An RXFP1 agonist
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AZD 5462

Item No. 40956

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cis-4-[2-fluoro-4-methoxy-5-[[[(1S,2R,3S,4R)-3-[[[(1-methylcyclobutyl)methyl]amino]carbonyl]bicyclo[2.2.1]hept-2-yl]amino]carbonyl]phenoxy]-1-methyl-cyclohexanecarboxylic acid
CAS Number
2787501-83-9
Molecular Formula
C30H41FN2O6
Formula Weight
544.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlDMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
[H][C@]1([C@H]2NC(C3=C(OC)C=C(F)C(O[C@H]4CC[C@](C(O)=O)(C)CC4)=C3)=O)CC[C@](C1)([C@@H]2C(NCC5(C)CCC5)=O)[H]
InChi Code
InChI=1S/C30H41FN2O6/c1-29(9-4-10-29)16-32-27(35)24-17-5-6-18(13-17)25(24)33-26(34)20-14-23(21(31)15-22(20)38-3)39-19-7-11-30(2,12-8-19)28(36)37/h14-15,17-19,24-25H,4-13,16H2,1-3H3,(H,32,35)(H,33,34)(H,36,37)/t17-,18+,19-,24+,25-,30+/m1/s1
InChi Key
LYUYYIGCZIZIGF-UNBDJWOASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $146

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    1 mg

    $277

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    5 mg

    $1,162

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    10 mg

    $1,743

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    Product Description

    AZD 5462 is an agonist of relaxin family peptide receptor 1 (RXFP1).1 It induces cAMP mobilization in HEK293 cells expressing the human RXFP1 (EC50 = 15.85 nM). AZD 5462 increases heart rate and mean arterial blood pressure (MABP) in rats. It increases left ventricular ejection fraction (LVEF) in a cynomolgus monkey model of heart failure induced by a high-fat diet and age when administered at doses of 1 or 10 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Granberg, K.L., Sakamaki, S., Larsson, N., et al. Discovery of clinical candidate AZD5462, a selective oral allosteric RXFP1 agonist for treatment of heart failure. J. Med. Chem. 67(6), 4419-4441 (2024).