A CCR2 antagonist (IC50s = 5.2

PF-4136309 – 10 mg

Brand:
Cayman
CAS:
1341224-83-6
Storage:
-20
UN-No:
Non-Hazardous - /

PF-4136309 is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively).{53022} It also inhibits the voltage-gated potassium channel subtype Kv11.1 by 35% when used at a concentration of 10 µM. PF-4136309 decreases isolated human monocyte chemotaxis induced by chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 3.9 nM.  

 

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Description

A CCR2 antagonist (IC50s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively); inhibits the voltage-gated potassium channel subtype Kv11.1 by 35% at 10 µM; decreases CCL2 induced chemotaxis of isolated human monocytes (IC50 = 3.9 nM)

Formal name: N-[2-[(3S)-3-[[trans-4-hydroxy-4-[5-(2-pyrimidinyl)-2-pyridinyl]cyclohexyl]amino]-1-pyrrolidinyl]-2-oxoethyl]-3-(trifluoromethyl)-benzamide

Synonyms:  INCB 8761

Molecular weight: 568.6

CAS: 1341224-83-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Innate Immunity

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