Art. -Nr.: HY-123449A

MK-761 TFA

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.93%
Formel: C₁₅H₂₀F₃N₃O₄
Molecular Weight:363.33

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

MK-761 TFA Chemical Structure

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

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

MK-761 (0.312-1.25 mg/kg; p.o.; single administration) TFA exhibits acute hypotensive activity in spontaneously hypertensive rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Wistar-Okamoto spontaneously hypertensive (SH) (male, 30-40 weeks, 290-350 g)^[1]
Dosage:

1.25 mg/kg (no pretreatment); 0.312 mg/kg (Timolol pretreatment)
Administration:

p.o.; single dose
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

Appearance Solid
Molecular Weight 363.33
Formel C₁₅H₂₀F₃N₃O₄
Color White to off-white
SMILES

N#CC1=CC=CN=C1OC[C@H](CNC(C)(C)C)O.O=C(C(F)(F)F)O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7523 mL

13.7616 mL

27.5232 mL

5 mM

0.5505 mL

2.7523 mL

5.5046 mL

10 mM

0.2752 mL

1.3762 mL

2.7523 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Scriabine A, et al. Antihypertensive and cardiac effects of two novel beta-adrenoceptor blocking drugs. Experientia. 1979 Dec 15;35(12):1634-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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MK-761 TFA

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Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MK-761 TFA

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MK-761 TFA Related Classifications

HY-123449A Related Classifications