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1359670-56-6

1359670-56-6 Structure

1359670-56-6 Structure
IdentificationBack Directory
[Name]

Anagliptin hydrochloride
[CAS]

1359670-56-6
[Synonyms]

AgliptinImpurity4
Anagliptin Impurity 4
Anagliptin hydrochloride
[Molecular Formula]

C19H26ClN7O2
[MDL Number]

MFCD30573863
[MOL File]

1359670-56-6.mol
[Molecular Weight]

419.91
Hazard InformationBack Directory
[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]
CompoundSpeciesCLtot
(l/h/kg)
Vdss
(l/h/kg)
Cmaxc
(ng/ml)
Tmaxc
(h)
T1/2
(h)
AUC
(ng/h/ml)
BA
(%)
Anagliptin hydrochloridea Rat2.00 (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).
[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
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