An ApoA trivalent binder
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Muvalaplin

Item No. 39746

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αS,α′S,α′′S,3R,3′R,3′′R)-α,α′,α′′-[nitrilotris(methylene-3,1-phenylenemethylene)]tris-3-pyrrolidineacetic acid
CAS Number
2565656-70-2
Synonyms
  • LY3473329
Molecular Formula
C42H54N4O6
Formula Weight
710.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C(O)[C@H]([C@@]1([H])CNCC1)CC2=CC(CN(CC3=CC(C[C@@H]([C@@]4([H])CCNC4)C(O)=O)=CC=C3)CC5=CC(C[C@@H]([C@@]6([H])CCNC6)C(O)=O)=CC=C5)=CC=C2
InChi Code
InChI=1S/C42H54N4O6/c47-40(48)37(34-10-13-43-22-34)19-28-4-1-7-31(16-28)25-46(26-32-8-2-5-29(17-32)20-38(41(49)50)35-11-14-44-23-35)27-33-9-3-6-30(18-33)21-39(42(51)52)36-12-15-45-24-36/h1-9,16-18,34-39,43-45H,10-15,19-27H2,(H,47,48)(H,49,50)(H,51,52)/t34-,35-,36+,37-,38-,39-/m0/s1
InChi Key
BRLGERLDHZRETI-IFATVDFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $495

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    10 mg

    $891

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    25 mg

    $1,485

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    Product Description

    Muvalaplin is a trivalent binder of apolipoprotein A (ApoA).1 It selectively binds to ApoA kringle domain IV type 8 (KIV8) over KIV2 (IC50s = 22 and 3,900 nM, respectively). Muvalaplin also binds to rat plasminogen (Kd = <10 nM). It reduces the formation of lipoprotein A in a cell-free assay (IC50 = 0.09 nM). Muvalaplin decreases plasma levels of lipoprotein A in mice expressing both human ApoA and human ApoB (LPA x ApoB100; ED50 = 3 mg/kg). It reduces plasma levels of lipoprotein A in cynomolgus monkeys when administered at a dose of 100 mg/kg per day. Muvalaplin (31.6 mg/kg for four days) decreases ex vivo plasmin activity and plasminogen levels after administration in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Diaz, N., Perez, C., Escribano, A.M., et al. Discovery of potent small-molecule inhibitors of lipoprotein(a) formation. Nature 629(8013), 945-950 (2024).