1006388-38-0
Chemical Structure
Cenupatide
Synonym(s): UPARANT
- CAS No.: 1006388-38-0
- Formula:C28H47N11O5
- Molecular Weight:617.74
IUPAC Name: (S)-2-acetamido-N-(1-(((S)-1-(((S)-1-amino-2-methyl-1-oxo-3-phenylpropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5-guanidinopentanamide
InChIKey: JDNFBDNDFFJJIB-JVAKCPTJSA-N
SMILES: N=C(N)NCCC[C@H](NC(C)=O)C(NC(C)(C)C(N[C@@H](CCCNC(N)=N)C(N[C@@](C(N)=O)(C)CC1=CC=CC=C1)=O)=O)=O
Biological Activity: Cenupatide (UPARANT) is a uPAR and FPR antagonist with anti-angiogenic, anti-inflammatory, and vascular barrier regulatory activities, as well as high stability and resistance to enzymatic degradation in blood/plasma. Cenupatide blocks the uPAR-FPR interaction, reduces VEGF-induced phosphorylation levels of AKT, VEGFR-2, STAT3, JNK, p38 MAPK, ERK1/2, and NF-κB p65, and inhibits αvβ3 integrin activation. Cenupatide suppresses endothelial cell migration, invasion, tube formation, and angiogenic signaling pathways, restores tight junctions and blood-retinal barrier integrity, reduces pro-inflammatory marker levels, and inhibits apoptosis. Cenupatide reduces retinal neovascularization, renal fibrosis, and vascular leakage, and restores visual function in preclinical models. Cenupatide is applicable to research related to retinopathy, diabetic complications, ocular diseases, cancer, and inflammatory diseases[1][2][3][4][5][6][7][8][9][10].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Cenupatide | 99.94% | Cenupatide (UPARANT) is a uPAR and FPR antagonist with anti-angiogenic, anti-inflammatory, and vascular barrier regulatory activities, as well as high stability and resistance to enzymatic degradation in blood/plasma. Cenupatide blocks the uPAR-FPR interaction, reduces VEGF-induced phosphorylation levels of AKT, VEGFR-2, STAT3, JNK, p38 MAPK, ERK1/2, and NF-κB p65, and inhibits αvβ3 integrin activation. Cenupatide suppresses endothelial cell migration, invasion, tube formation, and angiogenic signaling pathways, restores tight junctions and blood-retinal barrier integrity, reduces pro-inflammatory marker levels, and inhibits apoptosis. Cenupatide reduces retinal neovascularization, renal fibrosis, and vascular leakage, and restores visual function in preclinical models. Cenupatide is applicable to research related to retinopathy, diabetic complications, ocular diseases, cancer, and inflammatory diseases. | ||||||||||||||||||||
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- [1]. Motta C, et al. Molecular Mechanisms Mediating Antiangiogenic Action of the Urokinase Receptor-Derived Peptide UPARANT in Human Retinal Endothelial Cells. Investigative ophthalmology & visual science. 2016 Oct 01;57(13):5723-5735.
- [2]. Dal Monte M, et al. Antiangiogenic Effectiveness of the Urokinase Receptor-Derived Peptide UPARANT in a Model of Oxygen-Induced Retinopathy. Investigative ophthalmology & visual science. 2015 Apr;56(4):2392-407.
- [3]. Yuan C, et al. Development of inhibitors for uPAR: blocking the interaction of uPAR with its partners. Drug discovery today. 2021 Apr;26(4):1076-1085. [Content Brief]
- [4]. Locri F, et al. UPARANT is an effective antiangiogenic agent in a mouse model of rubeosis iridis. Journal of molecular medicine (Berlin, Germany). 2019 Sep;97(9):1273-1283.
- [5]. Dal Monte M, et al. Inhibiting the urokinase-type plasminogen activator receptor system recovers STZ-induced diabetic nephropathy. Journal of cellular and molecular medicine. 2019 Feb;23(2):1034-1049.
- [6]. Cammalleri M, et al. The Urokinase Receptor-Derived Peptide UPARANT Recovers Dysfunctional Electroretinogram and Blood-Retinal Barrier Leakage in a Rat Model of Diabetes. Investigative ophthalmology & visual science. 2017 Jun 01;58(7):3138-3148.
- [7]. Cammalleri M, et al. Diabetic Retinopathy in the Spontaneously Diabetic Torii Rat: Pathogenetic Mechanisms and Preventive Efficacy of Inhibiting the Urokinase-Type Plasminogen Activator Receptor System. Journal of diabetes research. 2017;2017:2904150.
- [8]. Carriero MV, et al. UPARANT: a urokinase receptor-derived peptide inhibitor of VEGF-driven angiogenesis with enhanced stability and in vitro and in vivo potency. Molecular cancer therapeutics. 2014 May;13(5):1092-104.
- [9]. D'Alonzo D, et al. COVID-19 and pneumonia: a role for the uPA/uPAR system. Drug discovery today. 2020 Aug;25(8):1528-1534.
- [10]. Boccella S, et al. Preclinical evaluation of the urokinase receptor-derived peptide UPARANT as an anti-inflammatory drug. Inflammation research : official journal of the European Histamine Research Society ... [et al.]. 2017 Aug;66(8):701-709.
Keywords
