Azelaprag

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{{Drugbox

{{Drugbox

| 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

| 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

}}

}}

”’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.<ref>Ason B, Chen Y, Guo Q, Hoagland KM, Chui RW, Fielden M, Sutherland W, Chen R, Zhang Y, Mihardja S, Ma X, Li X, Sun Y, Liu D, Nguyen K, Wang J, Li N, Rajamani S, Qu Y, Gao B, Boden A, Chintalgattu V, Turk JR, Chan J, Hu LA, Dransfield P, Houze J, Wong J, Ma J, Pattaropong V, Véniant MM, Vargas HM, Swaminath G, Khakoo AY. Cardiovascular response to small-molecule APJ activation. ”JCI Insight”. 2020 Apr 23;5(8):e132898. {{doi|10.1172/jci.insight.132898}} {{pmid|32208384}}</ref><ref>Hellawell J, et al. 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” 2020; 26(10):S68. {{doi|10.1016/j.cardfail.2020.09.200}}</ref><ref>Pi Z, Johnson JA, Meng W, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Generaux CN, Wang T, He Y, Gordon DA, Wexler RR, Finlay HJ. Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists. ”ACS Med Chem Lett”. 2021 Oct 22;12(11):1766-1772. {{doi|10.1021/acsmedchemlett.1c00385}} {{pmid|34795866}}</ref>

”’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.<ref>Ason B, Chen Y, Guo Q, Hoagland KM, Chui RW, Fielden M, Sutherland W, Chen R, Zhang Y, Mihardja S, Ma X, Li X, Sun Y, Liu D, Nguyen K, Wang J, Li N, Rajamani S, Qu Y, Gao B, Boden A, Chintalgattu V, Turk JR, Chan J, Hu LA, Dransfield P, Houze J, Wong J, Ma J, Pattaropong V, Véniant MM, Vargas HM, Swaminath G, Khakoo AY Cardiovascular response to small-molecule APJ activation JCI Insight 58e132898 |10.1172/jci.insight.132898 |}}</ref><ref>Hellawell J, Safety, , , and 986, a , in and . Journal of Cardiac Failure 2020 2610S68 |10.1016/j.cardfail.2020.09.200}}</ref><ref>Pi Z, Johnson JA, Meng W, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Generaux CN, Wang T, He Y, Gordon DA, Wexler RR, Finlay HJ Identification of 6-Hydroxypyrimidin-4()-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists ACS 1211 |10.1021/acsmedchemlett.1c00385 |}}</ref>

==See also==

==See also==

* [[AM-8123]]

* [[AM-8123]]

* [[BMS-986224]]

* [[BMS-986224]]

[[Category:Sulfonamides]]

[[Category:Sulfonamides]]

[[Category:Triazoles]]

[[Category:Triazoles]]

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