Muvalaplin
Based on 1 Customer Validation
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.
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
-
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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
Lipoprotein(a) (Lp(a))[1]
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%.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 2565656-70-2
-
性状 Solid
-
分子量 710.90
-
分子式 C42H54N4O6
-
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
-
別名
LY3473329
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
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)
純度とドキュメンテーション
-
データシート (277 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
[1]. Bhatia HS, et al. Lipoprotein(a): Evidence for Role as a Causal Risk Factor in Cardiovascular Disease and Emerging Therapies. J Clin Med. 2022 Oct 13;11(20):6040. [Content Brief]
[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]
[4]. Hooper AJ, et al. Potential of muvalaplin as a lipoprotein(a) inhibitor. Expert Opin Investig Drugs. 2024 Jan;33(1):5-7. [Content Brief]
[5]. Norata GD, et al. Oral strategies to target proprotein convertase subtilisin/kexin type 9 and lipoprotein(a): the new frontier of lipid lowering. Eur Heart J. 2023 Dec 21;44(48):5018-5020. [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 |
|---|---|---|---|---|---|
| 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
Powered by Bioz