Free shipping on all orders over $ 500

Piclamilast

Cat. No. M1906
Piclamilast Structure
Synonym:

RP 73401

Size Price Availability Quantity
10mg USD 200  USD200 In stock
50mg USD 680  USD680 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Piclamilast (RP 73401) is a selective PDE4 inhibitor with IC50 of 1 nM at PDE4 from human neutrophils. Inhibition of PDE4 blocks hydrolysis of cAMP thereby increasing levels of cAMP within cells. cAMP suppresses the activity of immune and inflammatory cells. Piclamilast also inhibits LTB4 synthesis in human neutrophils with IC50 of 2 nM. PDE4 inhibitor Piclamilast (RP 73401) displays >19,000-fold selectivity over other PDE isoenzymes. It is comparable to other PDE4 inhibitors for its anti-inflammatory effects. Piclamilast pre-treatment significantly inhibited the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63.

Chemical Information
Molecular Weight 381.25
Formula C18H18Cl2N2O3
CAS Number 144035-83-6
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mata M, et al. Free Radic Res. Piclamilast inhibits the pro-apoptotic and anti-proliferative responses of A549 cells exposed to H(2)O(2) via mechanisms involving AP-1 activation.

Related PDE Products
ME-3183

ME-3183 is an oral selective PDE4 inhibitor with anti-inflammatory activity for studies related to plaque psoriasis.

ART-648

ART-648 is a PDE4 inhibitor that may be used in studies related to non-alcoholic steatohepatitis.

(E/Z)-HA155

(E/Z)-HA155 is a potent Autotaxin (ATX) type I inhibitor for studies related to cancer, fibrous disorders, inflammation, pain and angiogenesis.

Autotaxin-IN-3

Autotaxin-IN-3 is an Autotaxin(ATX) inhibitor with an IC50 value of 2.4 nM.

HA155

HA155 is a potent and selective ATX inhibitor with an IC50 value of 5.7 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: Piclamilast, RP 73401 supplier, PDE, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.