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Details

Stereochemistry ABSOLUTE
Molecular Formula C25H36F3N5O3
Molecular Weight 511.5802
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PF-04634817

SMILES

CO[C@@H]1COCC[C@@H]1N[C@@H]2CC[C@](C2)(C(C)C)C(=O)N3C[C@@H]4C[C@H]3CN4C5=NC=NC(=C5)C(F)(F)F

InChI

InChIKey=MCRWZBYTLVCCJJ-DKALBXGISA-N
InChI=1S/C25H36F3N5O3/c1-15(2)24(6-4-16(10-24)31-19-5-7-36-13-20(19)35-3)23(34)33-12-17-8-18(33)11-32(17)22-9-21(25(26,27)28)29-14-30-22/h9,14-20,31H,4-8,10-13H2,1-3H3/t16-,17+,18+,19+,20-,24+/m1/s1

HIDE SMILES / InChI

Molecular Formula C25H36F3N5O3
Molecular Weight 511.5802
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 6 / 6
E/Z Centers 0
Optical Activity UNSPECIFIED

PF-04634817 is a small molecule chemokine CCR2 and CCR5 receptor dual antagonist. Treatment with PF-04634817 was associated with a modest improvement in best-corrected visual acuity, which was inferior to intravitreal ranibizumab. Analysis of the primary endpoint, Urine Albumin-to-Creatinine Ratio, indicated a modest effect of PF-04634817 in reducing albuminuria in subjects with type 2 diabetes who received angiotensin receptor blocker therapy after 12 weeks of treatment. Despite the tolerable safety profile shown by PF-04634817, clinical development was discontinued in light of the modest efficacy observed.

Approval Year

PubMed

PubMed

TitleDatePubMed
Effect of PF-04634817, an Oral CCR2/5 Chemokine Receptor Antagonist, on Albuminuria in Adults with Overt Diabetic Nephropathy.
2018 Nov

Sample Use Guides

200 mg once daily
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Tue Apr 01 16:38:03 GMT 2025
Edited
by admin
on Tue Apr 01 16:38:03 GMT 2025
Record UNII
51M3FB9B9E
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
1,5-ANHYDRO-2,3-DIDEOXY-4-O-METHYL-3-(((1R,3S)-3-(1-METHYLETHYL)-3-(((1S,4S)-5-(6-(TRIFLUOROMETHYL)-4-PYRIMIDINYL)-2,5-DIAZABICYCLO(2.2.1)HEPT-2-YL)CARBONYL)CYCLOPENTYL)AMINO)-D-ERYTHRO-PENTITOL
Preferred Name English
PF-04634817
Common Name English
D-ERYTHRO-PENTITOL, 1,5-ANHYDRO-2,3-DIDEOXY-4-O-METHYL-3-(((1R,3S)-3-(1-METHYLETHYL)-3-(((1S,4S)-5-(6-(TRIFLUOROMETHYL)-4-PYRIMIDINYL)-2,5-DIAZABICYCLO(2.2.1)HEPT-2-YL)CARBONYL)CYCLOPENTYL)AMINO)-
Systematic Name English
Code System Code Type Description
SMS_ID
300000041328
Created by admin on Tue Apr 01 16:38:03 GMT 2025 , Edited by admin on Tue Apr 01 16:38:03 GMT 2025
PRIMARY
DRUG BANK
DB14955
Created by admin on Tue Apr 01 16:38:03 GMT 2025 , Edited by admin on Tue Apr 01 16:38:03 GMT 2025
PRIMARY
FDA UNII
51M3FB9B9E
Created by admin on Tue Apr 01 16:38:03 GMT 2025 , Edited by admin on Tue Apr 01 16:38:03 GMT 2025
PRIMARY
PUBCHEM
46198579
Created by admin on Tue Apr 01 16:38:03 GMT 2025 , Edited by admin on Tue Apr 01 16:38:03 GMT 2025
PRIMARY
CAS
1228111-63-4
Created by admin on Tue Apr 01 16:38:03 GMT 2025 , Edited by admin on Tue Apr 01 16:38:03 GMT 2025
PRIMARY
ChEMBL
CHEMBL3545032
Created by admin on Tue Apr 01 16:38:03 GMT 2025 , Edited by admin on Tue Apr 01 16:38:03 GMT 2025
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
BINDING
IC50
OFF TARGET->NON-INHIBITOR
Related Record Type Details
ACTIVE MOIETY