SPH3127

SPH3127
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name Methyl N-[3-[3-[(1R)-1-[cyclopropyl-[(2R)-morpholine-2-carbonyl]amino]ethyl]-6-methylpyrazolo[3,4-b]pyridin-1-yl]propyl]carbamate;
CAS Number	1399849-02-5;
PubChem CID	117877477;
ChemSpider	76799450;
UNII	C2M78A9V6Z;
ChEMBL	ChEMBL4110551;
Chemical and physical data
Formula	C22H32N6O4
Molar mass	444.536 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=NC2=C(C=C1)C(=NN2CCCNC(=O)OC)[C@@H](C)N(C3CC3)C(=O)[C@H]4CNCCO4;
	InChI InChI=1S/C22H32N6O4/c1-14-5-8-17-19(26-27(20(17)25-14)11-4-9-24-22(30)31-3)15(2)28(16-6-7-16)21(29)18-13-23-10-12-32-18/h5,8,15-16,18,23H,4,6-7,9-13H2,1-3H3,(H,24,30)/t15-,18-/m1/s1; Key:GRTDDIZIUSADLD-CRAIPNDOSA-N;

SPH3127 is a small-molecule renin inhibitor developed by Shanghai Pharmaceuticals for hypertension and kidney disease. It is believed to be more potent than aliskiren.^[1]^[2]^[3]

References

^ Iijima, Daisuke; Sugama, Hiroshi; Takahashi, Yoichi; Hirai, Miki; Togashi, Yuko; Xie, Jianshu; Shen, Jingkang; Ke, Ying; Akatsuka, Hidenori; Kawaguchi, Takayuki; Takedomi, Kei; Kashima, Akiko; Nishio, Masashi; Inui, Yosuke; Yoneda, Hikaru; Xia, Guangxin; Iijima, Toru (25 August 2022). "Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor". Journal of Medicinal Chemistry. 65 (16): 10882–10897. doi:10.1021/acs.jmedchem.2c00834. PMID 35939295. S2CID 251400126.
^ Zhang, Leduo; Mao, Yu; Gao, Zhiwei; Chen, Xiaoyan; Li, Xin; Liu, Yanjun; Xia, Guangxin (February 2020). "The Nonclinical Pharmacokinetics and Prediction of Human Pharmacokinetics of SPH3127, a Novel Direct Renin Inhibitor". European Journal of Drug Metabolism and Pharmacokinetics. 45 (1): 15–26. doi:10.1007/s13318-019-00573-9. PMID 31494843. S2CID 201848935.
^ Jing, Shan; Xu, Ranchi; Yang, Kexu; Liu, Wenfang; Zhang, Leduo; Ke, Ying; Xia, Guangxin; Lin, Yang (April 2021). "Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of SPH3127: A Phase I, Randomized, Double-Blind, Placebo-Controlled Trial". Clinical Therapeutics. 43 (4): 735.e1–735.e14. doi:10.1016/j.clinthera.2021.01.025. PMID 33653620. S2CID 232104329.