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

TC-MCH 7c 

Cat. No.: HY-107623 Purity: >99.0%
Handling Instructions

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.

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

TC-MCH 7c Chemical Structure

TC-MCH 7c Chemical Structure

CAS No. : 864756-35-4

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10 mM * 1 mL in DMSO USD 526 In-stock
Estimated Time of Arrival: December 31
1 mg USD 195 In-stock
Estimated Time of Arrival: December 31
5 mg USD 585 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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]

In Vitro

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].

In Vivo

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].

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.
Molecular Weight

408.47

Formula

C₂₄H₂₅FN₂O₃

CAS No.

864756-35-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

TC-MCH 7cMCHR1 (GPR24)Melanin concentrating hormone receptor 1orallyavailablebrain-penetrableMCHObesityphenylpyridonederivativeInhibitorinhibitorinhibit

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TC-MCH 7c
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