2. GPCR/G Protein Neuronal Signaling
  3. MCHR1 (GPR24)
  4. TC-MCH 7c

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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TC-MCH 7c

TC-MCH 7c 構造式

CAS 番号 : 864756-35-4

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1 mg $195 在庫あり
5 mg $585 在庫あり
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TC-MCH 7c 関連抗体

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製品説明

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[1]. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively[2].

IC50 & Target

IC50: 5.6 nM (hMCH1R)[1]
Ki: 3.4 nM (hMCH1R) and 3.0 nM (mouse MCH1R)[1]
Cellular Effect
Cell Line Type Value Description References
CHO IC50
23 nM
Compound: 7c
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
[PMID: 21190859]
CHO IC50
5.6 nM
Compound: 7c
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
[PMID: 21190859]
CHO-K1 IC50
5.6 nM
Compound: 1
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
[PMID: 19632840]
CHO-K1 IC50
5.6 nM
Compound: 1
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
[PMID: 19632840]
HEK293 IC50
9 nM
Compound: 7c
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
[PMID: 21190859]
体外実験

TC-MCH 7c has an IC50 of 9.7 μM for MCH1R in [Ca2+]i mobilization[1].
TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively[2].

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

TC-MCH 7c 関連抗体
体内実験

TC-MCH 7c (oral; 3-30 mg/kg; once-daily for 1.5 months) exhibits excellent body weight reduction in a dose-dependent manner in DIO mice model[1].
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.

Animal Model: C57BL/6J DIO mice[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Oral; once-daily for 1.5 months
Result: Exhibited excellent body weight reduction in a dose-dependent manner.
Animal Model: Diet-induced obesity mice[2]
Dosage: 3, 10 and 30 mg/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: Plasma concentrations at 2, 15, and 24 hours were 5.1, 1.8, and 0.7 μM, respectively.
分子量

408.47

分子式

C24H25FN2O3
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C=CC(OCC2=CC=C(F)C=C2)=C1)C3=CC=C(OCCN4CCCC4)C=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4482 mL 12.2408 mL 24.4816 mL
5 mM 0.4896 mL 2.4482 mL 4.8963 mL
10 mM 0.2448 mL 1.2241 mL 2.4482 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション
参考文献

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
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
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TC-MCH 7c Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TC-MCH 7c864756-35-4MCHR1 (GPR24)Melanin concentrating hormone receptor 1orallyavailablebrain-penetrableMCHObesityphenylpyridonederivativeInhibitorinhibitorinhibit

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製品名:
TC-MCH 7c
製品番号:
HY-107623
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