Azelaprag
CAS No. : 2049980-18-7
(Synonyms: AMG 986)
| Size | Price | Stock |
|---|---|---|
| 1mg | $160 | In-stock |
| 5mg | $320 | In-stock |
| 10mg | $500 | In-stock |
| 25mg | $760 | In-stock |
| 50mg | $1140 | In-stock |
| 100mg | $1600 | In-stock |
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| Cat. No. : | HY-109111 |
| M.Wt: | 523.61 |
| Formula: | C25H29N7O4S |
| Purity: | >98 % |
| Solubility: | DMSO : 5 mg/mL (ultrasonic) |
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].
IC50 & Target:EC50: 0.32 nM (Apelin receptor)[1]
In Vivo: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 |
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