| Bioactivity | TRPC4/5-IN-2 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC4/5-IN-2 has good biosafety and low liver and kidney toxicity, and is expected to play an important role in the treatment of chronic kidney disease (CKD)[1]. |
| Target | IC50: 81 nM (TRPC5). |
| Invitro | TRPC4/5-IN-2 (化合物 12) (30 μM, 24 h) 对肝细胞和 HK-2 肾细胞具有较低的细胞毒性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> TRPC4/5-IN-2 相关抗体: Cell Viability Assay[1]. Cell Line: |
| In Vivo | TRPC4/5-IN-2 (化合物 12) (10 mL/kg, p.o.,) 在雄性 ICR 小鼠中药代动力学情况良好，且低血脑屏障通过率避免了中枢神经系统中 TRPC5 活性的不必要抑制[1]。TRPC4/5-IN-2 (化合物 12) (500 mg/kg, p.o.,) 在 C57 小鼠中具有良好的生物安全性[1]。TRPC4/5-IN-2 (化合物 12) (10 mg/kg, p.o., 每天 2 次，持续 3 周) 对大鼠低血压性肾损伤具有疗效[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C18H16Cl2FN5O2 |
| Molar Mass | 424.26 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Xu Yuanyuan, et al. Discovery of pyridazinone derivatives bearing tetrahydroimidazo[1,2-a] pyrazine scaffold as potent inhibitors of transient receptor potential canonical 5 to ameliorate hypertension-induced renal injury in rats. Eur.J.Med.Chem. 2024, 275:116565. |