MCHr1 antagonist 2
Modify Date: 2024-01-18 09:45:46
MCHr1 antagonist 2 structure
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Common Name | MCHr1 antagonist 2 | ||
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| CAS Number | 863115-70-2 | Molecular Weight | 424.42 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H21FN2O5 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of MCHr1 antagonist 2MCHr1 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. |
| Name | MCHr1 antagonist 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. |
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| Related Catalog | |
| 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]. |
| Kinase Assay | 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]. |
| References |
| Molecular Formula | C23H21FN2O5 |
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| Molecular Weight | 424.42 |
| Storage condition | 2-8℃ |