Delving into the Latest Updates on Apelin-13 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Target

APLNR

Mechanism

APLNR agonists(Apelin receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Le Centre Hospitalier Universitaire de Toulouse

Active Organization

Le Centre Hospitalier Universitaire de Toulouse

Inactive Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC69H111N23O16S

InChIKeyXXCCRHIAIBQDPX-PEWBXTNBSA-N

CAS Registry217082-58-1

Sequence Code 9616810

Source: *****

The purpose of this study is to
Determine blood peptide levels and investigate any tissue gradients of apelin in patients with idiopathic pulmonary arterial hypertension and healthy volunteers.
Evaluate the effect of exogenous apelin infusion on exercise performance in healthy volunteers and patients with idiopathic pulmonary arterial hypertension.

Start Date01 Mar 2012

Sponsor / Collaborator

Imperial College London

100 Clinical Results associated with Apelin-13

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100 Translational Medicine associated with Apelin-13

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100 Patents (Medical) associated with Apelin-13

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386

Literatures (Medical) associated with Apelin-13

01 Feb 2025·Journal of Molecular Histology

Protective effect of Apelin-13 on oxygen and glucose deprivation induced-damage in retinal ganglion cells cultured in vitro

Article

Author: Dai, Li ; Zhang, Ya ; Luo, Linlin ; Fu, Min ; Yu, Ling

Ischemic-anoxic injury plays an important role in the pathophysiology of diabetes retinopathy, optic neuropathy, even glaucoma and other ocular diseases. It may ultimately cause damage to neuronal death like retinal ganglion cells (RGCs) and subsequent visual loss. RGCs are essential elements of the retina and optic nerve that are crucial to visual formation. Ischemic-anoxic injury, inflammation, and oxidative stress are vital causes of RGC death. Thus, neuroprotection is essential for the treatment of these ocular diseases. Recent studies have shown the neuroprotective property of apelin-13 in many disease models. In this study, we isolated RGCs and found that apelin-13 promoted the viability of RGCs and increased the phosphorylation of Protein kinase B (PKB, Akt) in an in vitro oxygen-glucose deprivation model. Moreover, apelin-13 increased the expressions of glucose-6-phosphate dehydrogenase (G6PD) and nicotinamide adenine dinucleotide phosphate (NADPH) and reduced the level of reactive oxygen species (ROS). And, we also found that apelin-13 could promote the expressions of glucose transporter-1 (GLUT1) and adenosine triphosphate (ATP). These results indicated that apelin-13 could delay or stop RGC death, which might be as potential therapeutic targets for treatment of diseases mediated by ischemic-anoxic damage like diabetes retinopathy, optic neuropathy, even glaucoma.

01 Feb 2025·Neuroscience

Effects and mechanisms of Apelin in treating central nervous system diseases

Review

Author: Huang, Zimeng ; Liu, Qing ; Li, Liming ; Guo, Qixuan ; Gao, Jianqing ; Zhang, Luping

Apelin, an endogenous ligand of G protein-coupled receptor APJ, is widely distributed in the central nervous system (CNS). It can be divided into such subtypes as Apelin-13, Apelin-17, and Apelin-36 as they have different amino acid structures. All Apelin is widely studied as an adipokine, showing a significant protective effect through regulating apoptosis, autophagy, oxidative stress, angiogenesis, inflammation, and other pathophysiological processes. As an adipokine, Apelin has been found to play a crucial role in cardiovascular disease development. In this paper, we reviewed the effects and mechanisms of Apelin in treating CNS diseases, such as neurotrauma, stroke, spinal cord injury, primary tumors, neurodegenerative diseases, psychiatric diseases, epilepsy, and pain.

01 Jan 2025·Peptides

Apelin/APJ increased renal blood flow through endothelial BKCa channel induced p-eNOS and ET-1 in diabetic conditions

Article

Author: Huang, Mingcong ; Chang, Jing ; Liu, Yu ; Zeng, Xiangjun ; Yin, Jiming

Renal hemodynamics damage, an important driving mechanism of diabetic nephropathy (DN), is related to many abnormal endothelial released molecules, such as endothelial nitrogen monoxide synthase (eNOS) and endothelin-1 (ET-1), caused by glomerular endothelial cells dysfunction. Apelin, as the endogenous ligand for APJ, was reported to be associated with endothelial cell dysfunction in diabetes. Therefore, it is hypothesized that apelin/APJ increased renal perfusion in DN through regulating endothelial released molecules. Diabetic models were replicated via injecting STZ intraperitoneally (40 mg/kg/day) for 5 consecutive days. Apelin-13 was infused with micro-osmotic pump at 30 μg/kg/day for 4 weeks. The results showed that apelin increased renal blood flow by increasing phosphorylated eNOS and decreasing ET-1 in diabetic mice, which were cancelled in endothelial-specific APJ knockout mice or whole-body large conductance Ca^2 +-activated K⁺ (BKCa) channel knockout rats. Additionally, apelin/APJ activated BKCa channel via increasing expression of BKCa subunits through PI3K/AKT/GSK-3β/Nrf2 pathway but not increasing intracellular Ca²⁺ concentration under high glucose conditions. In conclusion, this study revealed that apelin/APJ increased renal blood flow in early phase of DN via increasing p-eNOS and decreasing ET-1 in glomerular endothelial cells dependent on PI3K/AKT/GSK-3β/Nrf2 pathway induced expression of BKCa subunits.

100 Deals associated with Apelin-13

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 1	-	Le Centre Hospitalier Universitaire de Toulouse	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Pubmed \| J Mol Cell Cardiol	Not Applicable	-	-	Apelin-13	(gysktgainz) = Apelin also increased I(Na) "window" current by up to 600% irmfseggzd (vhvwxakutp )	-	01 Apr 2010
				Apelin-17