1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Piclamilast

Piclamilast (Synonyms: RP 73401; RPR 73401)

Cat. No.: HY-12887
Handling Instructions

Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively.

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

Piclamilast Chemical Structure

Piclamilast Chemical Structure

CAS No. : 144035-83-6

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively[1][2][3][4].

IC50 & Target[4]

PDE4

16 nM (IC50, in pig aorta)

PDE4

2 nM (IC50, in eosinophil soluble)

PDE1

>100 μM (IC50)

PDE2

40 μM (IC50)

PDE3

>100 μM (IC50)

PDE5

14 μM (IC50)

In Vitro

Piclamilast (RP 73401, 1 μM, 30 min) significantly inhibits the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63[2].
Piclamilast (RP 73401) exhibits IC50 values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4].

RT-PCR[2]

Cell Line: Human A549 type II lung epithelial cells.
Concentration: 1 μM (H2O2 200 μM).
Incubation Time: 30 min.
Result: Prevented H2O2 -induced changes in gene expression levels in A549 cells.

Cell Viability Assay[3]

Cell Line: NB4 cells.
Concentration: 30 μM.
Incubation Time: 3 days.
Result: Exerted a significant enhancing effect on the induction of STAT1 observed in ATRA-treated NB4 cells.
Caused a significant increase in the number of cells expressing NBT-R activity.
In Vivo

Piclamilast (RP 73401, 10 mg/kg, 30 min) alone does not affect the MST of leukemia-bearing animals. Piclamilast combined with ATRA (HY-14649) significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals[3].

Animal Model: SCID mice[3].
Dosage: 10 mg/kg (combined with ATRA (HY-14649)).
Administration: Injection daily.
Result: Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.
Molecular Weight

381.25

Formula

C₁₈H₁₈Cl₂N₂O₃

CAS No.

144035-83-6

SMILES

O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC)C(OC3CCCC3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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.
  • 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

Keywords:

PiclamilastRP 73401RPR 73401RP73401RP-73401RPR73401RPR-73401Phosphodiesterase (PDE)AMLphosphodiesterasePDEcAMPATRARARInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Piclamilast
Cat. No.:
HY-12887
Quantity:
MCE Japan Authorized Agent: