Mirabegron
Based on 5 publication(s) in Google Scholar
Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.81%
- No. CAS: 223673-61-8
- Fòrmula: C21H24N4O2S
- Peso molecular:396.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Mirabegron
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Actividad biológica
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β adrenergic receptor |
Mirabegron (YM178) increases cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR). EC50 value is 22.4 nM. EC50 values of Mirabegron for human β1- and β2-ARs are 10,000 nM or more, respectively. EC50 of Mirabegron in rat bladder strips precontracted with 10-6 M Carbachol (CCh) is 5.1 μM, whereas that in human bladder strips precontracted with 10-7 M CCh is 0.78 μM. Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human β3-ARs, with an EC50 value and I.A. of 22.4 nM and 0.8, respectively. Mirabegron has little agonistic effect on β1- and β2-ARs. Compared by EC50 value, Mirabegron is approximately one third as potent as isoproterenol. The maximal relaxant effects of Mirabegron are 94±1%, that of CCh, indicating that Mirabegron acts a full agonist in the rat bladder. The maximal relaxant effects of Mirabegron is 89.4±2.3%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 223673-61-8
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Appearance Solid
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Peso molecular 396.51
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Fòrmula C21H24N4O2S
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Color White to light yellow
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SMILES
O=C(NC1=CC=C(CCNC[C@H](O)C2=CC=CC=C2)C=C1)CC3=CSC(N)=N3
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Synonyms
YM178
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Metab
2020 Aug 4;32(2):287-300.e7. PMID: 32755608 -
Adv Sci (Weinh)
Effective Prevention and Treatment of Acute Leukemias in Mice by Activation of Thermogenic Adipose Tissues. [Abstract]2024 Oct;11(38):e2402332. PMID: 39049685
Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]
Schematic diagram of experimental design for testing anti-leukemia effects of combination therapy of chemo drugs and Mirabegron (10 mg/kg per day, oral). After transplantation for 7 days, leukemia-bearing mice were treated with combination therapy for up to 14 days.
Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]
Flow cytometry analysis of GFP+ cells in BM, PB, spleen, and liver in vehicle- or chemo-treated MLL-NRIP3 leukemia-bearing mice under vehicle or Mirabegron (10 mg/kg per day, oral) treatment.
Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]
Quantification of infiltrated leukemia cells in BM, spleen and liver in vehicle- or chemo-treated MLL-NRIP3 leukemia-bearing mice under vehicle or Mirabegron (10 mg/kg per day, oral) treatment.
Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]
Overall survival of vehicle- or chemo-treated MLL-NRIP3 leukemia‐bearing mice under vehicle or Mirabegron (10 mg/kg per day, oral) treatment.
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J Transl Med
ZSWIM4 inhibition improves chemosensitivity in epithelial ovarian cancer cells by suppressing intracellular glycine biosynthesis. [Abstract]2024 Feb 21;22(1):192. PMID: 38383406 -
Cardiovasc Drugs Ther
Mirabegron Ameliorated Atherosclerosis of ApoE-/- Mice in Chronic Intermittent Hypoxia but Not in Normoxia. [Abstract]2022 Oct;36(5):805-815. PMID: 34152510 -
Solvente y solubilidad
DMSO : 100 mg/mL (252.20 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (5.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocolo
CHO cells (105) are seeded in each well of a 24-well culture plate and subcultured. Three days later, the medium is exchanged with 250 μL/well Hanks' balanced salt solution containing 0.1 mM 3-isobutyl-1-methylxanthine, pH 7.4. The cells are incubated with each compound (isoproterenol, Mirabegron, BRL37344, and CL316,243 at final concentrations of 10-10 to 10-4 M) for 10 min at 37°C, after which incubation is stopped by the addition of 250 μL of 0.2 M HCl. cAMP concentration in the reaction mixture is measured by radioimmunoassay using an 125I-cAMP assay system using a gamma counter. Fifty microliters of reaction mixture is incubated with 50 μL of succinyl agent for 10 min at room temperature, after which the reaction is stopped by the addition of 400 μL of buffer solution. Fifty microliters of succinylated sample is incubated with 50 μL of 125I-cAMP and 50 μL of anti-cAMP antibody for 24 h at 4°C. At the end of the incubation period, 250 μL of charcoal suspension is added and centrifuged for 10 min at 2800g at 4°C. Two hundred and fifty microliters of supernatant is transferred into a tube and counted for 1 min using a gamma counter. The intrinsic activity (I.A.) relative to isoproterenol for each β-adrenoceptor agonist is calculated using the maximal response of each compound[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Male (350 to 400 g) and female (225 to 290 g) Wistar rats are used. The free-form doses of 0.03, 0.1, 0.3, 1 and 3 mg/kg for Mirabegron and 0.0272, 0.0907, 0.272, 0.907, and 2.72 mg/kg for oxybutynin are used in this study.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5220 mL | 12.6100 mL | 25.2200 mL | 63.0501 mL |
| 5 mM | 0.5044 mL | 2.5220 mL | 5.0440 mL | 12.6100 mL | |
| 10 mM | 0.2522 mL | 1.2610 mL | 2.5220 mL | 6.3050 mL | |
| 15 mM | 0.1681 mL | 0.8407 mL | 1.6813 mL | 4.2033 mL | |
| 20 mM | 0.1261 mL | 0.6305 mL | 1.2610 mL | 3.1525 mL | |
| 25 mM | 0.1009 mL | 0.5044 mL | 1.0088 mL | 2.5220 mL | |
| 30 mM | 0.0841 mL | 0.4203 mL | 0.8407 mL | 2.1017 mL | |
| 40 mM | 0.0631 mL | 0.3153 mL | 0.6305 mL | 1.5763 mL | |
| 50 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2610 mL | |
| 60 mM | 0.0420 mL | 0.2102 mL | 0.4203 mL | 1.0508 mL | |
| 80 mM | 0.0315 mL | 0.1576 mL | 0.3153 mL | 0.7881 mL | |
| 100 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL |
Mirabegron Related Classifications
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