Azelaprag

• CAT Number: I019541
• CAS Number: 2049980-18-7
• Molecular Formula: C25H29N7O4S
• Molecular Weight: 523.61
• Purity: ≥95%
• Synonyms: (2S,3R)-N-[4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-1,2,4-triazol-3-yl]-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide
• 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
• InChIKey: DOMQFIFVDIAOOT-ROUUACIJSA-N
• SMILES: CC1=CC(=CN=C1)C2=NN=C(N2C3=C(C=CC=C3OC)OC)NS(=O)(=O)C(C)C(C)C4=NC=C(C=N4)C

Azelaprag (Example 263.0) is an apelin receptor agonist agent candidate[1].
Azelaprag (AMG 986) (1 mg/kg/min, acute i.v. infusion) increases cardiac reserve during Dobutamine (HY-15746A) challenge in a rat model of impaired metabolic function[2].
Azelaprag (AMG 986) (0.5 mg/kg for i.v., 2 mg/kg for p.o.) shows a T1/2 of 2.4 h in rat and 4.2 h in dog by i.v., and oral bioavailability (F%) of 73% in rat and 97% in dog[2].
Pharmacokinetic parameters for Azelaprag(AMG 986) in rat and dog[2]

Species
CL (L/h/kg)
VSS (L/kg)
T1/2 (h)
Oral F(%)

Rat
0.78
0.6
2.4
73

Dog
0.08
0.19
4.2
97

Reference

[1]. WO2016187308A1.

[2]. Ason B, et.al. Cardiovascular response to small-molecule APJ activation. JCI Insight. 2020 Apr 23;5(8):e132898.
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