Azelaprag

Azelaprag
Identifiers
	IUPAC name (2S,3R)-N-[4-(2,6-dimethoxyphenyl)-5-(5-methyl-3-pyridinyl)-1,2,4-triazol-3-yl]-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide;
CAS Number	2049980-18-7;
PubChem CID	122702529;
Chemical and physical data
Formula	C25H29N7O4S
Molar mass	523.61 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=CC(=CN=C1)C2=NN=C(N2C3=C(C=CC=C3OC)OC)NS(=O)(=O)[C@@H](C)[C@H](C)C4=NC=C(C=N4)C;
	InChI InChI=1S/C25H29N7O4S/c1-15-10-19(14-26-11-15)24-29-30-25(32(24)22-20(35-5)8-7-9-21(22)36-6)31-37(33,34)18(4)17(3)23-27-12-16(2)13-28-23/h7-14,17-18H,1-6H3,(H,30,31)/t17-,18-/m0/s1; Key:DOMQFIFVDIAOOT-ROUUACIJSA-N;

Azelaprag (original Amgen development code AMG 986, subsequently licensed to BioAge Labs and renamed BGE-105) is a drug which is a selective, small-molecule agonist for the apelin receptor. It was originally developed as a potential treatment for heart failure and has subsequently been investigated for other applications such as obesity and muscle wasting in elderly or bed-bound patients.^[1]^[2]^[3]

References

^ Ason B, Chen Y, Guo Q, Hoagland KM, Chui RW, Fielden M, et al. (April 2020). "Cardiovascular response to small-molecule APJ activation". JCI Insight. 5 (8) e132898. doi:10.1172/jci.insight.132898. PMC 7205427. PMID 32208384.
^ Hellawell J, Abbasi S, Trivedi A, Tsirtsonis K, Kaufman A (October 2020). "Safety, tolerability, pharmacokinetics, and pharmacodynamics of AMG 986, a novel small molecule apelin receptor agonist, in healthy subjects and heart failure patients". Journal of Cardiac Failure. 26 (10): S68. doi:10.1016/j.cardfail.2020.09.200.
^ Pi Z, Johnson JA, Meng W, Phillips M, Schumacher WA, Bostwick JS, et al. (November 2021). "Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists". ACS Medicinal Chemistry Letters. 12 (11): 1766–1772. doi:10.1021/acsmedchemlett.1c00385. PMC 8591725. PMID 34795866.

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

[1] Ason B, Chen Y, Guo Q, Hoagland KM, Chui RW, Fielden M, et al. (April 2020). "Cardiovascular response to small-molecule APJ activation". JCI Insight. 5 (8) e132898. doi:10.1172/jci.insight.132898. PMC 7205427. PMID 32208384.

[2] Hellawell J, Abbasi S, Trivedi A, Tsirtsonis K, Kaufman A (October 2020). "Safety, tolerability, pharmacokinetics, and pharmacodynamics of AMG 986, a novel small molecule apelin receptor agonist, in healthy subjects and heart failure patients". Journal of Cardiac Failure. 26 (10): S68. doi:10.1016/j.cardfail.2020.09.200.

[3] Pi Z, Johnson JA, Meng W, Phillips M, Schumacher WA, Bostwick JS, et al. (November 2021). "Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists". ACS Medicinal Chemistry Letters. 12 (11): 1766–1772. doi:10.1021/acsmedchemlett.1c00385. PMC 8591725. PMID 34795866.

[1]

[2]

[3]

See also

References