2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. MK-761 free base

MK-761 free base is an orally effective β2-adrenergic receptor antagonist. MK-761 free base 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 free base can be used in the research of hypertension.

For research use only. We do not sell to patients.

MK-761 free base

MK-761 free base Chemical Structure

CAS No. : 65321-41-7

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Based on 1 publication(s) in Google Scholar

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MK-761 free base Related Antibodies

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Description

MK-761 free base is an orally effective β2-adrenergic receptor antagonist. MK-761 free base 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 free base can be used in the research of hypertension[1].

IC50 & Target[1]

Beta-2 adrenergic receptor

 

In Vitro

MK-761 (0.125-2.0 μg/mL; 30 min) free base 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) free base 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.

MK-761 free base Related Antibodies
In Vivo

MK-761 (0.312-1.25 mg/kg; p.o.; single administration) free base 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.
Molecular Weight

249.31

Formula

C13H19N3O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (401.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0111 mL 20.0554 mL 40.1107 mL
5 mM 0.8022 mL 4.0111 mL 8.0221 mL
View the 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.

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Purity & Documentation
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
DMSO 1 mM 4.0111 mL 20.0554 mL 40.1107 mL 100.2768 mL
5 mM 0.8022 mL 4.0111 mL 8.0221 mL 20.0554 mL
10 mM 0.4011 mL 2.0055 mL 4.0111 mL 10.0277 mL
15 mM 0.2674 mL 1.3370 mL 2.6740 mL 6.6851 mL
20 mM 0.2006 mL 1.0028 mL 2.0055 mL 5.0138 mL
25 mM 0.1604 mL 0.8022 mL 1.6044 mL 4.0111 mL
30 mM 0.1337 mL 0.6685 mL 1.3370 mL 3.3426 mL
40 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5069 mL
50 mM 0.0802 mL 0.4011 mL 0.8022 mL 2.0055 mL
60 mM 0.0669 mL 0.3343 mL 0.6685 mL 1.6713 mL
80 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2535 mL
100 mM 0.0401 mL 0.2006 mL 0.4011 mL 1.0028 mL
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MK-761 free base Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-76165321-41-7MK761MK 761Adrenergic ReceptorBeta Receptortimololcatecholamineisoproterenolhypertensionspontaneously hypertensive ratscat heart papillary muscleβ-adrenoceptorInhibitorinhibitorinhibit

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