WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H563450
CAS#: 2049980-18-7
Description: Azelaprag, also known as AMG986, is a novel apelin receptor (APJ) agonist that improves cardiac contractility in animal models without adversely impacting hemodynamics. AMG 986 activate the APJ receptor in a manner similar to the endogenous ligands. AMG 986 inhibited forskolin-stimulated cAMP production and promoted Gα protein activation. AMG 986 is well tolerated, causing no adverse effects in nonclinical toxicology models.
Hodoodo Cat#: H563450
Name: Azelaprag
CAS#: 2049980-18-7
Chemical Formula: C25H29N7O4S
Exact Mass: 523.20
Molecular Weight: 523.610
Elemental Analysis: C, 57.35; H, 5.58; N, 18.73; O, 12.22; S, 6.12
Synonym: Azelaprag; AMG986; AMG-986; AMG 986;
IUPAC/Chemical Name: (2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide
InChi Key: DOMQFIFVDIAOOT-QZTJIDSGSA-N
InChi Code: 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-/m1/s1
SMILES Code: C[C@@H](S(=O)(NC1=NN=C(C2=CC(C)=CN=C2)N1C3=C(OC)C=CC=C3OC)=O)[C@H](C4=NC=C(C)C=N4)C
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.03.00
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 523.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Winkle P, Goldsmith S, Koren MJ, Lepage S, Hellawell J, Trivedi A, Tsirtsonis K, Abbasi SA, Kaufman A, Troughton R, Voors A, Hulot JS, Donal E, Kazemi N, Neutel J. A First-in-Human Study of AMG 986, a Novel Apelin Receptor Agonist, in Healthy Subjects and Heart Failure Patients. Cardiovasc Drugs Ther. 2023 Aug;37(4):743-755. doi: 10.1007/s10557-022-07328-w. Epub 2022 Apr 23. PMID: 35460392.
2: Trivedi A, Kiang YH, Saw RE, Cheng GC, Mather O, Vega S, Hellawell J, Lee E. Evaluation of the Pharmacokinetics and Safety of AMG 986 Tablet and Capsule Formulations in Healthy Adult Subjects: A Phase I, Open-Label, Randomized Study. Drugs R D. 2022 Jun;22(2):147-154. doi: 10.1007/s40268-022-00388-1. Epub 2022 Apr 12. PMID: 35412220; PMCID: PMC9167409.
3: Trivedi A, Mather O, Vega S, Hutton S, Hellawell J, Lee E. A Phase I, Open- label, Single-Dose Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of AMG 986 in Healthy Japanese Subjects. Drugs R D. 2022 Jun;22(2):141-146. doi: 10.1007/s40268-022-00386-3. Epub 2022 Mar 13. PMID: 35279815; PMCID: PMC9167390.
4: Trivedi A, Mather O, Vega S, Hutton S, Hellawell J, Lee E. A Phase 1, Open- Label Study to Evaluate the Effect of Food and Concomitant Itraconazole Administration on the Pharmacokinetics of AMG 986 in Healthy Subjects. Clin Pharmacol Drug Dev. 2022 Jul;11(7):849-856. doi: 10.1002/cpdd.1074. Epub 2022 Mar 5. PMID: 35247290.
5: Trivedi A, Mather O, Vega S, Simiens MA, Hellawell J, Lee E. Effect of Severe Renal Impairment on the Safety, Tolerability, and Pharmacokinetics of AMG 986. Drugs R D. 2022 Mar;22(1):89-94. doi: 10.1007/s40268-021-00380-1. Epub 2022 Jan 29. PMID: 35092583; PMCID: PMC8885944.
