MCHR1 antagonist 2
Based on 1 Customer Validation
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.
- Purity: 98.27%
- CAS No.: 863115-70-2
- Formula: C23H21FN2O5
- Molecular Weight:424.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 65 nM (melanin concentrating hormone receptor 1), 4.0 nM (hERG in IMR-32 cells)[1]
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Cell Line
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Type | Value | Description | References |
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| IMR-32 | IC50 |
0.004 μM
Compound: 1
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Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
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[PMID: 17188866] |
| IMR-32 | IC50 |
0.025 μM
Compound: 1
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Inhibition of MCH-mediated calcium release in IMR-32 cells
Inhibition of MCH-mediated calcium release in IMR-32 cells
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[PMID: 17188866] |
| IMR-32 | IC50 |
196 nM
Compound: 30
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Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
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[PMID: 17064075] |
| IMR-32 | IC50 |
65 nM
Compound: 30
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Displacement of [125I]MCH from MCHr1 expressed in IMR32 cells
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cells
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[PMID: 17064075] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 863115-70-2
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Appearance Solid
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Molecular Weight 424.42
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Formula C23H21FN2O5
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC(F)=CC=C2O1)=O)NC3CCN(CC4=CC=C(OCO5)C5=C4)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 10 mg/mL (23.56 mM; ultrasonic and adjust pH to 6 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.36 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.36 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3562 mL | 11.7808 mL | 23.5616 mL | 58.9039 mL |
| 5 mM | 0.4712 mL | 2.3562 mL | 4.7123 mL | 11.7808 mL | |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3562 mL | 5.8904 mL | |
| 15 mM | 0.1571 mL | 0.7854 mL | 1.5708 mL | 3.9269 mL | |
| 20 mM | 0.1178 mL | 0.5890 mL | 1.1781 mL | 2.9452 mL |
MCHR1 antagonist 2 Related Classifications
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