产品
编 号：F756276
分子式：C23H22N4O
分子量：370.45
分子式：C23H22N4O
分子量：370.45
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
结构图
CAS No: 2837128-41-1
产品详情
生物活性：
HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity.
体内研究：
HDAC6-IN-13 (Compound 35m) (20 mg/kg; p.o. and i.p.; once) displays a remarkable inhibition in LPS-induced inflammation in mice.HDAC6-IN-13 (20 mg/kg; p.o.; once) shows very high oral bioavailability (F% = 93.4%) and significant BBB permeability in mice.Animal Model:Male C57BL/6 WT mice, LPS-induced endotoxic shock model
Dosage:20 mg/kg
Administration:PO and IP, immediately after the LPS injection
Result:Significantly decreased the serum IL-1β levels in LPS-induced mice via both ip and po administration.
Animal Model:Male CD-1 mice
Dosage:5 mg/kg or 20 mg/kg
Administration:IV (5 mg/kg) or PO (20 mg/kg) (Pharmacokinetic Study)
Result:Pharmacokinetics Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral AdministrationaPK parametersHDAC6-IN-13 HDAC6-IN-13
administered dose (mg/kg)iv at 5 mg/kgoral at 20 mg/kg
Cmax (ng/mL)4604 ± 5515570 ± 551
t1/2 (h)7.95 ± 0.3706.80 ± 0.145
AUC0?inf (ng?h/mL)2755 ± 39510292 ± 1385
F%n/a93.4 ± 12.6
aHDAC6-IN-13 was administrated via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calculated using the linear trapezoidal method. The pharmacokinetic parameters were obtained using the noncompartmental method. Data are shown as mean ± SD.
体外研究：
HDAC6-IN-13 (Compound 35m) (0.1-1 μM; 24 h) is highly selective toward HDAC6 versus class I HDACs.HDAC6-IN-13 is a slow-on and slow-off tight-binding HDAC6 inhibitor, while exhibits fast-on properties for HDAC1, 2, and 3.HDAC6-IN-13 (5-20 μM; 8 h) shows anti-inflammatory activity in vitro.
HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity.
体内研究：
HDAC6-IN-13 (Compound 35m) (20 mg/kg; p.o. and i.p.; once) displays a remarkable inhibition in LPS-induced inflammation in mice.HDAC6-IN-13 (20 mg/kg; p.o.; once) shows very high oral bioavailability (F% = 93.4%) and significant BBB permeability in mice.Animal Model:Male C57BL/6 WT mice, LPS-induced endotoxic shock model
Dosage:20 mg/kg
Administration:PO and IP, immediately after the LPS injection
Result:Significantly decreased the serum IL-1β levels in LPS-induced mice via both ip and po administration.
Animal Model:Male CD-1 mice
Dosage:5 mg/kg or 20 mg/kg
Administration:IV (5 mg/kg) or PO (20 mg/kg) (Pharmacokinetic Study)
Result:Pharmacokinetics Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral AdministrationaPK parametersHDAC6-IN-13 HDAC6-IN-13
administered dose (mg/kg)iv at 5 mg/kgoral at 20 mg/kg
Cmax (ng/mL)4604 ± 5515570 ± 551
t1/2 (h)7.95 ± 0.3706.80 ± 0.145
AUC0?inf (ng?h/mL)2755 ± 39510292 ± 1385
F%n/a93.4 ± 12.6
aHDAC6-IN-13 was administrated via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calculated using the linear trapezoidal method. The pharmacokinetic parameters were obtained using the noncompartmental method. Data are shown as mean ± SD.
体外研究：
HDAC6-IN-13 (Compound 35m) (0.1-1 μM; 24 h) is highly selective toward HDAC6 versus class I HDACs.HDAC6-IN-13 is a slow-on and slow-off tight-binding HDAC6 inhibitor, while exhibits fast-on properties for HDAC1, 2, and 3.HDAC6-IN-13 (5-20 μM; 8 h) shows anti-inflammatory activity in vitro.
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