2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. Anagliptin hydrochloride

Anagliptin hydrochloride  (Synonyms: SK-0403 hydrochloride)

目录号: HY-14877A
产品使用指南

摩尔计算器

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-8 和 DDP-9 的选择性相对较弱，IC50 值分别为 68 nM 和 60 nM。

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Anagliptin hydrochloride Chemical Structure

Anagliptin hydrochloride Chemical Structure

CAS No. : 1359670-56-6

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Anagliptin hydrochloride 的其他形式现货产品:

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Other Forms of Anagliptin hydrochloride:

Anagliptin hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Dipeptidyl Peptidase 亚型特异性产品:

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anagliptin (SK-0403) hydrochloride 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[1].

IC50 & Target

DPP-4

3.8 nM (IC50)

DPP-8

68 nM (IC50)

DPP-9

60 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 500 μM
Compound: 4a, anagliptin hydrochloride
Inhibition of human ERG expressed in HEK293 cells by patch clamp assay
Inhibition of human ERG expressed in HEK293 cells by patch clamp assay
[PMID: 22019046]
Sf9 IC50
60 nM
Compound: 4a, anagliptin hydrochloride
Inhibition of human recombinant DPP-9 expressed in Sf9 cells using H-Gly-Pro-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by fluorescence assay
Inhibition of human recombinant DPP-9 expressed in Sf9 cells using H-Gly-Pro-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by fluorescence assay
[PMID: 22019046]
Sf9 IC50
68 nM
Compound: 4a, anagliptin hydrochloride
Inhibition of human recombinant DPP-8 expressed in Sf9 cells using H-Gly-Pro-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by fluorescence assay
Inhibition of human recombinant DPP-8 expressed in Sf9 cells using H-Gly-Pro-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by fluorescence assay
[PMID: 22019046]
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‐binding protein activity in HepG2 cells (21% decrease)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Anagliptin hydrochloride 相关抗体:

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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‐binding 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]
Compound Species CLtot
(l/h/kg)		 Vdss
(l/h/kg)		 Cmaxc
(ng/ml)		 Tmaxc
(h)		 T1/2
(h)		 AUC
(ng/h/ml)		 BA
(%)
Anagliptin hydrochloridea Rat 2.00 (iv) 0.68 (iv) 309 (62) (po) 0.8 (2.3) (po) 1.9 (po) 1160 (po) 23 (po)
Dog 0.65 (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
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.
纯度 & 产品资料
参考文献

Anagliptin hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Anagliptin1359670-56-6SK-0403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SK0403SK 0403Dipeptidyl PeptidaseDPPatherosclerosissmooth muscle celllipid‐loweringSMCDPP-8DPP-4Inhibitorinhibitorinhibit

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