MedKoo Cat#: 563450 | Name: Azelaprag
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Azelaprag
Azelaprag
CAS#2049980-18-7

Theoretical Analysis

MedKoo Cat#: 563450

Name: Azelaprag

CAS#: 2049980-18-7

Chemical Formula: C25H29N7O4S

Exact Mass: 523.2002

Molecular Weight: 523.61

Elemental Analysis: C, 57.35; H, 5.58; N, 18.73; O, 12.22; S, 6.12

Price and Availability

Size Price Availability Quantity
1mg USD 750.00 2 Weeks
5mg USD 3,650.00 2 Weeks
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Related CAS #
No Data
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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
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.