| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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PZ-128 (PZ128; P1pal-7) is a novel and potent PAR1 (protease-activated receptor-1) antagonist with antiplatelet, anti-metastatic, anti-angiogenic and anticancer activity and has the potential for the treatment of thrombosis. As a cell-penetrating lipopeptide pepducin, PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins.
| ln Vitro |
Ninety-nine percent of OVCAR-4 migration into human ovarian ascites and fibroblast-conditioned media is blocked by PZ-128 (P1pal-7; 3 μM). PZ-128 nearly entirely reduced the 2.2-fold increase in endothelial barrier permeability seen in conditioned media of peritoneal fibroblasts treated with OVCAR4 [1]. Targeting the cytoplasmic surface of PAR1, PZ-128 is a lipidated "pepducin" that obstructs internal G protein signaling. PZ-128's structure was discovered to replicate the closed state of PAR1's equivalent intracellular region, which is essential for coupling to G proteins [3].
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| ln Vivo |
PZ-128 (P1pal-7; 10 mg/kg; intraperitoneal injection; every other day; for 6 weeks) treatment significantly reduced mean ascites volume by 60%. PZ-128 treatment also resulted in a significant 84-96% reduction in vessel density in the center and edges of OVCAR-4 tumors [1].
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| Animal Protocol |
Animal/Disease Models: Female NCR Nu/nu (nude) mice (5-7 weeks) injected with OVCAR-4 or SKOV-3 cells [1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; every other day; for 6 weeks Experimental Results: The average ascites volume was Dramatically diminished by 60%. |
| References |
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| Additional Infomation |
PZ-128 has been used in trials studying the prevention and treatment of Heart Diseases, Coronary Disease, Arteriosclerosis, Vascular Diseases, and Myocardial Ischemia, among others.
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| Molecular Formula |
C55H99N13O9
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|---|---|
| Molecular Weight |
1086.47
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| Exact Mass |
1085.768
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| CAS # |
371131-16-7
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| PubChem CID |
72187679
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.585
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| LogP |
4.95
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
45
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| Heavy Atom Count |
77
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| Complexity |
1750
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| Defined Atom Stereocenter Count |
7
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| 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
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| InChi Key |
VZRIKWNVDCTBTF-BKGFHLQYSA-N
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| InChi Code |
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
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| Chemical 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
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| Synonyms |
PZ 128 PZ128 PZ-128
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~92.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9204 mL | 4.6021 mL | 9.2041 mL | |
| 5 mM | 0.1841 mL | 0.9204 mL | 1.8408 mL | |
| 10 mM | 0.0920 mL | 0.4602 mL | 0.9204 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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