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Anagliptin hydrochloride
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。
Anagliptin hydrochloride图片
CAS NO:1359670-56-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
SK-0403 hydrochloride
产品介绍
Anagliptin (SK-0403) hydrochloride 是一种高选择性的、有效的、具有口服活性的二肽酰肽酶 4 (DPP-4) 抑制剂,IC50值为 3.8 nM,对DPP-8DDP-9的选择性相对较弱,IC50值分别为 68 nM 和 60 nM。
生物活性

Anagliptin (SK-0403) hydrochloride is a highly selective, potent, orally active inhibitor ofdipeptidyl peptidase4 (DPP-4), with anIC50of 3.8 nM, and less selective atDPP-8andDDP-9withIC50s of 68 nM and 60 nM, respectively[1].

IC50& Target

DPP-4

3.8 nM (IC50)

DPP-9

60 nM (IC50)

DPP-8

68 nM (IC50)

体外研究
(In Vitro)

Anagliptin (SK-0403) (0-100 μM; 24 h) attenuates s-DPP-4-induced smooth muscle cells proliferation[2].
Anagliptin (100 μM; 10 min) reduces TNF-α production in cultured monocytes[2].
Anagliptin (0.001-10 μM; 24 h) significantly suppresses sterol regulatory element‐inding protein activity in HepG2 cells (21% decrease)[3].

Cell Proliferation Assay[2]

Cell Line:Rat smooth muscle cells (SMC)
Concentration:1, 10 and 100 μM
Incubation Time:24 h
Result:Attenuated s-DPP-4-induced SMC proliferation in a dose-dependent manner. Inhibited LPS-induced ERK phosphorylation and markedly suppressed LPS-induced nuclear translocation of NF-κBp65.

Western Blot Analysis[2]

Cell Line:Rat smooth muscle cells (SMC)
Concentration:100 μM
Incubation Time:10 min
Result:Blocked the early- but not the late-phase ERK phosphorylation induced by s-DPP-4.
体内研究
(In Vivo)

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[2].
Anagliptin (0.3%; in diet; 4 weeks) exhibits a lipid‐lowering effect in a hyperlipidemic mice model[3].

Animal Model:Male apoliporotein E (apoE)-deficient mice[2]
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)[3]
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‐inding protein‐2 messenger ribonucleic acid expression level was significantly decreased at night.
Animal Model:Male Sprague–Dawley rats and Beagle dogs[1]
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 dogs[1]
CompoundSpeciesCLtot
(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).
Clinical Trial
分子量

419.91

Formula

C19H26ClN7O2

CAS 号

1359670-56-6

中文名称

阿拉格列汀盐酸盐;安奈格列汀盐酸盐;盐酸阿拉格列汀;盐酸安奈格列汀

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.