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

PAT-505 

Cat. No.: HY-107781
Handling Instructions

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.

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

PAT-505 Chemical Structure

PAT-505 Chemical Structure

CAS No. : 1782070-22-7

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

IC50: 2 nM (Autotaxin, Hep3B cell), 9.7 nM (Autotaxin, Human blood), 62 nM (Autotaxin, Mouse plasma)[1]

In Vitro

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. 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[1].

In Vivo

PAT-505 suppresses ATX lysoPLD activity with an average IC50 value of 62 nM and an average IC90 value of 630 nM in mouse plasma, and the IC90 in rat plasma is ∼770 nM. 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)[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1101 mL 10.5503 mL 21.1006 mL
5 mM 0.4220 mL 2.1101 mL 4.2201 mL
10 mM 0.2110 mL 1.0550 mL 2.1101 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
NASH is induced in male C57BL/6 mice. Briefly, 5-week-old mice are acclimated for 1 week on normal chow before switching to a choline-deficient, l-amino acid-defined, high-fat diet (CDAHFD) containing 60% kcal% fat and 0.1% methionine. After 4 weeks of CDAHFD feeding, approximately 200 μL of blood is collected from each animal via a submandibular bleed and the serum analyzed for liver enzyme levels. Any animal with a total serum bilirubin level >1 mg/dL is removed from the study prior to compound dosing. Animals are fed CDAHFD for 5 weeks before randomization into treatment groups (n = 7-10 per group). Vehicle or PAT-505 (3-30 mg/kg) is administered by oral gavage in 0.5% methylcellulose (MC) once daily from weeks 5 to 12[1].

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

References
Molecular Weight

473.92

Formula

C₂₃H₁₈ClF₂N₃O₂S

CAS No.

1782070-22-7

SMILES

O=C(O)C1=CC=CC(SC2=C(C3CC3)N(C4=CN(CC)N=C4)C5=C2C=CC(Cl)=C5F)=C1F

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PAT-505
Cat. No.:
HY-107781
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PAT-505

Cat. No.: HY-107781