ML-290 (Synonyms: RXFP1 Agonist 8) |
| رقم الكتالوجGC18594 |
ML-290 هو الأول من نوعه في فئته وقوي مستقبلات الببتيد العائلي ريلاكسين / الأنسولين (RXFP1) ومنشط للجينات المضادة للليف ، مع EC50 من 94 نانومتر
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Cas No.: 1482500-76-4
Sample solution is provided at 25 µL, 10mM.
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ML-290 is an allosteric agonist of relaxin family peptide receptor 1 (RXFP1; EC50 = 94 nM for human RXFP1).[1],[2] It displays >15-fold selectivity for RXFP1 over RXFP2.[2] ML-290 activates human, rhesus macaque, pig, and rabbit RXFP1 but is weak or inactive at mouse or guinea pig RXFP1.[2],[3] Through RXFP1, ML-290 increases intracellular cAMP and induces VEGF expression (2.8-fold at 250 nM).[2] ML-290 is metabolically stable and displays excellent in vivo pharmacokinetics.[2]
Reference:
[1]. Paredes, R.M., Etzler, J.C., Watts, L.T., et al. Chemical calcium indicators. Methods 46(3), 143-151 (2008).
[2]. Minta, A., Kao, J.P., and Tsien, R.Y. Fluorescent indicators for cytosolic calcium based on rhodamine and fluorescein chromophores. The Journal of Biological Chemisty 264(14), 8171-8178 (1989).
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