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TK-129
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TK-129图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
TK-129 是一种口服有效的、低毒的强效KDM5B抑制剂 (具有高亲和力;IC50=44 nM)。TK-129 通过抑制KDM5B和阻断KDM5B相关的Wnt通路,来发挥心脏保护作用。TK-129 能在体外减少 Ang II 诱导的心脏成纤维细胞的活化,并在体内减少异丙肾上腺素诱导的心肌重塑和纤维化。TK-129 可用于心血管疾病的研究。
生物活性

TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity;IC50=44 nM). TK-129 exerts cardioprotective effects by inhibitingKDM5Band blocking theKDM5B-associatedWntpathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies ofcardiovascular disease[1].

IC50& Target[1]

KDM5

44 nM (IC50)

体外研究
(In Vitro)

TK-129 mediates inhibition of KDM5B activity significantly reduces the activation, migration, and proliferation of myofibroblasts induced by Ang II in vitro[1].
TK-129 (10 μM; 48 h) shows low cytotoxicity in NRCFs and NRCMs[1].
TK-129 (0.1, 0.2, 0.3, 0.4, 0.5 μM; 48 h) can engage toand inhibit KDM5B activity in NRCFs[1].

Cell Cytotoxicity Assay[1]

Cell Line:NRCFs and NRCMs
Concentration:10 μM
Incubation Time:48 h
Result:Exhibited the cell survival rates were almost more than 90%.

Western Blot Analysis[1]

Cell Line:NRCFs
Concentration:0.1, 0.2, 0.3, 0.4, 0.5 μM
Incubation Time:48 h
Result:Increased the expression level of KDM5B substrate H3K4me3 protein in a concentration-dependent manner.
体内研究
(In Vivo)

TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice[1].
TK-129 (50 mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo[1].
TK-129 (2 or 10 mg/kg; i.v. or p.o.; single) demonstrates favorable PK properties in vivo[1].

Animal Model:Wild C57BL/6 mice (8 to 10-week-old; half male and half female)[1].
Dosage:2 g/kg
Administration:Oral gavage, single.
Result:Exhibited all mice in the acute toxicity group survived and gained weight normally, after 2 weeks.
Animal Model:C57BL/6 mice (isoproterenol (ISO)-induced)[1].
Dosage:50 mg/kg
Administration:Oral gavage, twice daily for 24 days.
Result:Alleviated myocardial remodeling induced by ISO in vivo.
Animal Model:Male SD Rats (223.5-265.1 g)[1].
Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.).
Administration:Intravenous injection or oral gavage; single.
Result:1.19Pharmacokinetic Parameters of TK-129 in Male SD Rats[1].
PO (10 mg/kg)IV (2 mg/kg)
CL (L/h/kg)9.94.2
Vss(L/kg)33.42.7
T1/2(h)2.40.4
Tmax(h)0.4-
Cmax(ng/mL)709.71229.1
AUC0-24(ng/mLoh)1038.2479.6
F (%)42.37-
分子量

305.38

Formula

C15H23N5O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.