2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Pelrinone

Pelrinone is an orally active cardiotonic agent and PDE III inhibitor with an IC50 of 36 μM. Pelrinone elevates intracellular cAMP levels. The action of Pelrinone is independent of β-adrenergic receptors, and it does not inhibit Na+/K+-ATPase. Pelrinone exerts positive inotropic and vasodilatory effects. Pelrinone inhibits platelet aggregation, reduces thrombus formation, and exerts weak anticoagulant activity without altering hematocrit or circulating platelet counts. Pelrinone can be used in research related to congestive heart failure and coronary thrombosis.

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

Pelrinone

Pelrinone Chemical Structure

CAS No. : 94386-65-9

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of Pelrinone:

Pelrinone Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pelrinone is an orally active cardiotonic agent and PDE III inhibitor with an IC50 of 36 μM. Pelrinone elevates intracellular cAMP levels. The action of Pelrinone is independent of β-adrenergic receptors, and it does not inhibit Na+/K+-ATPase. Pelrinone exerts positive inotropic and vasodilatory effects. Pelrinone inhibits platelet aggregation, reduces thrombus formation, and exerts weak anticoagulant activity without altering hematocrit or circulating platelet counts. Pelrinone can be used in research related to congestive heart failure and coronary thrombosis[1][2][3].

IC50 & Target[1]

PDE Ⅲ

36 μM (IC50)

In Vitro

Pelrinone inhibits PDE in crude bovine heart extracts with an IC50 of 76 μM; it also inhibits purified bovine heart PDE component III with an IC50 of 36 μM, exhibiting stronger activity against the cAMP-specific component III isozyme[1].
Pelrinone (at different concentrations; pre-incubated for 3 min) inhibits platelet-rich plasma aggregation induced by Arachidonic acid (HY-109590), U46619 (HY-108566), Collagen, phase II adrenaline, and phase II adenosine diphosphate, with IC50 values of 2.8, 6.6, 13.3, 18.6, and 11.8 μM, respectively[2].

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

Pelrinone Related Antibodies
In Vivo

Pelrinone (0.01-1.0 mg/kg; intravenous injection; once every 30 min; 0.2 mg/kg; intraduodenal administration) produces dose-dependent positive inotropic effects and mild vasodilatory effects in pentobarbital-induced heart failure anesthetized dogs. The ED20/ED50 ratio is 4 for intravenous administration and >15 for intraduodenal administration, indicating that enteral administration has higher cardiac specificity[1].
Pirrinone (2.0 mg/kg; p.o.; single administration) enhances left ventricular contractility, increases heart rate, and transiently reduces blood pressure in conscious dogs[1].
Pelnirone (0.25-5.00 mg/kg; intravenous injection; single bolus) dose-dependently inhibits white thrombus formation in a rabbit arteriovenous shunt model, with an inhibition rate of 76.7% at the highest tested dose of 5.00 mg/kg i.v[2].
Pirfenidone (0.625-2.5 mg/kg; intravenous injection; 10% bolus, 90% continuous infusion for 4.5 h) exerts antithrombotic activity in a canine coronary thrombosis model, inhibits epinephrine-sensitized platelet aggregation, and produces dose-dependent hemodynamic effects, including hypotension, tachycardia, and increased myocardial contractility[3].

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

Animal Model: Unselected breed/sex, 10-20 kg (pentobarbital-induced congestive heart failure)[1]
Dosage: 0.01-1.0 mg/kg (i.v.); 0.2 mg/kg (i.d.)
Administration: i.v. (every 30 minutes, non-cumulative); i.d. (single dose)
Result: Achieved an ED50 of 0.03 mg/kg for increasing peak positive dP/dt by 50% and an ED20 of 0.12 mg/kg for reducing mean arterial blood pressure by 20% via intravenous administration, resulting in an ED20/ED50 ratio of 4.
Produced a dose-related increase in myocardial contractility (dP/dt max) from 11% to 222% relative to failed control via intravenous doses of 0.01-1.0 mg/kg.
Produced a dose-related increase in heart rate from 4% to 52% relative to failed control via intravenous doses of 0.01-1.0 mg/kg.
Produced a dose-related reduction in mean aortic blood pressure from 0 to 38% relative to failed control via intravenous doses of 0.01-1.0 mg/kg.
Achieved an ED50 of 0.2 mg/kg for increased dP/dt and an ED20 of >3 mg/kg for blood pressure reduction via intraduodenal administration, resulting in an ED20/ED50 ratio of >15.
Animal Model: Unselected breed/sex, with chronically implanted Konigsberg left ventricular pressure transducers[1]
Dosage: 2.0 mg/kg
Administration: p.o. (single dose; monitored for 6 hours)
Result: Showed a slightly more rapid onset of action and longer duration of action compared to milrinone and compound 49.
Increased heart rate and decreased mean blood pressure that lasted during the first 2.5 hours post-dosing.
Increased left ventricular dP/dt.
Animal Model: New Zealand rabbits (male, 2.0-2.5 kg)[2]
Dosage: 0.25 mg/kg; 0.50 mg/kg; 1.00 mg/kg; 5.00 mg/kg
Administration: i.v.; single bolus
Result: Reduced white thrombus formation (platelet accretion) by 7.3% at 0.25 mg/kg.
Reduced white thrombus formation (platelet accretion) by 41.7% at 0.50 mg/kg.
Reduced white thrombus formation (platelet accretion) by 56.8% at 1.00 mg/kg.
Reduced white thrombus formation (platelet accretion) by 76.7% at 5.00 mg/kg.
Molecular Weight

241.25

Formula

C12H11N5O
CAS No.
SMILES

N#CC=1C(=O)N=C(NC1NCC=2C=NC=CC2)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Pelrinone Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

Pelrinone94386-65-9Phosphodiesterase (PDE)PDE IIIcoronary artery thrombosishuman platelet-rich plasmacAMP phosphodiesteraseNa+/K+-ATPaserabbit arteriovenous shunt modelanesthetized dogsβ-adrenergic receptorscongestive heart failurethrombosisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Pelrinone
Cat. No.:
HY-106830
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.