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PZ-128 - 99%, high purity , Proteinase-activated receptor 1 inhibitor, CAS No.371131-16-7, Proteinase-activated receptor 1 inhibitor

COA

Grade & Purity:

≥99%

Cas Number: 371131-16-7
Molecular Weight: 1086.46
PubChem CID: 72187679

In stock

Item Number

P651809

Grouped product items
SKU	Size	Availability	Price
P651809-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$150.90
P651809-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$250.90
P651809-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$500.90
P651809-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$800.90
P651809-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,250.90

View related series

Class A GPCR (4138) GPCR/G Protein (3172) Protease Activated Receptor (PAR) (55)

Basic Description

Synonyms	MS-31946 \| UNII-IYT6MP4NS9 \| PZ 128 \| L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl- \| N-[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-
Specifications & Purity	≥99%
Biochemical and Physiological Mechanisms	PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-
Storage Temp	Desiccated,Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Action Type	INHIBITOR
Mechanism of action	Proteinase-activated receptor 1 inhibitor
Product Description	PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects In Vitro PZ-128 (P1pal-7; 3 μM) blocks 90-94% of OVCAR-4 migration toward human ovarian ascites and fibroblast conditioned media. The OVCAR4-treated peritoneal fibroblast conditioned media elicits a 2.2-fold increase in endothelial barrier permeability which could be nearly completely inhibited by PZ-128. PZ-128 is a lipidated ‘pepducin’ which targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G proteins. The structure of PZ-128 is found to mimic the off-state of the corresponding intracellular region of PAR1 which is critical for coupling to G proteins. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PZ-128 (P1pal-7; 10 mg/kg; intraperitoneal injection; every other day; for 6 weeks) treatment significantly reduces mean ascites fluid volume by 60%. PZ-128 treatment also causes a highly significant 84-96% reduction in blood vessel density in both the center and edge of the OVCAR-4 tumors . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NCR Nu/Nu mice (5-7 weeks) injected with OVCAR-4 or SKOV-3 cells Dosage: 10 mg/kg Administration: Intraperitoneal injection; every other day; for 6 weeks Result: Significantly reduced mean ascites fluid volume by 60%. Form:Solid IC50& Target:PAR1

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Organic acids and derivatives
  - Class Carboxylic acids and derivatives
    - Subclass Amino acids, peptides, and analogues
      - Level5 Peptides
        Level6 Oligopeptides

Kingdom	Organic compounds
Superclass	Organic acids and derivatives
Class	Carboxylic acids and derivatives
Subclass	Amino acids, peptides, and analogues
Intermediate Tree Nodes	Peptides
Direct Parent	Oligopeptides
Alternative Parents	Phenylalanine and derivatives Leucine and derivatives N-acyl-alpha amino acids and derivatives Serine and derivatives Alpha amino acid amides Alanine and derivatives Amphetamines and derivatives N-acyl amines Secondary carboxylic acid amides Guanidines Primary carboxylic acid amides Carboximidamides Propargyl-type 1,3-dipolar organic compounds Organopnictogen compounds Monoalkylamines Primary alcohols Hydrocarbon derivatives Carbonyl compounds Organic oxides
Molecular Framework	Aromatic homomonocyclic compounds
Substituents	Alpha-oligopeptide - Phenylalanine or derivatives - Leucine or derivatives - N-acyl-alpha amino acid or derivatives - Alpha-amino acid amide - Serine or derivatives - Alanine or derivatives - N-substituted-alpha-amino acid - Alpha-amino acid or derivatives - Amphetamine or derivatives - N-acyl-amine - Fatty amide - Monocyclic benzene moiety - Benzenoid - Fatty acyl - Secondary carboxylic acid amide - Primary carboxylic acid amide - Guanidine - Amino acid or derivatives - Carboxamide group - Carboximidamide - Propargyl-type 1,3-dipolar organic compound - Organic 1,3-dipolar compound - Alcohol - Primary aliphatic amine - Organonitrogen compound - Organooxygen compound - Primary alcohol - Carbonyl group - Primary amine - Hydrocarbon derivative - Organic oxide - Amine - Organopnictogen compound - Organic oxygen compound - Organic nitrogen compound - Aromatic homomonocyclic compound
Description	This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

Names and Identifiers

IUPAC Name	N-[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]hexadecanamide
INCHI	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
InChIKey	VZRIKWNVDCTBTF-BKGFHLQYSA-N
Smiles	CCCCCCCCCCCCCCCC(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(C)C(=O)NC(CC(C)C)C(=O)NC(CC1=CC=CC=C1)C(=O)N
Isomeric SMILES	CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(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(=O)N
Alternate CAS	371131-16-7
PubChem CID	72187679
MeSH Entry Terms	P1pal-7;PZ-128 peptide
Molecular Weight	1086.46

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	DMSO : 100 mg/mL (92.04 mM; Need ultrasonic)
Molecular Weight	1086.500 g/mol
XLogP3	4.900
Hydrogen Bond Donor Count	13
Hydrogen Bond Acceptor Count	12
Rotatable Bond Count	45
Exact Mass	1085.77 Da
Monoisotopic Mass	1085.77 Da
Topological Polar Surface Area	383.000 Å²
Heavy Atom Count	77
Formal Charge	0
Complexity	1750.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	7
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

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