2681302-83-8
Chemical Structure
TMDJ-035
- CAS No.: 2681302-83-8
- Formula:C16H12F3N5O
- Molecular Weight:347.29
InChIKey: IRUXEBHABFUBKY-UHFFFAOYSA-N
SMILES: FC1=CC(F)=CC(C2=NN(CC(N(C3=CC=C(F)C=C3)C)=O)N=N2)=C1
Biological Activity: TMDJ-035 is a high-affinity, selective RyR2 inhibitor with an EC50 of 0.0130 μM. TMDJ-035 reduces RyR2 protein expression without affecting action potential-induced Ca2+ transients. TMDJ-035 decreases ATP content and intracellular Ca2+ levels. TMDJ-035 inhibits arrhythmias in a CPVT mouse model carrying mutant RyR2s. TMDJ-035 has no effect on electrocardiogram parameters or cardiac systolic function. TMDJ-035 exacerbates heart failure in mouse myocardial infarction models and hypoxic cardiomyocytes by altering cardiac function, causing tissue damage, promoting inflammatory infiltration, collagen deposition, and changes in Myosin heavy chain/actin expression. TMDJ-035 can be used in studies related to heart failure, catecholaminergic polymorphic ventricular tachycardia, and arrhythmias[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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TMDJ-035 | 99.92% | TMDJ-035 is a high-affinity, selective RyR2 inhibitor with an EC50 of 0.0130 μM. TMDJ-035 reduces RyR2 protein expression without affecting action potential-induced Ca2+ transients. TMDJ-035 decreases ATP content and intracellular Ca2+ levels. TMDJ-035 inhibits arrhythmias in a CPVT mouse model carrying mutant RyR2s. TMDJ-035 has no effect on electrocardiogram parameters or cardiac systolic function. TMDJ-035 exacerbates heart failure in mouse myocardial infarction models and hypoxic cardiomyocytes by altering cardiac function, causing tissue damage, promoting inflammatory infiltration, collagen deposition, and changes in Myosin heavy chain/actin expression. TMDJ-035 can be used in studies related to heart failure, catecholaminergic polymorphic ventricular tachycardia, and arrhythmias. | ||||||||||||||||||||
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- [1]. Jiang S, et al. CACNB4 attenuates cardiac dysfunction by regulating calcium and ATP levels via interaction with RyR2. Eur J Med Res. 2025;30(1):1071. Published 2025 Nov 5. [Content Brief]
- [2]. Kurebayashi N, et al. Effects of a high-affinity and selective RyR2 inhibitor on Ca2+ signals in cardiomyocytes and arrhythmias in CPVT model mice[J]. Biophysical Journal, 2024, 123(3): 23a.
- [3]. Ishida R, et al. A potent and selective cis-amide inhibitor of ryanodine receptor 2 as a candidate for cardiac arrhythmia treatment. Eur J Med Chem. 2023;262:115910. [Content Brief]
Keywords
