1. MAPK/ERK Pathway
  2. p38 MAPK
  3. PF-03715455

PF-03715455 

Cat. No.: HY-18862
Handling Instructions

PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease).

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

PF-03715455 Chemical Structure

PF-03715455 Chemical Structure

CAS No. : 1056164-52-3

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Description

PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease)[1][2].

IC50 & Target[1]

p38α

0.88 nM (IC50)

p38β

23 nM (IC50)

In Vitro

PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4[2].

In Vivo

PF-03715455 treatment shows that the Vss and T1/2 are 0.19 L/kg, 1 hour, respectively[2].

Animal Model: Male CD Sprague Dawley rats (300-450 g)[2]
Dosage: 1 mg/kg
Administration: I.v. (Pharmacokinetic Analysis)
Result: The Vss, and T1/2 were 0.19 L/kg, 1 hour, respectively.
Molecular Weight

700.27

Formula

C₃₅H₃₄ClN₇O₃S₂

CAS No.

1056164-52-3

SMILES

CC(C)(C1=NN(C2=CC=C(O)C(Cl)=C2)C(NC(NCC3=CC=CC=C3SC4=CN5C(C6=CC=CC=C6SCCO)=NN=C5C=C4)=O)=C1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PF-03715455PF03715455PF 03715455p38 MAPKselectivityCOPDLPSTNFαproductioninhaledairwayinflammationInhibitorinhibitorinhibit

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PF-03715455
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HY-18862
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