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Chemical Structure| 906093-29-6 Chemical Structure| 906093-29-6

Structure of Teneligliptin HBr
CAS No.: 906093-29-6

Chemical Structure| 906093-29-6

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Teneligliptin Hydrobromide is a DPP4 inhibitor with IC50 value of <1 nM. It is commonly used as an add on treatment when meformin is not achieving the expected glycemic goals.

Synonyms: MP-513 hydrobromide; Teneligliptin hydrobromide anhydrous; Teneligliptin hydrobromide

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Product Details of Teneligliptin HBr

CAS No. :906093-29-6
Formula : C44H65Br5N12O2S2
M.W : 1257.72
SMILES Code : O=C(N1CSCC1)[C@H]2NC[C@H](C2)N3CCN(CC3)C4=CC(C)=NN4C5=CC=CC=C5.[H]Br.[H]Br.[H]Br.[H]Br.[H]Br.O=C(N6CSCC6)[C@H]7NC[C@H](C7)N8CCN(CC8)C9=CC(C)=NN9C%10=CC=CC=C%10
Synonyms :
MP-513 hydrobromide; Teneligliptin hydrobromide anhydrous; Teneligliptin hydrobromide
MDL No. :MFCD23098790

Safety of Teneligliptin HBr

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
3T3-L1 adipocytes 1, 5, 10 µM 12 hours With DPP-4 pretreatment for 12 hours, teneligliptin significantly decreased the expression of Xdh by 19%, 30%, and 26% (at 1, 5, and 10 μM concentrations, respectively). J Diabetes Res. 2016;2016:3201534
Primary human brain microvascular endothelial cells (HBMVECs) 1, 3 mM 24 and 48 hours Teneligliptin significantly attenuated OGD/R-induced reduction in cell viability and decreased LDH release, indicating its protective effect against ischemia/reperfusion-induced cell death. RSC Adv. 2020 Jan 22;10(7):3765-3774
Primary mouse cardiomyocytes 2.5 or 5 µM 24 hours Teneligliptin significantly inhibited high glucose-induced NLRP3 inflammasome activation and increases in myocardial injury indicators (CK-MB, AST), and increased p-AMPK levels. World J Diabetes. 2024 Apr 15;15(4):724-734
3T3-L1 adipocytes 1, 5, 10 µM 3 hours Teneligliptin significantly decreased the expression of Xdh by 45%, 35%, and 34% (at 1, 5, and 10 μM concentrations, respectively). J Diabetes Res. 2016;2016:3201534
Human umbilical vein endothelial cells (HUVECs) 5 µM 48 hours TE alone or combined with CA promoted increased E-cadherin expression and suppressed VEGF expression. Int J Mol Sci. 2020 Mar 21;21(6):2164
Activated hepatic stellate cells (Ac-HSCs) 5 µM 48 hours TE alone or combined with CA significantly attenuated Ac-HSC proliferation as well as TGF-β1 and α1(I)-procollagen mRNA expression. Int J Mol Sci. 2020 Mar 21;21(6):2164

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Fischer 344 rats Choline-deficient, L-amino acid-defined diet (CDAA)-induced non-alcoholic steatohepatitis (NASH) model Oral gavage 0.3 mg/kg/day Once daily for 16 weeks TE significantly attenuated CDAA diet-induced hepatic fibrogenesis and carcinogenesis by inhibiting HSC activation, angiogenesis, and oxidative stress. Int J Mol Sci. 2020 Mar 21;21(6):2164
Wistar rats Streptozotocin-induced diabetic neuropathic pain model Intrathecal injection 2 µg/h Continuous for 7 days at a rate of 1 µL/h Co-infusion of Teneligliptin with morphine significantly attenuated morphine analgesic tolerance in diabetic neuropathic pain rats by restoring the expression of neuroprotective proteins Nrf2 and HO-1 and suppressing microglial cell activation in the spinal dorsal horn. Antioxidants (Basel). 2023 Jul 24;12(7):1478
Japanese patients with type 2 diabetes Human patients Oral 20 mg Once daily for 4 days Add-on treatment with teneligliptin significantly improved 24-h mean glucose levels, the proportion of time in normoglycemia, mean amplitude of glycemic excursions, and total area under the curve within 2 h after each meal. The proportion of time in hypoglycemia and hsCRP levels did not increase significantly compared with before teneligliptin. Values of 1,5-AG and GA were significantly improved by treatment with teneligliptin. Diabetes Technol Ther. 2014 Dec;16(12):840-5
C57BL/6 male mice Streptozotocin (STZ)-induced diabetic mouse model Oral 30 mg/kg Once daily for 4 weeks Teneligliptin significantly reversed the deterioration of myocardial hypertrophy, cardiac function indicators (fractional shortening, ejection fraction, heart rate), reduced myocardial injury indicators (CK-MB, AST, LDH) levels, and inhibited NLRP3 inflammasome activation and IL-1β release in diabetic mice. World J Diabetes. 2024 Apr 15;15(4):724-734
ICR mice MSG/HFD-induced NAFLD model mice Oral administration in drinking water 30 mg/kg per day Daily administration for 10 weeks Teneligliptin improved the histopathological appearance of the liver and decreased intrahepatic triglyceride levels, associated with downregulation of hepatic lipogenesis-related genes due to AMPK activation. Int J Mol Sci. 2015 Dec 8;16(12):29207-18
C57/BL6 mice MCAO mouse model Intraperitoneal injection 30 mg/kg/day Once daily for 14 days Teneligliptin significantly reduced brain infarct volume, ameliorated neurological damage, and improved brain permeability by increasing the expression of the tight junction protein occludin. RSC Adv. 2020 Jan 22;10(7):3765-3774
Male Wistar rats High-fat diet (HFD)-induced obesity model Oral 4.0 mg/kg/day Once daily for 4 weeks Under the HFD condition, teneligliptin significantly decreased plasma uric acid levels (by 21%) and significantly reduced Xdh expression in epididymal adipose tissue (by 32%). J Diabetes Res. 2016;2016:3201534
Wistar rats Partial sciatic nerve transection (PSNT)-induced neuropathic pain model Intrathecal injection 5 µg/1 µL/h Continuous for 7 days Teneligliptin had mild antinociceptive effects against acute pain but remarkable analgesic effects against neuropathic pain. Additionally, Teneligliptin alleviated pain by suppressing spinal astrocyte activation. Antioxidants (Basel). 2021 Sep 9;10(9):1438
Human Patients with type 2 diabetes mellitus Oral 5 mg, 10 mg, 20 mg, 40 mg Once daily for 12 to 24 weeks To evaluate the efficacy and safety of teneligliptin in patients with type 2 diabetes mellitus. Results showed that compared to placebo, teneligliptin at doses of 5 mg, 10 mg, 20 mg, and 40 mg demonstrated better efficacy in reducing HbA1c and fasting plasma glucose (FPG), with acceptable safety. Front Endocrinol (Lausanne). 2023 Dec 18;14:1282584
Mice Db/db diabetic mice Oral 60 mg/kg/day Once daily for 10 weeks Teneligliptin alleviated diabetes-related cognitive impairment by inhibiting the ER stress and NLRP3 inflammasome Aging (Albany NY). 2023 Dec 19;16(9):8336-8347

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.80mL

0.16mL

0.08mL

3.98mL

0.80mL

0.40mL

7.95mL

1.59mL

0.80mL

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
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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

References

 

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