2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. 4-Hydroxypropranolol hydrochloride

4-Hydroxypropranolol hydrochloride  (Synonyms: (±)-4-hydroxy Propranolol hydrochloride)

製品番号: HY-100634 純度: 99.73%
COA 取扱説明書 Technical Support

4-Hydroxypropranolol hydrochloride is a non-cardiac selective β-adrenergic receptor antagonist and a metabolite produced after oral administration of Propranolol (HY-B0573B). 4-Hydroxypropranolol hydrochloride also acts as a membrane stabilizer and possesses intrinsic sympathomimetic inhibitory activity. 4-Hydroxypropranolol hydrochloride blocks β-adrenergic receptors to antagonize the effects of catecholamines, acts as a partial β-adrenergic receptor agonist, and induces membrane stabilization. 4-Hydroxypropranolol hydrochloride alters heart rate, left ventricular contractility, and atrioventricular conduction time. 4-Hydroxypropranolol hydrochloride can be used in research related to cardiovascular and cerebrovascular diseases.

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4-Hydroxypropranolol hydrochloride

4-Hydroxypropranolol hydrochloride 構造式

CAS 番号 : 14133-90-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 247 在庫あり
Solution
10 mM * 1 mL in DMSO USD 247 在庫あり
Solid
5 mg $225 在庫あり
10 mg $360 在庫あり
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4-Hydroxypropranolol hydrochloride 関連抗体

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製品説明

4-Hydroxypropranolol hydrochloride is a non-cardiac selective β-adrenergic receptor antagonist and a metabolite produced after oral administration of Propranolol (HY-B0573B). 4-Hydroxypropranolol hydrochloride also acts as a membrane stabilizer and possesses intrinsic sympathomimetic inhibitory activity. 4-Hydroxypropranolol hydrochloride blocks β-adrenergic receptors to antagonize the effects of catecholamines, acts as a partial β-adrenergic receptor agonist, and induces membrane stabilization. 4-Hydroxypropranolol hydrochloride alters heart rate, left ventricular contractility, and atrioventricular conduction time. 4-Hydroxypropranolol hydrochloride can be used in research related to cardiovascular and cerebrovascular diseases[1][2].

IC50 & Target

β adrenergic receptor

 

体内実験

4-Hydroxypropranolol (54 μg/kg, i.v.) hydrochloride achieves 50% inhibition of Isoprenaline (HY-108353)-induced tachycardia in anesthetized cats[1].
4-Hydroxypropranolol (10-80 μg/kg; i.v.) hydrochloride possesses intrinsic sympathomimetic activity, which causes a dose-dependent increase in heart rate in catecholamine-depleted rats[1].
4-Hydroxypropranolol (0.025-0.8 mg/kg, s.c.) hydrochloride antagonizes the protective effect of isoprenaline against histamine-induced bronchospasm in guinea pigs[1].
4-Hydroxypropranolol (0.09-13.25 mg/kg, i.v.) hydrochloride exerts β-adrenergic receptor blocking activity and membrane-stabilizing activity, thereby producing dose-dependent cardiovascular effects in normal anesthetized dogs, including decreased heart rate, reduced contractility, diminished aortic blood flow, and prolonged atrioventricular conduction time[1].

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

Animal Model: Cat (2-5 kg, anaesthetized with chloralose)[1]
Dosage: 1 μg/kg/min; 2 μg/kg/min; 4 μg/kg/min; 54 μg/kg (50% tachycardia inhibition)
Administration: i.v.; 30 min
Result: Produced 50% reduction in isoprenaline-induced tachycardia at a total dose of 54 μg/kg.
Inhibited isoprenaline-induced vasodepression by 89% at this dose.
Animal Model: Rat (anaesthetized with pentobarbitone sodium, catecholamine-depleted via syrosingopine pretreatment)[1]
Dosage: 10 μg/kg; 80 μg/kg
Administration: i.v.
Result: Produced a dose-dependent increase in heart rate in catecholamine-depleted rats, with mean resting heart rate of 300 beats/minute across 64 rats tested.
Blocked the heart rate increase in response to 10 and 80 μg/kg doses when rats were pretreated with 0.5 mg/kg propranolol.
Animal Model: (either sex, 250-400 g)[1]
Dosage: 0.025 mg/kg; 0.05 mg/kg; 0.8 mg/kg
Administration: s.c.; 15 minutes before isoprenaline exposure
Result: Partially antagonized isoprenaline's protective effect at doses of 0.025 or 0.05 mg/kg, resulting in 50-70% survival from histamine bronchospasm.
Completely antagonized isoprenaline's protection at 0.8 mg/kg, resulting in 0% survival.
Animal Model: male beagle (12-16 kg, anaesthetized with pentobarbitone sodium)[1]
Dosage: 0.09 mg/kg; 0.16 mg/kg; 1.0 mg/kg; 4.0 mg/kg; 8.0 mg/kg (cumulative doses: 0.09, 0.25, 1.25, 5.25, 13.25 mg/kg)
Administration: i.v.
Result: Produced a significant decrease in heart rate (-16.5%), dP/dt (-21.6%), and aortic flow (-10.9%), with no change in mean blood pressure at a cumulative dose of 0.09 mg/kg (unpaced).
Decreased heart rate an additional 6.5% at 0.25 mg/kg cumulative dose, stabilizing at ~-24% of control by 1.25 mg/kg cumulative dose, with no further decreases in dP/dt or aortic flow, and a slight increase in mean blood pressure.
Caused dose-dependent additional decreases in dP/dt (to -52.0% at 13.25 mg/kg), mean blood pressure, heart rate, and aortic flow at cumulative doses of 5.25 and 13.25 mg/kg.
Increased A-V conduction time by 4.8% (unpaced) and 11.9% (paced) at 0.09 mg/kg cumulative dose, remaining elevated until 5.25 and 13.25 mg/kg cumulative doses, which produced marked, dose-dependent additional increases.
分子量

311.80

分子式

C16H22ClNO3
CAS 番号
Appearance

Solid

Color

Light brown to brown

SMILES

OC1=C2C=CC=CC2=C(OCC(O)CNC(C)C)C=C1.Cl[H]
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (320.72 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 3.2072 mL 16.0359 mL 32.0718 mL
5 mM 0.6414 mL 3.2072 mL 6.4144 mL
10 mM 0.3207 mL 1.6036 mL 3.2072 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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  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

V1

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濃度 （終了）

C2

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体積 （終了）

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体内:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.02 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.02 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
参考文献

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 3.2072 mL 16.0359 mL 32.0718 mL 80.1796 mL
5 mM 0.6414 mL 3.2072 mL 6.4144 mL 16.0359 mL
10 mM 0.3207 mL 1.6036 mL 3.2072 mL 8.0180 mL
15 mM 0.2138 mL 1.0691 mL 2.1381 mL 5.3453 mL
20 mM 0.1604 mL 0.8018 mL 1.6036 mL 4.0090 mL
25 mM 0.1283 mL 0.6414 mL 1.2829 mL 3.2072 mL
30 mM 0.1069 mL 0.5345 mL 1.0691 mL 2.6727 mL
40 mM 0.0802 mL 0.4009 mL 0.8018 mL 2.0045 mL
50 mM 0.0641 mL 0.3207 mL 0.6414 mL 1.6036 mL
60 mM 0.0535 mL 0.2673 mL 0.5345 mL 1.3363 mL
80 mM 0.0401 mL 0.2004 mL 0.4009 mL 1.0022 mL
100 mM 0.0321 mL 0.1604 mL 0.3207 mL 0.8018 mL
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4-Hydroxypropranolol hydrochloride Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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Keywords:

4-Hydroxypropranolol14133-90-5(±)-4-hydroxy PropranololAdrenergic ReceptorBeta Receptorcatecholamine-depleted ratsguinea-pigsperfused rat liverβ-adrenoceptoratrioventricular conduction timeanaesthetized dogsrat liver microsomeshistamine bronchospasmleft ventricular contractilityanaesthetized catsInhibitorinhibitorinhibit

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