B7-33 is a single-chain peptide. It is derived from a naturally occurring compound called H2-Relaxin. Relaxin proteins are a family of four proteins comprising Relaxin, Insulin-like peptide 3, H3-relaxin, and insulin-like peptide 5. They all possess pleiotropic actions impacting the cardiovascular system, musculoskeletal system, reproduction system, etc. These proteins perform these actions through four types of receptors, namely (RXFP1/2 and RXFP3/4). Various ligands, such as cAMP and corticotropin-releasing hormone, stimulate these receptors. All these agonists can express antioxidant, anti-inflammatory, and wound healing properties. However, Relaxin, in addition to possessing above mentioned properties, also exhibits antihypertrophic, vasodilator, and angiogenic properties. This is why Relaxin and its derivatives have been of great interest for researchers to explore its further benefits.
B7-33 preferentially stimulates the pERK pathway over the cAMP pathway. The pERK pathway regulates cell cycle arrest in the G1 phase and has been implicated in several diseases like Alzheimer's and Crutzfeld-Jacob. By blocking cell cycle progression in cells with RXFP1 receptors, B7-33 exercises its anti-fibrotic effects through the ability to stimulate RXFP1-angiotensin II type 2 receptor heterodimering, which activates pERK1/2 signaling and, thus triggers the increased production of the collagen-degrading enzyme matrix metalloproteinase (MMP) -2.
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