An APJ agonist
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Azelaprag

Item No. 44644

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αS,βR)-N-[4-(2,6-dimethoxyphenyl)-5-(5-methyl-3-pyridinyl)-4H-1,2,4-triazol-3-yl]-α,β,5-trimethyl-2-pyrimidineethanesulfonamide
CAS Number
2049980-18-7
Synonyms
  • AMG 986
  • BGE-105
Molecular Formula
C25H29N7O4S
Formula Weight
523.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Slightly soluble: 0.1-1mg/mlDMSO: Slightly soluble: 0.1-1mg/ml
SMILES
C[C@H](C1=NC=C(C)C=N1)[C@H](C)S(NC2=NN=C(C3=CN=CC(C)=C3)N2C4=C(C=CC=C4OC)OC)(=O)=O
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-/m0/s1
InChi Key
DOMQFIFVDIAOOT-ROUUACIJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $139

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    5 mg

    $313

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    10 mg

    $487

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    Product Description

    Azelaprag is an agonist of the apelin receptor (APJ).1 It inhibits forskolin-induced cAMP accumulation in CHO cells expressing human APJ (EC50 = 0.23 nM). Azelaprag (1 mg/kg, i.v.) increases stroke volume and heart rate and decreases systemic vascular resistance, indicating increased cardiac reserve, in ZSF1 obese rats in a model of diastolic dysfunction driven by impaired metabolism, endothelial dysfunction, and hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ason, B., Chen, Y., Guo, Q., et al. Cardiovascular response to small-molecule APJ activation. JCI Insight 5(8), e132898 (2020).