2.Granberg KL, et al. (2024) Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure. J Med Chem. doi: 10.1021/acs.jmedchem.3c02184. END 【智药研习社近期直播预告】
1.中国国家药监局药品审评中心(CDE)网站 2.Granberg KL, et al. (2024) Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure. J Med Chem. doi: 10.1021/acs.jmedchem.3c02184.
描述 AZD5462 is a potent orally available relaxin receptor RXFP1 agonist for the study of heart failure and cancer. 体外活性 AZD5462 (example 1) exhibits stimulatory activity on cAMP or cGMP production with EC50s of 17 nM and 50 nM, respectively[1]. Binding to human plasma proteins with a...
In summary, AZD5462 is a small molecule pharmacological mimetic of relaxin H2 signaling at RXFP1 and holds promise as a potential therapeutic approach to treat heart failure patients.doi:10.1021/acs.jmedchem.3c02184Granberg, Kenneth L.Sakamaki, Shigeki...
生化试剂 全部产品列表 产品简介 CAS2787501-83-9分子量544.65 分子式C₃₀H₄₁FN₂O₆供货周期现货 货号HY-148087应用领域医疗卫生,化工,生物产业,制药 AZD5462 | MCEAZD5462 is a RXFP1 modulator, can be used for heart failure research. RXFP1 is the cognate receptor for human relaxin, bel...
产品活性:AZD5462 is a RXFP1 modulator, can be used for heart failure research. RXFP1 is the cognate receptor for human relaxin, belongs to GPCR family 1c number with anti-fibrotic and anti-inflammatory properties. 研究领域:Others 作用靶点:Others In Vitro: AZD5462 (example 1) shows stimulator...
近日,阿斯利康在TOP期刊JMC上背靠背连发2篇文章详细报道了目前处于二期临床的RXFP1激动剂AZD5462的发现过程。2013年,美国NIH对35万多个化合物通过高通量筛选发现了化合物ML290。此后近10年时间,AZ以ML290为先导进行优化,最终开发的AZD5462在2022年6月成为首个进入临床的口服小分子RXFP1激动剂。图1 JMC上线AZ两篇文章...
The potential therapeutic benefits of RXFP1 agonism are the subject of on-going clinical trials in heart failure patients.Lal MarkRyberg ErikAlthage MagnusBergstrm FredrikHansen Pernille B LPettersen DanielConnolly KatRosenmeier JayaNephrology Dialysis Transplantation...