1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)
  3. PZ-128

PZ-128 (Synonyms: P1pal-7)

Cat. No.: HY-107146 Purity: 99.47%
Handling Instructions

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.

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

PZ-128 Chemical Structure

PZ-128 Chemical Structure

CAS No. : 371131-16-7

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10 mM * 1 mL in DMSO USD 299 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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[1][2][3][4].

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[1].
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[3].

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[1].

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[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; every other day; for 6 weeks
Result: Significantly reduced mean ascites fluid volume by 60%.
Molecular Weight

1086.46

Formula

C₅₅H₉₉N₁₃O₉

CAS No.

371131-16-7

Sequence Shortening

{Palmitate}-KKSRALF-NH2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
References

Purity: 99.47%

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Keywords:

PZ-128P1pal-7PZ128PZ 128Protease-Activated Receptor (PAR)Thrombin receptorsPAR1antiplateletlipopeptidecell-penetratingreversibleanti-metastaticanti-angiogenicanticancerInhibitorinhibitorinhibit

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Product Name:
PZ-128
Cat. No.:
HY-107146
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