PZ-128, 蛋白酶激活受体 1 抑制剂

蛋白质

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-

PZ-128

P651809-5mg

5mg

≥99%

干燥,-80℃储存

超低温冰袋运输

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

PZ-128（P1pal-7）是一种细胞穿透性脂肽蛋白肽，是第一类特异性可逆蛋白酶激活受体-1（PAR1）拮抗剂。PZ-128 以 PAR1 的细胞质表面为靶点，中断向内部定位的 G（PAR1-7）发出信号。

371131-16-7

C55H99N13O9

1086.46 g/mol

72187679

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

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

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

VZRIKWNVDCTBTF-BKGFHLQYSA-N

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

72187679

371131-16-7

P1pal-7;PZ-128 peptide

DMSO : 100 mg/mL (92.04 mM; Need ultrasonic)

13

12

45

1085.77 Da

1085.77 Da

383.000 Ų

77

0

1750.000

0

1

4.900

4.9

抑制剂

蛋白酶激活受体 1 抑制剂