MCHr1 antagonist 2 |
| Catalog No.GC31505 |
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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 863115-70-2
Sample solution is provided at 25 µL, 10mM.
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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.
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].
[1]. Lynch JK, et al. Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety. J Med Chem. 2006 Nov 2;49(22):6569-84.
Kinase experiment: | 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: [1]. Lynch JK, et al. Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety. J Med Chem. 2006 Nov 2;49(22):6569-84. | |
| Cas No. | 863115-70-2 | SDF | |
| Canonical SMILES | O=C(C1=CC(C2=CC(F)=CC=C2O1)=O)NC3CCN(CC4=CC=C(OCO5)C5=C4)CC3 | ||
| Formula | C23H21FN2O5 | M.Wt | 424.42 |
| Solubility | DMSO : 10 mg/mL (23.56 mM; ultrasonic and adjust pH to 6 with HCl) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3562 mL | 11.7808 mL | 23.5616 mL |
| 5 mM | 0.4712 mL | 2.3562 mL | 4.7123 mL |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3562 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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