1. GPCR/G Protein
    Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. MCHR1 (GPR24)
    Potassium Channel
  3. MCHr1 antagonist 2

MCHr1 antagonist 2 

Cat. No.: HY-100321
Handling Instructions

MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.

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

MCHr1 antagonist 2 Chemical Structure

MCHr1 antagonist 2 Chemical Structure

CAS No. : 863115-70-2

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Description

MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.

IC50 & Target

IC50: 65 nM (melanin concentrating hormone receptor 1), 4.0 nM (hERG in IMR-32 cells)[1]

In Vitro

MCHr1 antagonist 2 (Compound 30) is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM. MCHr1 antagonist 2 has inhibitory effects on Ca2+ flux, and hERG, with IC50s of 196 ± 30 nM and 4.0 ± 0.8 nM, respectively, in IMR-32 cells[1].

Molecular Weight

424.42

Formula

C₂₃H₂₁FN₂O₅

CAS No.

863115-70-2

SMILES

O=C(C1=CC(C2=CC(F)=CC=C2O1)=O)NC3CCN(CC4=CC=C(OCO5)C5=C4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Kinase Assay
[1]

In 96-well plates, IMR-32 cells (I3.4.2) membranes (6 μg/well) are incubated in the presence of test compound (MCHr1 antagonist 2) in binding buffer (25 mM HEPES pH 7.4, 1 mM CaCl2, 5 mM MgCl2 and 0.5% BSA) and with 0.05 nM [125I]MCH (2200 Ci/mmol) per well for 60 min at room temperature. Nonspecific binding controls consist of I3.4.2 membranes, 0.05 nM [125I]MCH, and 300 nM human MCH. Total binding controls of I3.4.2 membranes and 0.05 nM [125I]MCH are also included on each plate. The plates are centrifuged for 5 min at 1380 g in a GS-6R desktop centrifuge. The reaction buffer is carefully aspirated from each well without disturbing the pellet. Wash buffer (25 mM HEPES, pH 7.4, 1 mM CaCl2, 5 mM MgCl2, and 0.5 M NaCl) is added to each well and then transferred to a 0.5% polyethylenimine-treated GF/B filtration plate using a plate Filtermate Harvester. The filter plate is washed three times with wash buffer, MicroScint 20 is added to each well, and the plate is read using a Topcount microplate scintillation counter[1].

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

References
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KeyWords:

MCHr1 antagonist 2 | MCHR1 (GPR24) | Potassium Channel | Melanin concentrating hormone receptor 1 | KcsA | Inhibitor | inhibitor | inhibit

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MCHr1 antagonist 2
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HY-100321
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