Chemistry:ML221

From HandWiki

ML221 is a drug which is a selective, small-molecule antagonist for the apelin receptor. It is primarily used for research into the function of this receptor pathway, but also has potential medical applications.[1][2][3][4][5][6][7][8][9]

References

  1. ↑ "Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor". Bioorganic & Medicinal Chemistry Letters 22 (21): 6656–6660. November 2012. doi:10.1016/j.bmcl.2012.08.105. PMID 23010269. 
  2. ↑ "Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth". Cancer Letters 386: 179–188. February 2017. doi:10.1016/j.canlet.2016.11.025. PMID 27894959. 
  3. ↑ "Expression of apelin and apelin receptor (APJ) in porcine ovarian follicles and in vitro effect of apelin on steroidogenesis and proliferation through APJ activation and different signaling pathways". Theriogenology 96: 126–135. July 2017. doi:10.1016/j.theriogenology.2017.04.014. PMID 28532828. http://ruj.uj.edu.pl/xmlui/handle/item/41342. 
  4. ↑ "An apelin receptor antagonist prevents pathological retinal angiogenesis with ischemic retinopathy in mice". Scientific Reports 7 (1). November 2017. doi:10.1038/s41598-017-15602-3. PMID 29118394. Bibcode: 2017NatSR...715062I. 
  5. ↑ "Multifunctional APJ Pathway Promotes Ovarian Cancer Progression and Metastasis". Molecular Cancer Research 17 (6): 1378–1390. June 2019. doi:10.1158/1541-7786.MCR-18-0989. PMID 30858172. 
  6. ↑ "Targeting APLN/APJ restores blood-testis barrier and improves spermatogenesis in murine and human diabetic models". Nature Communications 13 (1). November 2022. doi:10.1038/s41467-022-34990-3. PMID 36443325. Bibcode: 2022NatCo..13.7335S. 
  7. ↑ "Apelin receptor antagonist (ML221) treatment has a stimulatory effect on the testicular proliferation, antioxidants system and steroidogenesis in adult mice". Neuropeptides 101. October 2023. doi:10.1016/j.npep.2023.102354. PMID 37379791. 
  8. ↑ "APLN promotes the proliferation, migration, and glycolysis of cervical cancer through the PI3K/AKT/mTOR pathway". Archives of Biochemistry and Biophysics 755. May 2024. doi:10.1016/j.abb.2024.109983. PMID 38561035. 
  9. ↑ "Novel small molecule analogs for advancing apelin receptor antagonism with enhanced plasma and microsomal stability". Bioorganic & Medicinal Chemistry Letters 129. December 2025. doi:10.1016/j.bmcl.2025.130367. PMID 40784515. 



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