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Cat. No.: HY-189036

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H87/07

H87/07 is a cardioselective β1-adrenoceptor antagonist with intrinsic sympathomimetic activity. H87/07 has a pK_i of 7.00 for the human β1-adrenoceptor. In isolated cat and guinea pig atrial/papillary muscle models, H87/07 exerts β-blocking effects at low concentrations and exhibits cardiac stimulatory effects only at higher concentrations. H87/07 can be used for research on angina pectoris.

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CAS No.: 30311-37-6
Formule: C₁₅H₂₅NO₄
Masse moléculaire:283.36

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

H87/07 Chemical Structure

CAS No.: 30311-37-6

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

IC₅₀ & Target

^[1]

β1 adrenoceptor

7.00 (pKi)

Voir tous les produits spécifiques à Isoform Adrenergic Receptor :

In Vitro

Cardiovascular RegulationRegulation of Cardiac Pump Function

Cardiovascular Regulation

H87/07 (compound 7) binds to the human β₁-adrenoceptor expressed in CHO cell membranes with a pKi of 7.00; it antagonizes the β1-AR chronotropic response mediated by (-)-isoproterenol in isolated rat atria with a pA₂ of 7.37^[1].

Cardiovascular Regulation

Regulation of Cardiac Pump Function

H87/07 (compound 3) acts as a partial chronotropic agonist in isolated cat and guinea pig right atria, with higher intrinsic activity in kitten atria; it blocks the chronotropic response to isoproterenol, with mean -log K_B values of 6.9 and 6.7 in kitten and guinea pig right atria, respectively^[2].
H87/07 (2 × 10^-6 M) yields -log K_B values of 6.62 and 6.45/6.47 in kitten right atrium and left atrium, indicating similar apparent affinities for chronotropic and inotropic responses^[2].
H87/07 has a -log K_S of 7.0 in both kitten and guinea pig atria, a -log EC₅₀ of 7.3 in kitten atria, and 6.9 in guinea pig atria^[2].

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

In Vivo

Cardiovascular RegulationRegulation of Cardiac Pump Function

Cardiovascular Regulation

Compared with Metoprolol (HY-17503), H87/07 produces a smaller reduction in resting heart rate and a longer recovery time of ST-segment depression after exercise^[3].

Cardiovascular Regulation

Regulation of Cardiac Pump Function

H87/07 is a cardioselective β-blocker with intrinsic sympathomimetic activity, and its potency in blocking isoproterenol-induced tachycardia in vivo is 0.4 times that of propranolol^[3].

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

Chemical Information

CAS No. 30311-37-6
Masse moléculaire 283.36
Formule C₁₅H₂₅NO₄
SMILES

OC(CNC(C)C)COC1=CC=C(C=C1)OCCOC
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 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)
Instruction de manipulation (2659 KB)

Références

[1]. Louis SN, et al. CoMFA analysis of the human beta(1)-adrenoceptor binding affinity of a series of phenoxypropanolamines. Eur J Med Chem. 2002 Feb;37(2):111-25.

[2]. Kaumann A J. beta-Adrenoceptor blocking agents as partial agonists in isolated heart muscle: dissociation of stimulation and blockade. Naunyn-schmiedeberg's Archives of Pharmacology, 1980, 311(3): 237-248.

[3]. Clarkson R, et al. Chapter 6. β-Adrenergic Blocking Agents. In: Annual Reports in Medicinal Chemistry, 1975, 10: 51-60.

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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.

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Chemical Information
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H87/07

Voir tous les produits spécifiques à Isoform Adrenergic Receptor

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In Vivo

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