1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Anagliptin

Anagliptin  (Synonyms: SK-0403)

Cat. No.: HY-14877 Purity: 99.91%
COA Handling Instructions

Anagliptin (SK-0403) 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.

For research use only. We do not sell to patients.

Anagliptin Chemical Structure

Anagliptin Chemical Structure

CAS No. : 739366-20-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 127 In-stock
Solution
10 mM * 1 mL in DMSO USD 127 In-stock
Solid
5 mg USD 115 In-stock
10 mg USD 190 In-stock
50 mg USD 610 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

Anagliptin (SK-0403) 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-9

60 nM (IC50)

DPP-8

68 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‐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
Molecular Weight

383.45

Formula

C19H25N7O2

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (260.79 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6079 mL 13.0395 mL 26.0790 mL
5 mM 0.5216 mL 2.6079 mL 5.2158 mL
10 mM 0.2608 mL 1.3040 mL 2.6079 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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Anagliptin Related Classifications

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.

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Product Name:
Anagliptin
Cat. No.:
HY-14877
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