Azelaprag  (Synonyms: AMG 986)

Azelaprag (Example 263.0) is a candidate active molecule for an Apelin receptor agonist with an EC₅₀ of 0.32 nM for the apelin receptor^[1].

EC50: 0.32 nM (Apelin receptor)^[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 T_1/2 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]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

523.61

C₂₅H₂₉N₇O₄S

2049980-18-7

Solid

White to light yellow

O=S(NC1=NN=C(C2=CN=CC(C)=C2)N1C(C(OC)=CC=C3)=C3OC)([C@@H](C)[C@@H](C4=NC=C(C)C=N4)C)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. WO2016187308A1.

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