[Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist.
[Pyr1]-apelin-13 encapsulation in lipoPEG particles (lipoPEG-PA13) results in sustained and extended drug release under physiological conditions[1].
[Pyr1]-apelin-13 nanocarriers in a mouse model of pressure-overload induced heart failure demonstrate a sustainable long-term effect of [Pyr1]-apelin-13 in preventing cardiac dysfunction[1]. [Pyr1] apelin-13 (1, 5 μg) improves locomotor activity and reduces pain symptoms, cavity size and caspase-3 levels in rats. [Pyr1] apelin-13 (1, 5 μg) significantly increases thermal paw withdrawal latency. [Pyr1] apelin-13 in 5 μg dose also produces significant attenuation in paw withdrawal threshold compared to SCI animals from the second week post SCI[2].
References:
[1]. Serpooshan V, et al. [Pyr1]-Apelin-13 delivery via nano-liposomal encapsulation attenuates pressure overload-induced cardiac dysfunction. Biomaterials. 2015 Jan;37:289-98.
[2]. Hajimashhadi Z, et al. Chronic administration of [Pyr1] apelin-13 attenuates neuropathic pain after compression spinal cord injury in rats. Neuropeptides. 2017 Feb;61:15-22.