MK-761 TFA
Based on 1 Customer Validation
MK-761 TFA is an orally effective β2-adrenergic receptor antagonist. MK-761 TFA attenuates positive inotropic effects, reduces arterial pressure, enhances the contractility of papillary muscles in cat hearts, and exerts effects mediated by catecholamine release. MK-761 TFA can be used in the research of hypertension.
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- Pureza : 99.93%
- Fòrmula: C15H20F3N3O4
- Peso molecular:363.33
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
MK-761 (0.125-2.0 μg/mL; 30 min) TFA enhances the contractility of isolated cat papillary muscles in a dose-dependent manner, and this positive inotropic effect is significantly inhibited by pretreatment with Timolol (HY-17494)[1].
MK-761 (0.03-1.0 μg/mL; 30 min) TFA blocks the positive inotropic effect of isoprenaline (HY-B0468) on isolated cat papillary muscles[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar-Okamoto spontaneously hypertensive (SH) (male, 30-40 weeks, 290-350 g)[1]
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Dosage:1.25 mg/kg (no pretreatment); 0.312 mg/kg (Timolol pretreatment)
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Administration:p.o.; single dose
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Result:Lowered mean arterial pressure in SH rats, with maximal effect reached at 1 hour after administration of 1.25 mg/kg p.o.
Showed no significant difference in heart rate changes compared to vehicle control.
Exhibited an antihypertensive effect at 0.312 mg/kg p.o. that was not antagonized by pretreatment with 8 mg/kg p.o. timolol.
Had a relative antihypertensive potency of 3.4 (relative to hydralazine, potency = 1) with 95% confidence limits of 1.8 and 7.3.
Chemical Information
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Appearance Solid
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Peso molecular 363.33
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Fòrmula C15H20F3N3O4
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Color White to off-white
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SMILES
N#CC1=CC=CN=C1OC[C@H](CNC(C)(C)C)O.O=C(C(F)(F)F)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (275.23 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
In Vivo:
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: ≥ 2.5 mg/mL (6.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7523 mL | 13.7616 mL | 27.5232 mL | 68.8080 mL |
| 5 mM | 0.5505 mL | 2.7523 mL | 5.5046 mL | 13.7616 mL | |
| 10 mM | 0.2752 mL | 1.3762 mL | 2.7523 mL | 6.8808 mL | |
| 15 mM | 0.1835 mL | 0.9174 mL | 1.8349 mL | 4.5872 mL | |
| 20 mM | 0.1376 mL | 0.6881 mL | 1.3762 mL | 3.4404 mL | |
| 25 mM | 0.1101 mL | 0.5505 mL | 1.1009 mL | 2.7523 mL | |
| 30 mM | 0.0917 mL | 0.4587 mL | 0.9174 mL | 2.2936 mL | |
| 40 mM | 0.0688 mL | 0.3440 mL | 0.6881 mL | 1.7202 mL | |
| 50 mM | 0.0550 mL | 0.2752 mL | 0.5505 mL | 1.3762 mL | |
| 60 mM | 0.0459 mL | 0.2294 mL | 0.4587 mL | 1.1468 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8601 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6881 mL |
MK-761 TFA Related Classifications
HY-123449A Related Classifications
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