Muvalaplin
Based on 1 Customer Validation
Muvalaplin (LY3473329) is an orally active small molecule apolipoprotein a (apolipoprotein a) inhibitor that binds to the KIV8 domain (Kd = 22 nM) and kringle IV domains 7 and 8, blocks the non-covalent interaction between apo (a) and apoB-100, and prevents Lp (a) assembly, thereby lowering circulating Lp (a) levels. Muvalaplin can be used in research on atherosclerotic cardiovascular disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.96%
- CAS 番号: 2565656-70-2
- 分子式: C42H54N4O6
- 分子量:710.90
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[3]|
apo(a) |
apoB |
体外実験
Muvalaplin (LY3473329 ) (2 h) effectively inhibits the formation of Lp (a) particles with an IC50 of 0.09 nM[3].
Muvalaplin does not affect plasmin activity and reduces Lp (a) formation in a cell-free in vitro assembly assay[1].
Muvalaplin selectively binds to the apo (a) KIV8 domain with a Kd of 22 nM, demonstrating selectivity over the KIV2 domain[3].
Muvalaplin (0.001-1000 µM; 15 h) does not directly modulate plasminogen activation or plasmin activity in human platelet-poor plasma[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
Muvalaplin (1-100 mg/kg; p.o.; twice daily; 5 days) reduces Lp (a) levels in Lp (a) transgenic mice with an ED50 of 3 mg/kg and a maximum reduction of 92%[3].
Muvalaplin (1-100 mg/kg; p.o.; q.d.; 14 days) reduces median Lp (a) levels by up to 71% in cynomolgus monkeys[3].
Muvalaplin (3.2-31.6 mg/kg; p.o.; QD; 4 days) reduces plasma plasmin activity and plasminogen protein levels in rats in a dose-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lp(a) double transgenic mice (B6.SJL-Tg(APOB)1102Sgy Tg(Alb-LPA)32Arte; female; 7-17 months)[3]
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Dosage:1, 3, 10, 30, and 100 mg/kg
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Administration:p.o.; BID; 5 days
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Result:Reduced Lp(a) levels with an absolute ED50 of 3 mg/kg.
Achieved a maximum Lp(a) reduction of 92% after five days of BID oral dosing.
Increased plasma levels of LY3473329-HCl salt in a dose-dependent manner.
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Animal Model:Macaca fascicularis (female or male; 2.0-5.0 kg)[3]
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Dosage:1, 10, and 100 mg/kg
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Administration:p.o.; QD; 14 days
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Result:Reduced median Lp(a) levels in a dose-dependent manner by up to 71% in the 100 mg/kg once daily (QD) cohort, compared with baseline.
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Animal Model:Sprague Dawley (male; 8-9 weeks old; average body weight 310 g)[3]
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Dosage:3.2, 10.5, and 31.6 mg/kg
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Administration:p.o.; QD; 4 days
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Result:Decreased plasma plasmin activity.
Decreased plasma levels of plasminogen protein in a dose-dependent manner.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2565656-70-2
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性状 Solid
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分子量 710.90
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分子式 C42H54N4O6
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Color White to light yellow
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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
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別名
LY3473329
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
純度とドキュメンテーション
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データシート (293 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Nicholls SJ, et al. Muvalaplin, an Oral Small Molecule Inhibitor of Lipoprotein(a) Formation: A Randomized Clinical Trial. JAMA. 2023 Sep 19;330(11):1042-1053. [Content Brief]
[3]. Diaz N, et al. Discovery of potent small-molecule inhibitors of lipoprotein(a) formation. Nature. 2024 May;629(8013):945-950. [Content Brief]
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 |
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| 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 |
Muvalaplin 関連分類
HY-152857 関連分類
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