Absorption, Distribution and Excretion
90%. Metabolites are primarily excreted in urine. Approximately 90% of metabolites are excreted in urine. Metabolism/Metabolites In the liver, metabolites undergo hydroxylation and glucuronide conjugation to form glucuronide metabolites and semi-active 4-hydroxy metabolites. Biological Half-Life The plasma half-life is approximately 5 hours; the bound half-life is approximately 20 hours in healthy individuals, approximately 25 hours in healthy elderly individuals, and approximately 100 hours in patients undergoing kidney dialysis.

Hepatotoxicity
In patients taking pentbuprofen, the incidence of mild to moderate elevations in serum transaminase levels is less than 2%, usually transient and asymptomatic, and returns to normal with continued treatment. Despite its widespread use, there is no conclusive evidence that pentbuprofen is associated with clinically significant liver injury. Other beta-blockers have been associated with rare cases of acute liver injury with a latency period of 4 to 24 weeks, characterized by hepatocellular elevations of serum enzymes, a milder course, self-limiting nature, and no evidence of hypersensitivity or autoimmune reactions. Probability score: E (unlikely a cause of clinically significant liver injury). Pregnancy and Lactation Effects ◉ Overview of Use During Lactation Penbutolol is not marketed in the United States. Based on its physicochemical properties, the risk of pentbuprofen to breastfed infants appears to be low. Since there is currently no published experience regarding the use of pentbuprofen during breastfeeding, other medications may be preferred, especially in breastfed newborns or preterm infants.
◉ Effects on Breastfed Infants
As of the revision date, no published information was found regarding penteprolol. A study of mothers taking beta-blockers while breastfeeding found a numerically increased number of adverse events, but this was not statistically significant. Although the infants were age-matched to control groups, the age of affected infants was not specified. None of the mothers were taking penteprolol.
◉ Effects on Lactation and Breast Milk
As of the revision date, no published information was found regarding the effects of beta-blockers or penteprolol on normal breastfeeding. A study of six patients with hyperprolactinemia and galactorrhea found no change in serum prolactin levels after beta-adrenergic blockade with propranolol.

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Protein Binding
80-98% bound to plasma proteins. Extensively bound to α1-acid glycoprotein 1.

Penbutolol belongs to the ethanolamine class of drugs. Penbutolol is a beta-blocker used to treat hypertension. It binds to both β1 and β2 adrenergic receptors, making it a non-selective beta-blocker. As a sympathomimetic drug, it acts as a partial agonist of beta-adrenergic receptors. Penbutolol also has a high affinity for and antagonistic effect on serotonin receptor 1A. The application of this binding property in antidepressant treatment is currently under investigation. Penbutolol is contraindicated in patients with cardiogenic shock, sinus bradycardia, second- or third-degree atrioventricular block, bronchial asthma, and those with known hypersensitivity to Penbutolol. Penbutolol is a beta-adrenergic blocker. Its mechanism of action is as a beta-adrenergic receptor antagonist.
Pemprolol is a non-selective β-adrenergic receptor blocker (β-blocker) used to treat hypertension. Currently, there is no conclusive evidence that penteprolol is associated with clinically significant liver damage.
There are reports on the effects of penteprolol in C. elegans, and relevant data are available.
Pemprolol is a lipophilic, non-selective β-adrenergic receptor antagonist with antianginal and antihypertensive effects. Penprolol competitively binds to and blocks the action of β1-adrenergic receptors in the heart, thereby reducing myocardial contractility and heart rate. This leads to a decrease in cardiac output and a reduction in blood pressure. Furthermore, penteprolol inhibits the release of renin, a hormone secreted by the kidneys that causes vasoconstriction.
Pemprolol is a non-selective β-blocker used as an antihypertensive and antianginal drug.
Drug Indications

Pemprolol is indicated for the treatment of mild to moderate hypertension.
It can be used alone or in combination with other antihypertensive drugs, especially thiazide diuretics. Penbutolol is contraindicated in patients with cardiogenic shock, sinus bradycardia, second- or third-degree atrioventricular block, bronchial asthma, and those with known hypersensitivity to pentbuprofen.
FDA Label

Mechanism of Action

Pentbuprofen acts on β1-adrenergic receptors in the heart and kidneys. When catecholamines activate β1 receptors, they stimulate a coupled G protein, leading to the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). The increase in cAMP activates protein kinase A (PKA), thereby altering the movement of calcium ions in the myocardium and increasing heart rate. Penbutolol blocks the activation of β1-adrenergic receptors by catecholamines, reducing heart rate and thus lowering blood pressure.
Pharmacodynamics

Pentbuprofen is a β1, β2 (non-selective) adrenergic receptor antagonist.
Experimental studies have shown that intravenous injection of 0.25 to 1.0 mg/kg of pentbuprofen in reserpine-depleted rats can induce a dose-dependent increase in heart rate, suggesting that pentbuprofen possesses certain intrinsic sympathomimetic activity. However, in human studies, the decrease in heart rate was similar to that observed after administration of propranolol.

(C18H29NO2)2.H2SO4

680.94

291.219

38363-32-5

38363-40-5;38363-32-5 (sulfate);

37464

White to off-white solid powder

438.2ºC at 760mmHg

216-218℃ (Decomposition)

218.8ºC

3.862

2

3

7

21

294

1

CC(C)(C)NC[C@@H](COC1=CC=CC=C1C2CCCC2)O

KQXKVJAGOJTNJS-HNNXBMFYSA-N

InChI=1S/C18H29NO2/c1-18(2,3)19-12-15(20)13-21-17-11-7-6-10-16(17)14-8-4-5-9-14/h6-7,10-11,14-15,19-20H,4-5,8-9,12-13H2,1-3H3/t15-/m0/s1

(2S)-1-(tert-butylamino)-3-(2-cyclopentylphenoxy)propan-2-ol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~1.67 mg/mL (~4.90 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)