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SR7826

CAS No. : 1219728-20-7

MCE 站：SR7826

产品活性：SR7826 是一类由双芳基脲衍生的有效，选择性和具有口服活性的 LIM 激酶 (LIMK) 抑制剂，对于 LIMK1 的 IC₅₀ 为 43 nM。SR7826 对 LIMK1 的选择性比 ROCK 和 JNK 激酶高 100 倍以上。

研究领域：Cell Cycle/DNA Damage

作用靶点：LIM Kinase (LIMK)

In Vitro: In the profiling against a panel of 61 kinases, SR7826 (compound 18b) at 1 μM inhibits only Limk1 and STK16 with ≥80% inhibition. SR7826 is highly efficient in inhibiting cell-invasion/migration in PC-3 cells. SR7826 (compound 18b) inhibits cofilin phosphorylation in A7r5 (IC₅₀ = 470 nM) and PC-3 cells (IC₅₀ < 1 ?M).
SR7826 (1 μM) inhibits contractions of prostate strips, which were induced by electrical field stimulation and inhibits cofilin phosphorylation in prostate tissues and cultured stromal cells (WPMY-1). In WPMY-1 cells, SR7826 causes breakdown of actin filaments and reduced viability.

In Vivo: SR7826 (10 mg/kg; oral gavage; once daily; for 11 days; hAPPJ20 mice) treatment significantly reduces the phosphorylation of cofilin at Ser3. SR7826 also increases both apical and basal thin spine density significantly in hAPPJ20 mice over mock-treated animals.
The plasma pharmacokinetics studies on rats are investigated. After intravenous injection, the PK properties of SR7826 (compound 18b; 1mg/kg) with a Cl of 5.2 mL/min/kg, a T_1/2 of 2.2h, an AUC of 8.4 μM*h and a C_max of 7.7 μM, and has 36% oral bioavailability in rats (oral administration; 2mg/kg).

相关产品：BMS-5  |  BMS-3  |  R-10015  |  TH-257  |  T56-LIMKi

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