Anagliptin hydrochloride (Synonyms: SK-0403 hydrochloride)

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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.

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Anagliptin hydrochloride Chemical Structure

CAS No. : 1359670-56-6

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Anagliptin In-stock

3 Publications Citing Use of MCE Anagliptin hydrochloride

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

DPP-4

3.8 nM (IC₅₀)

DPP-8

68 nM (IC₅₀)

DPP-9

60 nM (IC₅₀)

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].

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

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.

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].

MedChemExpress (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‐Ldlr^tm1Her/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	CL_tot (l/h/kg)	V_dss (l/h/kg)	C_max^c (ng/ml)	T_max^c (h)	T_1/2 (h)	AUC (ng/h/ml)	BA (%)
Anagliptin hydrochloride^a	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

Molecular Weight

419.91

Formula

C₁₉H₂₆ClN₇O₂

CAS No.

1359670-56-6

SMILES

O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[C@H](C#N)CCC3)=O)C.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Anagliptin hydrochloride Related Classifications

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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-0403SK0403SK 0403Dipeptidyl PeptidaseDPPatherosclerosissmooth muscle celllipid‐loweringSMCDPP-8DPP-4Inhibitorinhibitorinhibit

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