SAR7334是一种高效的TRPC6通道特异性抑制剂（IC50=7.9nM）。
Cas No.:1333210-07-3
Sample solution is provided at 25 µL, 10mM.
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SAR7334 is a highly potent and specific TRPC6 channel inhibitor (IC₅₀=7.9nM). SAR7334 also inhibits TRPC3- and TRPC7-mediated Ca²⁺ influx into cells[1-2]. SAR7334 can be used in research related to fibrotic diseases such as focal segmental glomerulosclerosis, skeletal muscle dysfunction, as well as pulmonary arterial hypertension and pulmonary edema[3-4].
In vitro, hippocampal neurons isolated from young, middle-aged, and aged mice were treated with SAR7334 (0.1μM or 1μM) for 15 minutes. SAR7334 dose-dependently reduced the resting intracellular calcium ([Ca²⁺]ᵣ) and sodium ([Na⁺]ᵣ) concentrations in neurons, with a more pronounced reduction observed in middle-aged and aged neurons compared to young ones[5]. MPC5 podocytes were pretreated with SAR7334 (1μM) for 30 minutes, followed by stimulation with AngII (1μM) for 24 hours. SAR7334 significantly inhibited the expression of TRPC6, AT1R, and Caspase-3 proteins, increased the expression of the podocyte structural proteins Nephrin and Podocin, and reduced intracellular Ca²⁺ fluorescence intensity and cell apoptosis[6].
In vivo, spontaneously hypertensive rats (SHR) were treated with SAR7334 (oral administration; 10mg/kg) for two days. Compared to the vehicle-treated control group, the SAR7334-treated group showed no significant change in mean arterial pressure (MAP)[7]. In establishing a chemotherapy-induced peripheral neuropathy (CIPN) mouse model via cisplatin intervention, SAR7334 (10mg/kg; i.p.) was administered beginning one day before the second cycle of cisplatin treatment and continued for 7 days. SAR7334 significantly alleviated cisplatin-induced CIPN symptoms, including improving the paw withdrawal threshold in mechanical allodynia tests, shortening the response time to an adhesive stimulus, and preventing the loss of intraepidermal nerve fibers and Merkel cells in the plantar skin. Concurrently, SAR7334 ameliorated anxiety-like behaviors in CIPN mice[8].
References:
[1] Ilatovskaya DV, Palygin O, Levchenko V, et al. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299.
[2] Fang X, Dong S, Wu Y, et al. Ameliorated biomechanical properties of carotid arteries by puerarin in spontaneously hypertensive rats. BMC Complement Med Ther. 2021 Jun 22;21(1):173.
[3] Ducrocq GP, Anselmi L, Stella SL Jr, et al. Inhibition and potentiation of the exercise pressor reflex by pharmacological modulation of TRPC6 in male rats. J Physiol. 2025 Sep;603(18):5027-5052.
[4] Obara K, Takahashi S, Otake M, et al. Pharmacological Characteristics of Extracellular Ca2+ Influx Pathways Responsible for Platelet-Activating Factor-Induced Contractions in Rat Esophagus Smooth Muscle: Involvement of L-Type, Receptor-Operated, and Store-Operated Ca2+ Channels. Biol Pharm Bull. 2025;48(6):932-940.
[5] Uryash A, Flores V, Adams JA, et al. Memory and Learning Deficits Are Associated With Ca2+ Dyshomeostasis in Normal Aging. Front Aging Neurosci. 2020 Jul 16;12:224.
[6] Feng Y, Li M, Wang Y, et al. Activation of TRPC6 by AngⅡ Induces Podocyte Injury and Participates in Proteinuria of Nephrotic Syndrome. Front Pharmacol. 2022 Aug 3;13:915153.
[7] Maier T, Follmann M, Hessler G, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.
[8] Jiang YY, Li X, Hu FX, et al. Electroacupuncture alleviates chemotherapy-induced peripheral neuropathy and anxiety by reducing TRPC6/PKC-dependent activation of glutamatergic neurons in the paraventricular thalamic nucleus. Neuroscience. 2026 Jan 9;592:97-110.
SAR7334是一种高效的TRPC6通道特异性抑制剂（IC50=7.9nM）。SAR7334还可抑制TRPC3和TRPC7介导的Ca2+流入细胞[1-2]。SAR7334可用于纤维化疾病如局灶性节段性肾小球硬化、骨骼肌功能障碍以及肺动脉高压、肺水肿的相关研究[3-4]。
在体外，SAR7334（0.1μM或1μM）处理从年轻、中年和老年小鼠分离的海马神经元15分钟。SAR7334可剂量依赖性地降低神经元的静息细胞内钙离子浓度（[Ca2+]r）和钠离子浓度（[Na+]r），且在中年和老年神经元中的降低效果比在年轻神经元中更为显著[5]。SAR7334（1μM）预处理MPC5足细胞30分钟，随后以AngII（1μM）刺激24小时。SAR7334显著抑制了TRPC6、AT1R和Caspase-3蛋白的表达，增加了足细胞结构蛋白Nephrin和Podocin的表达，并降低了细胞内钙离子(Ca2+)的荧光强度及细胞凋亡[6]。
在体内，SAR7334（口服给药；10mg/kg）处理自发性高血压大鼠（SHR）两天，与仅给予溶媒的对照组相比，SAR7334处理组的平均动脉压（MAP）未见显著变化[7]。在通过顺铂干预建立化疗诱导性周围神经病变（CIPN）小鼠模型中，于顺铂给药第二周期前一天开始腹腔注射SAR7334（10mg/kg），持续7天。SAR7334显著缓解了顺铂诱导的CIPN症状，包括提高了机械性痛觉过敏的爪退缩阈值、缩短了对粘附刺激的反应时间，并阻止了足底皮肤表皮内神经纤维和Merkel细胞的丢失。同时，SAR7334改善了CIPN小鼠的焦虑样行为[8]。
| Cell experiment [1]: | |
Cell lines | Immortalized mouse MPC5 podocytes |
Preparation Method | MPC5 podocytes were cultured and matured in RPMI 1640 medium supplemented with 10% fetal bovine serum at 37°C with 5% CO₂. Cells pretreated with SAR7334 (1μM) for 30 minutes, followed by stimulation with Angiotensin II (AngII; 1μM) for 24 hours. |
Reaction Conditions | 1μM; 30min pretreatment. |
Applications | SAR7334 significantly inhibited the AngII-induced overexpression of TRPC6, AT1R, and Caspase-3 proteins. SAR7334 also attenuated the degradation of podocyte structural proteins Nephrin and Podocin. SAR7334 inhibited the fluorescence intensity of intracellular calcium (Ca²⁺) and reduced cell apoptosis. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice with cisplatin-induced chemotherapy-induced peripheral neuropathy (CIPN) |
Preparation Method | A CIPN mouse model was established by administering cisplatin. SAR7334 (10mg/kg) was intraperitoneally injected beginning one day before the second cycle of cisplatin administration and continued for 7 days. |
Dosage form | 10mg/kg; i.p.; once daily for 7 days. |
Applications | SAR7334 alleviated cisplatin-induced CIPN, indicated by an increased paw withdrawal threshold and a shortened response time to an adhesive stimulus. SAR7334 also blocked the loss of intra-epidermal nerve fibers (IENFs) and Merkel cells in the plantar skin. Furthermore, SAR7334 improved anxiety-like behaviors in CIPN mice, increasing activity in the central area of the open field and in the open arms of the elevated plus maze. SAR7334 inhibited the activation of TRPC6 and PKC, and downregulated the excitability markers p-CAMKII and c-Fos in the paraventricular thalamic nucleus (PVT). |
References: | |
| Cas No. | 1333210-07-3 | SDF | |
| Canonical SMILES | N[C@@H](C1)CCCN1[C@@H]2CC3=CC=CC=C3[C@H]2OC4=C(Cl)C=C(C#N)C=C4 | ||
| 分子式 | C21H22ClN3O | 分子量 | 367.87 |
| 溶解度 | DMSO : ≥ 370 mg/mL (1005.79 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7184 mL | 13.5918 mL | 27.1835 mL |
| 5 mM | 543.7 μL | 2.7184 mL | 5.4367 mL |
| 10 mM | 271.8 μL | 1.3592 mL | 2.7184 mL |
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