| Company Name: |
Chengdu DingDang Pharmaceutical Co., Ltd.
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| Tel: |
028-86040038 13980902949; |
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market@dingdangchem.com |
| Products Intro: |
Product Name:Anagliptin hydrochloride
CAS:1359670-56-6
Purity:＞96% Package:25mg;50mg;100mg;500mg
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| Company Name: |
Artis Biotech Co. Ltd.
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| Tel: |
19138486554 18108108965 |
| Email: |
sales@artisbio.com |
| Products Intro: |
Product Name:Anagliptin hydrochloride
CAS:1359670-56-6
Purity:98% Package:1mg 5mg 10mg 100mg 500mg 1kg
|
| Company Name: |
Chengdu Novel Biomedical Co., Ltd.
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| Tel: |
028-85255396 18302801538 |
| Email: |
cdnovell@163.com |
| Products Intro: |
Product Name:Anagliptin hydrochloride
CAS:1359670-56-6
Purity:98% HPLC Package:50mg;1g
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Anagliptin hydrochloride manufacturers
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| | Anagliptin hydrochloride Basic information |
| | Anagliptin hydrochloride Chemical Properties |
| | 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]
| 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).
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| | 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 hydrochloride Preparation Products And Raw materials |
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