Agonist API GW501516 pauda keʻokeʻo

ʻO GW 501516 kahi agonist o PPARδ me ka waiwai EC50 o 1.1 nM.
Hōʻike ʻia ʻo GW501516 i nā agonists PPARα ikaika loa a koho i ʻike ʻia me kahi EC 50 o 1. 1 nM kūʻē iā PPARα a me 1000-fold selectivity ma luna o nā subtypes kanaka ʻē aʻe, PPARα a me -γ.Hoʻohana ʻo GW501516 i nā hopena anti-inflammatory i loko o nā kiʻi moʻomeheu proximal tubular (mProx) cell.Kāohi ʻo GW501516 i ka hoʻonui ʻana i ka palmitate- a me ka TNFα i hoʻonui ʻia i ka hōʻike MCP-1 mRNA ma ke ʻano i hilinaʻi ʻia.
ʻO GW501516 ke kumu o ka hoʻokumu ʻana o ka iwi, e alakaʻi ana i ka emi ʻana o ka BMD a me ka emi ʻana o nā waiwai iwi i nā ʻiole OVX.Hoʻopiʻi ʻo GW501516 i ka ʻāʻī interstitial a me ka pōʻino o nā cell tubular proximal i loko o kahi kumu hoʻohālike nephropathy kiʻekiʻe o ka protein.Hoʻonui ka hoʻomaʻamaʻa GW501516 i ka hoʻomanawanui holo ʻana a me ka hapa o ka succinate dehydrogenase (SDH) i nā ʻiole i hoʻomaʻamaʻa ʻole ʻia.