Need Assistance?

US & Canada:
+
UK: +

Our Highlights

GMP Grade Efficient workshop for GMP production.
Optimal Prices Buying products on this site guarantees the best price!
Commercial Batches Independent GMP manufacturing suites that handle commercial batches
Prompt Delivery Warehouses in multiple cities to ensure timely delivery
Flexible Quantity Quantities available from milligrams to ton

Parstatin (human)

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

Parstatin is a 41-amino acid peptide, formed by proteolytic cleavage on activation of the protease activated receptor-1, with antiangiogenic properties. Parstatin (human) attenuates endothelial cell migration and proliferation (IC50 ~ 3 μM), and induces cell cycle arrest. It promotes activation of caspase-3 and exhibits pro-apoptotic activity in vitro.

Category

Functional Peptides

Catalog number

BAT-013363

CAS number

1065755-99-8

Molecular Formula

C191H330N64O53S3

Molecular Weight

4467.29

Specification
Reference Reading

IUPAC Name

(4S)-5-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(1S)-4-carbamimidamido-1-carboxybutyl]carbamoyl]pyrrolidin-1-yl]-3-carboxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]propanoyl]amino]-3-sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid

Synonyms

H-Met-Gly-Pro-Arg-Arg-Leu-Leu-Leu-Val-Ala-Ala-Cys-Phe-Ser-Leu-Cys-Gly-Pro-Leu-Leu-Ser-Ala-Arg-Thr-Arg-Ala-Arg-Arg-Pro-Glu-Ser-Lys-Ala-Thr-Asn-Ala-Thr-Leu-Asp-Pro-Arg-OH; L-methionyl-glycyl-L-prolyl-L-arginyl-L-arginyl-L-leucyl-L-leucyl-L-leucyl-L-valyl-L-alanyl-L-alanyl-L-cysteinyl-L-phenylalanyl-L-seryl-L-leucyl-L-cysteinyl-glycyl-L-prolyl-L-leucyl-L-leucyl-L-seryl-L-alanyl-L-arginyl-L-threonyl-L-arginyl-L-alanyl-L-arginyl-L-arginyl-L-prolyl-L-alpha-glutamyl-L-seryl-L-lysyl-L-alanyl-L-threonyl-L-asparagyl-L-alanyl-L-threonyl-L-leucyl-L-alpha-aspartyl-L-prolyl-L-arginine

Related CAS

1065756-01-5 (mouse)

Appearance

White Lyophilized Solid

Purity

≥98%

Sequence

MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPR

Storage

Store at -20°C

Solubility

Soluble in Water (1 mg/ml)

InChI

InChI=1S/C191H330N64O53S3/c1-90(2)73-118(233-158(281)112(48-34-63-211-187(199)200)226-156(279)113(49-35-64-212-188(201)202)228-174(297)133-53-39-68-252(133)138(263)83-216-152(275)108(193)59-72-311-26)162(285)234-119(74-91(3)4)163(286)236-124(79-96(13)14)169(292)248-142(97(15)16)178(301)223-98(17)146(269)218-99(18)149(272)246-132(89-310)173(296)238-125(80-107-43-28-27-29-44-107)168(291)245-130(87-258)172(295)237-121(76-93(7)8)167(290)247-131(88-309)153(276)217-84-139(264)253-69-40-54-134(253)175(298)239-122(77-94(9)10)164(287)235-120(75-92(5)6)166(289)244-128(85-256)170(293)222-101(20)148(271)225-114(50-36-65-213-189(203)204)160(283)251-145(106(25)261)179(302)230-110(46-32-61-209-185(195)196)155(278)219-100(19)147(270)224-111(47-33-62-210-186(197)198)157(280)231-116(51-37-66-214-190(205)206)182(305)254-70-41-55-135(254)176(299)229-115(57-58-140(265)266)159(282)243-129(86-257)171(294)227-109(45-30-31-60-192)154(277)220-102(21)150(273)250-144(105(24)260)181(304)241-126(81-137(194)262)161(284)221-103(22)151(274)249-143(104(23)259)180(303)240-123(78-95(11)12)165(288)242-127(82-141(267)268)183(306)255-71-42-56-136(255)177(300)232-117(184(307)308)52-38-67-215-191(207)208/h27-29,43-44,90-106,108-136,142-145,256-261,309-310H,30-42,45-89,192-193H2,1-26H3,(H2,194,262)(H,216,275)(H,217,276)(H,218,269)(H,219,278)(H,220,277)(H,221,284)(H,222,293)(H,223,301)(H,224,270)(H,225,271)(H,226,279)(H,227,294)(H,228,297)(H,229,299)(H,230,302)(H,231,280)(H,232,300)(H,233,281)(H,234,285)(H,235,287)(H,236,286)(H,237,295)(H,238,296)(H,239,298)(H,240,303)(H,241,304)(H,242,288)(H,243,282)(H,244,289)(H,245,291)(H,246,272)(H,247,290)(H,248,292)(H,249,274)(H,250,273)(H,251,283)(H,265,266)(H,267,268)(H,307,308)(H4,195,196,209)(H4,197,198,210)(H4,199,200,211)(H4,201,202,212)(H4,203,204,213)(H4,205,206,214)(H4,207,208,215)/t98-,99-,100-,101-,102-,103-,104+,105+,106+,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,142-,143-,144-,145-/m0/s1

InChI Key

PSNCGLAAPGGYMJ-YLKYZDBHSA-N

Canonical SMILES

CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)N1CCCC1C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C)C(=O)NC(C(C)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)O)C(=O)N2CCCC2C(=O)NC(CCCNC(=N)N)C(=O)O)NC(=O)C3CCCN3C(=O)CNC(=O)C(CS)NC(=O)C(CC(C)C)NC(=O)C(CO)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CS)NC(=O)C(C)NC(=O)C(C)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C5CCCN5C(=O)CNC(=O)C(CCSC)N

1. Parstatin, a novel protease-activated receptor 1-derived inhibitor of angiogenesis

Raghu Kalluri, Michael B Duncan Mol Interv . 2009 Aug;9(4):168-70. doi: 10.1124/mi.9.4.4.

Angiogenesis, the process of forming new blood vessels, is a well established and clinically relevant feature of a variety of disease states. Whether blood vessels sprout in a given tissue environment depends on the balance between factors that stimulate angiogenesis and those that impede it. Potent pro-angiogenic factors such as vascular endothelial growth factor (VEGF) have been identified, validated, and successfully used in the clinic. Likewise, anti-angiogenic factors are also emerging as biologically relevant and therapeutically useful entities. PAR1 is a G protein-coupled receptor (GPCR) that participates in hemostasis and vascular development and that mediates the angiogenic activity of thrombin. PAR1 is activated through proteolytic cleavage of its first forty-one extracellular residues by a variety of proteases, most notably thrombin. However, little effort has focused on the forty-one-residue peptide fragment liberated during PAR1 activation. Tsopanoglou and colleagues have now demonstrated that this peptide, parstatin, has intriguing antiangiogenic activity, and, in a follow-up study, they demonstrate its potential pharmacological utility using a rat model of ischemic heart disease.

2. Combined Treatment With Exenatide and Cyclosporine A or Parstatin 1-26 Results in Enhanced Reduction of Infarct Size in a Rabbit Model

Panagiotis Alexopoulos, Efstratios Koletsis, Konstantina Panoutsopoulou, George Vogiatzis, Dimitrios Dougenis, Nikos E Tsopanoglou J Cardiovasc Pharmacol . 2017 Jul;70(1):34-41. doi: 10.1097/FJC.0000000000000492.

Exenatide and cyclosporine A have been shown to moderately protect against myocardial reperfusion injury leading to reduction of infarct size in patients. Our objective was to investigate whether the combined treatment with exenatide (glucagon-like peptide 1 receptor agonist) and cyclosporine A or parstatin 1-26 (inhibitors of mitochondrial permeability transition pore and/or inflammation) is more beneficial than either agent alone. Rabbits underwent 40 minutes of ischemia and 120 minutes of reperfusion. Intravenous bolus administration of exenatide or cyclosporine A, 10 minutes before reperfusion, reduced infarct size by 38% (P < 0.05) and 40% (P < 0.05), and cardiac troponin I (cTnI) plasma levels by 48% (P < 0.05) and 36% (P < 0.05), respectively, compared with control. The combined administration of both agents resulted in an additive decrease of infarct size by 55% (P < 0.05) and cTnI release by 61% (P < 0.05). Also, combined treatment of exenatide and parstatin 1-26 enhanced infarct size reduction (62%, P < 0.05), compared with monotherapies (41% for parstatin 1-26, P < 0.05; 43% for exenatide, P < 0.05). In contrast, the combined administration of parstatin 1-26 and cyclosporine A canceled out the cardioprotective effects observed by monotherapies. These results suggest that, for the therapy of myocardial reperfusion injury the combined administration of exenatide and cyclosporine A or parstatin 1-26 is more effective than monotherapies and may provide advantageous clinical outcome.

3. The protease-activated receptor 1 possesses a functional and cleavable signal peptide which is necessary for receptor expression

Claudia Rutz, Doreen Wüstenhagen, Ralf Schülein, Stefan Kubick, Antje Schmidt, Jens Furkert, Dimitris E Zampatis, Nikos E Tsopanoglou FEBS Lett . 2012 Jul 30;586(16):2351-9. doi: 10.1016/j.febslet.2012.05.042.

The protease-activated receptor 1 (PAR1) is activated by thrombin cleavage releasing the physiologically-relevant parstatin peptide (residues 1-41). However, the actual length of parstatin was unclear since the receptor may also possess a cleavable signal peptide (residues 1-21) according to prediction programs. Here, we show that this putative signal peptide is indeed functional and removed from the PAR1 resolving the question of parstatin length. Moreover, we show that the sequence encoding the signal peptide may surprisingly play a role in stabilization of the PAR1 mRNA, a function which would be novel for a G protein-coupled receptor.