Free shipping on all orders over $ 500

PAT-505

Cat. No. M11452
PAT-505  Structure
Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma, respectively. 

PAT-505 is selective for ATX versus other ENPP proteins, and shows marginal inhibition of radiolabeled agonist or antagonist binding to the adenosine A3 receptor, MT1 melatonin receptor, prostaglandin E2 EP4 receptor, 5-HT5a serotonin receptor, and GABA-gated Cl- channel with 50%-70% inhibition at 10 µM. 

In vivo, PAT-505 (30 mg/kg, p.o.) significantly reduces fibrotic score, the percentage of PSR-positive area, and α-SMA immunoreactivity in mouse model of nonalcoholic steatohepatitis (NASH).

Chemical Information
Molecular Weight 473.92
Formula C23H18ClF2N3O2S
CAS Number 1782070-22-7
Solubility (25°C) DMSO 45 mg/mL
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] Gretchen Bain, et al. J Pharmacol Exp Ther. Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis

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: PAT-505 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.