2. Metabolic Enzyme/Protease
  3. LDLR
  4. Muvalaplin

Muvalaplin (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, preventing the disulphide bond and Lp(a) formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys.

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Muvalaplin

Muvalaplin Chemical Structure

CAS No. : 2565656-70-2

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Description

Muvalaplin (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, preventing the disulphide bond and Lp(a) formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys[1][2][3][4][5].

IC50 & Target

Lipoprotein(a) (Lp(a))[1]
In Vivo

Muvalaplin (1-30 mg/kg, p.o., daily for 5 days) reduces the levels of Lp(a) in the Lp (a) transgenic mouse model[3].
Muvalaplin (1-100 mg/kg, p.o., daily for 15 days) reduces the levels of Lp (a) levels in cynomolgus monkeys[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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%.
Essai clinique
Masse moléculaire

710.90

Formule

C42H54N4O6
CAS No.
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 22.22 mg/mL (31.26 mM; ultrasonic 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4067 mL 7.0333 mL 14.0667 mL
5 mM 0.2813 mL 1.4067 mL 2.8133 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Pureté et documentation

Purity: 99.96%

SDS (252 KB)

COA (254 KB) HNMR (314 KB) LCMS (86 KB)

Instruction de manipulation (2659 KB)
Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4067 mL 7.0333 mL 14.0667 mL 35.1667 mL
5 mM 0.2813 mL 1.4067 mL 2.8133 mL 7.0333 mL
10 mM 0.1407 mL 0.7033 mL 1.4067 mL 3.5167 mL
15 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3444 mL
20 mM 0.0703 mL 0.3517 mL 0.7033 mL 1.7583 mL
25 mM 0.0563 mL 0.2813 mL 0.5627 mL 1.4067 mL
30 mM 0.0469 mL 0.2344 mL 0.4689 mL 1.1722 mL
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Muvalaplin Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Muvalaplin2565656-70-2LY3473329LY 3473329LY-3473329LDLRLow-density lipoprotein receptororally activeLp (a)transgenic micecynomolgus monkeysInhibitorinhibitorinhibit

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