES
O=C1N(C=CC(OCC2=CC=C(F)C=C2)=C1)C3=CC=C(OCCN4CCCC4)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 20 mg/mL (48.96 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (270 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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Handling Instructions (2659 KB)
Verweise
[1]. Ito M, et al. Melanin-concentrating hormone 1-receptor antagonist suppresses body weight gain correlated with high receptor occupancy levels in diet-induced obesity mice. Eur J Pharmacol. 2009 Dec 10;624(1-3):77-83. [Content Brief]
[2]. Haga Y, et al. Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists. Bioorg Med Chem. 2011 Jan 15;19(2):883-93. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4482 mL | 12.2408 mL | 24.4816 mL | 61.2040 mL |
| 5 mM | 0.4896 mL | 2.4482 mL | 4.8963 mL | 12.2408 mL | |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4482 mL | 6.1204 mL | |
| 15 mM | 0.1632 mL | 0.8161 mL | 1.6321 mL | 4.0803 mL | |
| 20 mM | 0.1224 mL | 0.6120 mL | 1.2241 mL | 3.0602 mL | |
| 25 mM | 0.0979 mL | 0.4896 mL | 0.9793 mL | 2.4482 mL | |
| 30 mM | 0.0816 mL | 0.4080 mL | 0.8161 mL | 2.0401 mL | |
| 40 mM | 0.0612 mL | 0.3060 mL | 0.6120 mL | 1.5301 mL |
TC-MCH 7c Related Classifications
HY-107623 Related Classifications
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