产品
编 号：F444081
分子式：C19H25N7O2
分子量：383.45
分子式：C19H25N7O2
分子量：383.45
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是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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CAS No: 739366-20-2
产品详情
生物活性：
Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.
体内研究：
Anagliptin (SK-0403) (0.3%; in diet; 16 weeks) reduces atherosclerotic lesion and does not increase the number of circulating EPCs in apoliporotein E (apoE)-deficient mice.Anagliptin (0.3%; in diet; 4 weeks) exhibits a lipid‐lowering effect in a hyperlipidemic mice model.Animal Model:Male apoliporotein E (apoE)-deficient mice
Dosage:0.3%
Administration:In diet, 16 weeks
Result:Reduced DPP-4 activity in the plasma as expected and did not affect food consumption or body weight gain. Significantly reduced total cholesterol level, especially VLDL and LDL-C without affecting triglyceride level. Also decreased the α-SMA-positive area within the individual plaque.
Animal Model:Male low‐density lipoprotein receptor‐deficient mice (B6.129S7‐Ldlrtm1Her/J)
Dosage:0.3%
Administration:In diet, 4 weeks
Result:Significantly decreased the plasma total cholesterol (14% reduction) and triglyceride levels (27% reduction). Significantly decreased low‐density lipoprotein cholesterol and very low‐density lipoprotein cholesterol. Sterol regulatory element‐binding protein‐2 messenger ribonucleic acid expression level was significantly decreased at night.
Animal Model:Male Sprague–Dawley rats and Beagle dogs
Dosage:0.2, 0.5, 1 and 10 mg/kg
Administration:Oral or intravenous administration (Pharmacokinetic Studies)
Result:Selected PK parameters of Anagliptin hydrochloride in rats and dogsCompoundSpecies CLtot(l/h/kg) Vdss(l/h/kg) Cmaxc(ng/ml) Tmaxc(h) T1/2(h) AUC(ng/h/ml) BA(%)
Anagliptin hydrochlorideaRat2.00 (iv)0.68 (iv)309 (62) (po)0.8 (2.3) (po)1.9 (po)1160 (po)23 (po)
Dog0.65 (iv)0.83 (iv)261 (po)1.5 (po)1.0 (po)824 (po)100 (po)
aAnagliptin hydrochloride dose in rats, 1 mg/kg, iv (n = 3); 10 mg/kg, po (n = 3). 4a dose in dogs, 0.2 mg/kg, iv (n = 3); 0.5 mg/kg, po (n = 2).cValues in parentheses were obtained at a dose of 3 mg/kg (n = 3).
体外研究：
Anagliptin (SK-0403) (0-100 μM; 24 h) attenuates s-DPP-4-induced smooth muscle cells proliferation.Anagliptin (100 μM; 10 min) reduces TNF-α production in cultured monocytes.Anagliptin (0.001-10 μM; 24 h) significantly suppresses sterol regulatory element‐binding protein activity in HepG2 cells (21% decrease).
Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.
体内研究：
Anagliptin (SK-0403) (0.3%; in diet; 16 weeks) reduces atherosclerotic lesion and does not increase the number of circulating EPCs in apoliporotein E (apoE)-deficient mice.Anagliptin (0.3%; in diet; 4 weeks) exhibits a lipid‐lowering effect in a hyperlipidemic mice model.Animal Model:Male apoliporotein E (apoE)-deficient mice
Dosage:0.3%
Administration:In diet, 16 weeks
Result:Reduced DPP-4 activity in the plasma as expected and did not affect food consumption or body weight gain. Significantly reduced total cholesterol level, especially VLDL and LDL-C without affecting triglyceride level. Also decreased the α-SMA-positive area within the individual plaque.
Animal Model:Male low‐density lipoprotein receptor‐deficient mice (B6.129S7‐Ldlrtm1Her/J)
Dosage:0.3%
Administration:In diet, 4 weeks
Result:Significantly decreased the plasma total cholesterol (14% reduction) and triglyceride levels (27% reduction). Significantly decreased low‐density lipoprotein cholesterol and very low‐density lipoprotein cholesterol. Sterol regulatory element‐binding protein‐2 messenger ribonucleic acid expression level was significantly decreased at night.
Animal Model:Male Sprague–Dawley rats and Beagle dogs
Dosage:0.2, 0.5, 1 and 10 mg/kg
Administration:Oral or intravenous administration (Pharmacokinetic Studies)
Result:Selected PK parameters of Anagliptin hydrochloride in rats and dogsCompoundSpecies CLtot(l/h/kg) Vdss(l/h/kg) Cmaxc(ng/ml) Tmaxc(h) T1/2(h) AUC(ng/h/ml) BA(%)
Anagliptin hydrochlorideaRat2.00 (iv)0.68 (iv)309 (62) (po)0.8 (2.3) (po)1.9 (po)1160 (po)23 (po)
Dog0.65 (iv)0.83 (iv)261 (po)1.5 (po)1.0 (po)824 (po)100 (po)
aAnagliptin hydrochloride dose in rats, 1 mg/kg, iv (n = 3); 10 mg/kg, po (n = 3). 4a dose in dogs, 0.2 mg/kg, iv (n = 3); 0.5 mg/kg, po (n = 2).cValues in parentheses were obtained at a dose of 3 mg/kg (n = 3).
体外研究：
Anagliptin (SK-0403) (0-100 μM; 24 h) attenuates s-DPP-4-induced smooth muscle cells proliferation.Anagliptin (100 μM; 10 min) reduces TNF-α production in cultured monocytes.Anagliptin (0.001-10 μM; 24 h) significantly suppresses sterol regulatory element‐binding protein activity in HepG2 cells (21% decrease).
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