产品
编 号：F763027
分子式：C15H23N5O2
分子量：305.38
分子式：C15H23N5O2
分子量：305.38
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 3031476-73-7
产品详情
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 inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. 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 of cardiovascular disease.
体内研究：
TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice.TK-129 (50 mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo.TK-129 (2 or 10 mg/kg; i.v. or p.o.; single) demonstrates favorable PK properties in vivo.Animal Model:Wild C57BL/6 mice (8 to 10-week-old; half male and half female).
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).
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).
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. 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/mL?h)1038.2479.6
F (%)42.37-
体外研究：
TK-129 mediates inhibition of KDM5B activity significantly reduces the activation, migration, and proliferation of myofibroblasts induced by Ang II in vitro.TK-129 (10 μM; 48 h) shows low cytotoxicity in NRCFs and NRCMs.TK-129 (0.1, 0.2, 0.3, 0.4, 0.5 μM; 48 h) can engage toand inhibit KDM5B activity in NRCFs.
TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. 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 of cardiovascular disease.
体内研究：
TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice.TK-129 (50 mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo.TK-129 (2 or 10 mg/kg; i.v. or p.o.; single) demonstrates favorable PK properties in vivo.Animal Model:Wild C57BL/6 mice (8 to 10-week-old; half male and half female).
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).
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).
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. 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/mL?h)1038.2479.6
F (%)42.37-
体外研究：
TK-129 mediates inhibition of KDM5B activity significantly reduces the activation, migration, and proliferation of myofibroblasts induced by Ang II in vitro.TK-129 (10 μM; 48 h) shows low cytotoxicity in NRCFs and NRCMs.TK-129 (0.1, 0.2, 0.3, 0.4, 0.5 μM; 48 h) can engage toand inhibit KDM5B activity in NRCFs.
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