| Description | Reldesemtiv (CK-2127107) is a selective activator of fast skeletal muscle troponin with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in the heart failure model. |
| In vitro | Reldesemtiv 选择性地与快速骨骼肌肌钙蛋白复合体结合，并对钙[1]增敏。 |
| In vivo | Reldesemtiv提高了去皮LAD-HF骨骼纤维的肌节Ca2+敏感性。在运动耐受性差的LAD-HF大鼠中，Reldesemtiv（10 mg/kg; p.o.）显著改善了旋转木马测试的表现。此外，Reldesemtiv（10 mg/kg; i.v.）提高了快速骨骼肌纤维的Ca2+敏感性，并在次最大刺激频率下增加了肌肉力量[1]。 |
| Synonyms | CK-2127107 |
| molecular weight | 384.38 |
| Molecular formula | C19H18F2N6O |
| CAS | 1345410-31-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 225 mg/mL (585.4 mM), Sonication is recommended. |
| References | 1. Hwee DT, et al. The small-molecule fast skeletal troponin activator, CK-2127107, improves exercise tolerance in a rat model of heart failure. J Pharmacol Exp Ther. 2015 Apr;353(1):159-68. 2. Andrews JA, et al. CK-2127107 amplifies skeletal muscle response to nerve activation in humans. Muscle Nerve. 2018 May;57(5):729-734. |