| Field | Specification |
|---|---|
| Alternative names | LY3473329 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C42H54N4O6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Muvalaplin, also known as LY3473329, is an orally active, selective small-molecule inhibitor of lipoprotein(a) (Lp(a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, thereby preventing disulphide bond formation and assembly of Lp(a). It lowers Lp(a) levels in transgenic mice and in cynomolgus monkeys[1][2][3][4][5]. It is supplied as a white to light yellow solid (C42H54N4O6, MW 710.90) at 99.96% purity.
Physical & Chemical Properties
| CAS Number | 2565656-70-2 |
|---|---|
| Molecular Formula | C42H54N4O6 |
| Molecular Weight | 710.90 g/mol |
| Purity | 99.96% |
| Appearance | Solid |
| Color | White to light yellow |
| SMILES | OC([C@H]([C@H]1CCNC1)CC2=CC(CN(CC3=CC(C[C@@H]([C@H]4CCNC4)C(O)=O)=CC=C3)CC5=CC(C[C@@H]([C@H]6CCNC6)C(O)=O)=CC=C5)=CC=C2)=O |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 22.22 mg/mL (31.26 mM; Requires sonication and adjust pH to 7 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: < 0.1 mg/mL (insoluble) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 22.22 mg/mL (31.26 mM) | requires sonication and adjust pH to 7 with 1 M HCl; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vivo
In the Lp(a) transgenic mouse model, Muvalaplin (1-30 mg/kg, p.o., daily for 5 days) lowers Lp(a) levels[3]. In cynomolgus monkeys, Muvalaplin (1-100 mg/kg, p.o., daily for 15 days) lowers Lp (a) levels[3].
| Animal Model | Lp (a) transgenic mouse model[3] |
|---|---|
| Dosage | 1-30 mg/kg |
| Administration | p.o., daily for 5 days |
| Result | Reduced the levels of Lp(a) with an absolute ED50 of 3 mg/kg. |
| Animal Model | Cynomolgus monkeys[3] |
|---|---|
| Dosage | 1-100 mg/kg |
| Administration | p.o., daily for 15 days |
| Result | Reduced median Lp(a) levels in a dose-dependent manner by up to 71%. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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