{{cs1 config|name-list-style=vanc|display-authors=6}} {{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 | image = Azelaprag_structure.png | image_class = skin-invert-image | width = 240
<!--Clinical data--> | tradename = | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | pregnancy_US = <!-- A / B / C / D / X --> | pregnancy_category = | legal_AU = <!-- S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> | legal_CA = | legal_UK = | legal_US = <!-- Schedule I / Schedule II / Schedule III --> | legal_status = | routes_of_administration =
<!--Pharmacokinetic data--> | bioavailability = | protein_bound = | excretion =
<!--Identifiers--> | CAS_number = 2049980-18-7 | UNII = | PubChem = 122702529 | IUPHAR_ligand = | DrugBank = | ChemSpiderID = | ChEBI = | ChEMBL = | StdInChI = 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 | StdInChIKey = DOMQFIFVDIAOOT-ROUUACIJSA-N <!--Chemical data--> | C=25 | H=29 | N=7 | O=4 | S=1 | 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 }}
'''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>{{cite journal | vauthors = 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 | title = Cardiovascular response to small-molecule APJ activation | journal = JCI Insight | volume = 5 | issue = 8 | date = April 2020 | article-number = e132898 | pmid = 32208384 | doi = 10.1172/jci.insight.132898 | pmc = 7205427 }}</ref><ref>{{cite journal | vauthors = Hellawell J, Abbasi S, Trivedi A, Tsirtsonis K, Kaufman A | title = Safety, tolerability, pharmacokinetics, and pharmacodynamics of AMG 986, a novel small molecule apelin receptor agonist, in healthy subjects and heart failure patients. | journal = Journal of Cardiac Failure | date= October 2020 | volume = 26 | issue = 10 | pages = S68 | doi = 10.1016/j.cardfail.2020.09.200 }}</ref><ref>{{cite journal | vauthors = 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 | title = Identification of 6-Hydroxypyrimidin-4(1''H'')-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists | journal = ACS Medicinal Chemistry Letters | volume = 12 | issue = 11 | pages = 1766–1772 | date = November 2021 | pmid = 34795866 | doi = 10.1021/acsmedchemlett.1c00385 | pmc = 8591725 }}</ref>
== See also == * AM-8123 * BMS-986224 * CMF-019
== References == {{reflist}}
Category:Benzene derivatives Category:Methoxy compounds Category:Pyridines Category:Pyrimidines Category:Sulfonamides Category:Triazoles
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