Anagliptin hydrochloride
Anagliptin hydrochloride Basic information
- Product Name:
- Anagliptin hydrochloride
- Synonyms:
-
- Anagliptin hydrochloride
- Anagliptin Impurity 4
- AgliptinImpurity4
- CAS:
- 1359670-56-6
- MF:
- C19H26ClN7O2
- MW:
- 419.91
- Mol File:
- 1359670-56-6.mol
Anagliptin hydrochloride Usage And Synthesis
Uses
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].
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‐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]
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). |
IC 50
DPP-4: 3.8 nM (IC50); DPP-8: 68 nM (IC50); DPP-9: 60 nM (IC50)
References
[1] Kato N, et al. Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor. Bioorg Med Chem. 2011 Dec 1;19(23):7221-7. DOI:10.1016/j.bmc.2011.09.043
[2] Ervinna N, et al. Anagliptin, a DPP-4 inhibitor, suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction and attenuates atherosclerosis in male apo E-deficient mice. Endocrinology. 2013 Mar;154(3):1260-70. DOI:10.1210/en.2012-1855
[3] Yano W, et al. Mechanism of lipid-lowering action of the dipeptidyl peptidase-4 inhibitor, anagliptin, in low-density lipoprotein receptor-deficient mice. J Diabetes Investig. 2017 Mar;8(2):155-160. DOI:10.1111/jdi.12593
Anagliptin hydrochlorideSupplier
- Tel
- 028-86040038 13980902949;
- market@dingdangchem.com
- Tel
- 028-85255396 18302801538
- cdnovell@163.com
- Tel
- +86-400-002-6226 +86-13028896684;
- sales@rrkchem.com
- Tel
- 020-36607679 19925672674
- 3008233746@qq.com
- Tel
- 86-714-3992388
- overseasales1@yongstandards.com