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Details

Stereochemistry ABSOLUTE
Molecular Formula C55H99N13O9
Molecular Weight 1086.4563
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PZ-128

SMILES

CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CC=CC=C1)C(N)=O

InChI

InChIKey=VZRIKWNVDCTBTF-BKGFHLQYSA-N
InChI=1S/C55H99N13O9/c1-5-6-7-8-9-10-11-12-13-14-15-16-20-31-47(70)63-41(28-21-23-32-56)51(74)64-42(29-22-24-33-57)52(75)68-46(37-69)54(77)65-43(30-25-34-61-55(59)60)50(73)62-39(4)49(72)67-45(35-38(2)3)53(76)66-44(48(58)71)36-40-26-18-17-19-27-40/h17-19,26-27,38-39,41-46,69H,5-16,20-25,28-37,56-57H2,1-4H3,(H2,58,71)(H,62,73)(H,63,70)(H,64,74)(H,65,77)(H,66,76)(H,67,72)(H,68,75)(H4,59,60,61)/t39-,41-,42-,43-,44-,45-,46-/m0/s1

HIDE SMILES / InChI
PZ-128 (also known as P1pal7 ) is a cell-penetrating pepducin inhibitor of PAR1 that targets the receptor-G-protein interface on the inside surface of platelets. In preclinical studies, PZ-128 suppresses PAR1 aggregation and arterial thrombosis in guinea pigs and baboons and strongly synergized with oral clopidogrel. PZ-128 shows potent anti-metastatic and anti-angiogenic activity in Breast, Ovarian, and Lung Cancer preclinical studies. In clinical trials, PZ-128 shows a promising antiplatelet activity that provides rapid, specific, dose-dependent, and reversible inhibition of platelet protease-activated receptor-1 through a novel intracellular mechanism.

Approval Year

PubMed

PubMed

TitleDatePubMed
Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease.
2016 Jan
Patents

Patents

Sample Use Guides

continuous intravenous infusion 0.01-2 mg/kg
Route of Administration: Intravenous
Name Type Language
PZ-128
Common Name English
L-PHENYLALANINAMIDE, N2-(1-OXOHEXADECYL)-L-LYSYL-L-LYSYL-L-SERYL-L-ARGINYL-L-ALANYL-L-LEUCYL-
Systematic Name English
PALMITATE-KKSRALF-NH2
Common Name English
Code System Code Type Description
FDA UNII
IYT6MP4NS9
Created by admin on Sat Dec 16 10:58:36 GMT 2023 , Edited by admin on Sat Dec 16 10:58:36 GMT 2023
PRIMARY
CAS
371131-16-7
Created by admin on Sat Dec 16 10:58:36 GMT 2023 , Edited by admin on Sat Dec 16 10:58:36 GMT 2023
PRIMARY
PUBCHEM
72187679
Created by admin on Sat Dec 16 10:58:36 GMT 2023 , Edited by admin on Sat Dec 16 10:58:36 GMT 2023
PRIMARY
DRUG BANK
DB11839
Created by admin on Sat Dec 16 10:58:36 GMT 2023 , Edited by admin on Sat Dec 16 10:58:36 GMT 2023
PRIMARY