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Chemical Structure| 739366-20-2 Chemical Structure| 739366-20-2

Structure of Anagliptin
CAS No.: 739366-20-2

Chemical Structure| 739366-20-2

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Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM) and > 10 fold less potent for DPP-8 and DPP-9.

Synonyms: SK-0403

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Product Details of Anagliptin

CAS No. :739366-20-2
Formula : C19H25N7O2
M.W : 383.45
SMILES Code : O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[C@H](C#N)CCC3)=O)C
Synonyms :
SK-0403
MDL No. :N/A

Safety of Anagliptin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RAW264.7 macrophages 100 µM 10 min To evaluate the effect of Anagliptin on LPS-stimulated inflammatory responses in macrophages. Results showed Anagliptin significantly reduced the production of TNF-α, MCP-1, and IL-6, and inhibited phosphorylation of p65 and ERK1/2. J Am Heart Assoc. 2017 Jun 19;6(6):e004777

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 J mice Antigen-induced arthritis (AIA) model Oral 0.3% 4 and 8 weeks To evaluate the effect of Anagliptin on RA progression, results showed Anagliptin decreased FABP4 levels in serum and synovial macrophages, alleviating RA symptoms. Bone Res. 2022 Jun 22;10(1):45.
Sprague Dawley rats Intracranial aneurysm model Oral 300 mg/kg 2 to 4 weeks To evaluate the inhibitory effect of Anagliptin on intracranial aneurysm growth. Results showed Anagliptin significantly reduced aneurysm size, inhibited macrophage infiltration and MCP-1 expression, and decreased phosphorylation of p65. J Am Heart Assoc. 2017 Jun 19;6(6):e004777
Human Patients with type 2 diabetic nephropathy Oral 200 mg/day Once daily for 24 weeks To evaluate the effect of Anagliptin on glucose/lipid metabolism and renoprotection. Results showed that Anagliptin significantly reduced urinary albumin to creatinine ratio (UACR) and urinary liver-type fatty acid-binding protein (ULFABP) excretion, but had no significant effect on HbA1c, lipid data, systolic blood pressure, and renal function. BMJ Open Diabetes Res Care. 2017 Jul 7;5(1):e000391

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01131091 Type 2 Diabetes Mellitus PHASE1 COMPLETED 2025-11-10 Orlando, Florida, United State... More >>s|Minneapolis, Minnesota, United States Less <<
NCT00532506 Type 2 Diabetes Mellitus PHASE2 COMPLETED - Fukuoka, Japan|Gifu, Japan|Gun... More >>ma, Japan|Hokkaido, Japan|Ibaragi, Japan|Kanagawa, Japan|Kumamoto, Japan|Oita, Japan|Okinawa, Japan|Tokyo, Japan Less <<
NCT04267601 Type 2 Diabetes Mellitus UNKNOWN 2021-09-30 The Catholic University of Kor... More >>ea, Bucheon ST. Mary's hopsital, Bucheon, 14647, Korea, Republic of Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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