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TC-MCH 7c

SKU: orb1708402

Description

TC-MCH 7c is a phenylpyridone-derived, orally bioavailable and brain-penetrant antagonist of the melanin-concentrating hormone receptor 1 (MCH1R). It exhibits high affinity with Ki values of 3.4 nM for human and 3.0 nM for mouse MCH1R, making it a valuable tool for investigating MCH1R function in both in vitro assays and in vivo models of energy homeostasis and mood regulation.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number864756-35-4
MW408.47
Purity99.54%
FormulaC24H25FN2O3
SMILESFc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1
TargetMelanin-concentrating Hormone Receptor (MCHR),GPCR
SolubilityDMSO:55 mg/mL (134.65 mM)

Bioactivity

Target IC50
MCH1R (human):(ki)3.4 nM |MCH1R (human):5.6 nM |MCH1R (human):5.6 nM|MCH1R (human):3.4 nM (ki)|MCH1R (mouse):3.0 nM |MCH1R (mouse):3.0 nM
In Vivo
In DIO mice model, TC-MCH 7c (oral; 3-30 mg/kg; once-daily for 1.5 months) shows excellent body weight reduction in a dose-dependent manner . TC-MCH 7c(oral; 3 to 30mg /kg) and 30mg /kg at 2, 15 and 24 h were 5.1, 1.8 and 0.7 μM, respectively.
In Vitro
In [Ca2+]i mobilization, TC-MCH 7c has an IC50 of 9.7 μM for MCH1R . TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

MCH1-R, MCHR, Melanin-concentrating Hormone Receptor, Melaninconcentrating Hormone Receptor (MCHR), MelaninconcentratingHormoneReceptor, MelaninconcentratingHormoneReceptor(MCHR), mouse MCH1R, hMCH1R, TCMCH 7c, TC-MCH 7c, TC MCH 7c
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Key Properties

No computed properties available.

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Protocol Information

TC-MCH 7c (orb1708402)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 140.00
1 ml x 10 mM (in DMSO)
$ 310.00
5 mg
$ 330.00
10 mg
$ 460.00
25 mg
$ 680.00
50 mg
$ 900.00
100 mg
$ 1,190.00
500 mg
$ 2,350.00
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