Teneligliptin
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MedKoo CAT#: 565087

CAS#: 760937-92-6

Description: Teneligliptin is a long-acting, orally-bioavailable inhibitor of dipeptidyl peptidase-4 (DPP-4), with hypoglycemic activity.


Chemical Structure

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Teneligliptin
CAS# 760937-92-6

Theoretical Analysis

MedKoo Cat#: 565087
Name: Teneligliptin
CAS#: 760937-92-6
Chemical Formula: C22H30N6OS
Exact Mass: 426.22
Molecular Weight: 426.580
Elemental Analysis: C, 61.94; H, 7.09; N, 19.70; O, 3.75; S, 7.52

Price and Availability

Size Price Availability Quantity
10mg USD 250 2 Weeks
50mg USD 650 2 Weeks
100mg USD 950 2 Weeks
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Related CAS #: 906093-29-6 (HBr)   1572583-29-9 (HBr hydrate)  

Synonym: Teneligliptin

IUPAC/Chemical Name: [(2S,4S)-4-[4-(5-Methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone

InChi Key: WGRQANOPCQRCME-PMACEKPBSA-N

InChi Code: InChI=1S/C22H30N6OS/c1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27/h2-6,13,19-20,23H,7-12,14-16H2,1H3/t19-,20-/m0/s1

SMILES Code: O=C([C@H]1NC[C@@H](N2CCN(C3=CC(C)=NN3C4=CC=CC=C4)CC2)C1)N5CSCC5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 426.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Imazu M, Nakano A, Ito S, Hamasaki T, Kitakaze M; TOPLEVEL investigators and study coordinators. Effects of Teneligliptin on the Progressive Left Ventricular Diastolic Dysfunction in Patients with Type 2 Diabetes Mellitus in Open-Label, Marker-Stratified Randomized, Parallel-Group Comparison, Standard Treatment-Controlled Multicenter Trial (TOPLEVEL Study): Rationale and Study Design. Cardiovasc Drugs Ther. 2019 Mar 9. doi: 10.1007/s10557-019-06871-3. [Epub ahead of print] PubMed PMID: 30850916.

2: Iwakura T, Zhao Z, Marschner JA, Devarapu SK, Yasuda H, Anders HJ. Dipeptidyl peptidase-4 inhibitor teneligliptin accelerates recovery from cisplatin-induced acute kidney injury by attenuating inflammation and promoting tubular regeneration. Nephrol Dial Transplant. 2019 Jan 8. doi: 10.1093/ndt/gfy397. [Epub ahead of print] PubMed PMID: 30624740.

3: Agrawal P, Jain A, Bansal S, Raj A. Diffuse erythematous rash after teneligliptin therapy: A case report. J Family Med Prim Care. 2018 Nov-Dec;7(6):1571-1572. doi: 10.4103/jfmpc.jfmpc_283_18. PubMed PMID: 30613561; PubMed Central PMCID: PMC6293926.

4: Takeda K, Sawazaki H, Takahashi H, Yeh YS, Jheng HF, Nomura W, Ara T, Takahashi N, Seno S, Osato N, Matsuda H, Kawada T, Goto T. The dipeptidyl peptidase-4 (DPP-4) inhibitor teneligliptin enhances brown adipose tissue function, thereby preventing obesity in mice. FEBS Open Bio. 2018 Sep 19;8(11):1782-1793. doi: 10.1002/2211-5463.12498. eCollection 2018 Nov. PubMed PMID: 30410858; PubMed Central PMCID: PMC6212644.

5: Zhang Z, Jin X, Yang C, Li Y. Teneligliptin protects against hypoxia/reoxygenation-induced endothelial cell injury. Biomed Pharmacother. 2019 Jan;109:468-474. doi: 10.1016/j.biopha.2018.10.016. Epub 2018 Nov 3. PubMed PMID: 30399583.

6: Kim Y, Kang ES, Jang HC, Kim DJ, Oh T, Kim ES, Kim NH, Choi KM, Kim SR, You J, Kim SJ, Lee MK. Teneligliptin versus sitagliptin in Korean patients with type 2 diabetes inadequately controlled with metformin and glimepiride: A randomized, double-blind, non-inferiority trial. Diabetes Obes Metab. 2019 Mar;21(3):631-639. doi: 10.1111/dom.13566. Epub 2018 Nov 22. PubMed PMID: 30362280.

7: Guliani A, Bishnoi A, Aggarwal D, Parsad D. Teneligliptin-associated bullous pemphigoid in an elderly man with diabetes. Postgrad Med J. 2018 Nov;94(1117):662-663. doi: 10.1136/postgradmedj-2018-136044. Epub 2018 Oct 13. PubMed PMID: 30317183.

8: Okahata S, Sakamoto K, Mitsumatsu T, Kondo Y, Tanaka S, Shiba T. Mechanistic insights from sequential combination therapy with a sodium glucose co-transporter-2 inhibitor and a dipeptidyl peptidase-4 inhibitor: Results from the CANARIS Trial using canagliflozin and teneligliptin. Diabetes Obes Metab. 2019 Feb;21(2):388-392. doi: 10.1111/dom.13505. Epub 2018 Sep 26. PubMed PMID: 30146790.

9: Kitada M, Ogura Y, Nitta K, Fujii M, Kanasaki K, Konishi K, Iida Y, Nakagawa A, Koya D. Effect of switching to teneligliptin from other dipeptidyl peptidase-4 inhibitors on glucose control and renoprotection in type 2 diabetes patients with diabetic kidney disease. J Diabetes Investig. 2018 Aug 23. doi: 10.1111/jdi.12917. [Epub ahead of print] PubMed PMID: 30136384.

10: Li X, Huang X, Bai C, Qin D, Cao S, Mei Q, Ye Y, Wu J. Efficacy and Safety of Teneligliptin in Patients With Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Front Pharmacol. 2018 May 4;9:449. doi: 10.3389/fphar.2018.00449. eCollection 2018. Review. PubMed PMID: 29780322; PubMed Central PMCID: PMC5946087.

11: Kadowaki T, Haneda M, Ito H, Sasaki K, Hiraide S, Matsukawa M, Ueno M. Relationship of Eating Patterns and Metabolic Parameters, and Teneligliptin Treatment: Interim Results from Post-marketing Surveillance in Japanese Type 2 Diabetes Patients. Adv Ther. 2018 Jun;35(6):817-831. doi: 10.1007/s12325-018-0704-2. Epub 2018 May 17. PubMed PMID: 29777520; PubMed Central PMCID: PMC6015125.

12: Takenaka Y, Inoue I, Nakano T, Ikeda M, Kakinuma Y, Ikegami Y, Shimada A, Noda M. Evaluation of Teneligliptin Effects on Transcriptional Activity of PPARγ in Cell-Based Assays. J Nippon Med Sch. 2018;85(2):95-101. doi: 10.1272/jnms.2018_85-15. PubMed PMID: 29731503.

13: Haneda M, Kadowaki T, Ito H, Sasaki K, Hiraide S, Ishii M, Matsukawa M, Ueno M. Safety and Efficacy of Teneligliptin in Patients with Type 2 Diabetes Mellitus and Impaired Renal Function: Interim Report from Post-marketing Surveillance. Diabetes Ther. 2018 Jun;9(3):1083-1097. doi: 10.1007/s13300-018-0416-2. Epub 2018 Apr 10. PubMed PMID: 29637459; PubMed Central PMCID: PMC5984919.

14: Minezumi T, Takeda SI, Igarashi Y, Sato K, Murakami Y, Nagata D. Hypoglycemic Coma in a Hemodialysis Patient Receiving Blood Glucose-Lowering Therapy With the Single Agent Teneligliptin. Clin Med Insights Case Rep. 2018 Mar 20;11:1179547618763358. doi: 10.1177/1179547618763358. eCollection 2018. PubMed PMID: 29581705; PubMed Central PMCID: PMC5863859.

15: Shah PA, Shrivastav PS, Vanol PG, Sanyal M. Mechanistic study for the simultaneous determination of metformin and teneligliptin in human plasma using hydrophilic interaction liquid chromatography-MS/MS. Bioanalysis. 2018 Apr 1;10(7):475-488. doi: 10.4155/bio-2018-0007. Epub 2018 Mar 21. PubMed PMID: 29561645.

16: Gosho M. Risk of Hypoglycemia After Concomitant Use of Antidiabetic, Antihypertensive, and Antihyperlipidemic Medications: A Database Study. J Clin Pharmacol. 2018 Oct;58(10):1324-1331. doi: 10.1002/jcph.1147. Epub 2018 May 15. PubMed PMID: 29762878.

17: Yajima T, Yajima K, Takahashi H, Yasuda K. The effect of dulaglutide on body composition in type 2 diabetes mellitus patients on hemodialysis. J Diabetes Complications. 2018 Aug;32(8):759-763. doi: 10.1016/j.jdiacomp.2018.05.018. Epub 2018 Jun 1. PubMed PMID: 29937137.

18: Tanaka H, Ishii T. Analysis of patients with drug-induced pemphigoid using the Japanese Adverse Drug Event Report database. J Dermatol. 2019 Mar;46(3):240-244. doi: 10.1111/1346-8138.14741. Epub 2018 Dec 21. PubMed PMID: 30575097.

19: Terasaki M, Hiromura M, Mori Y, Kohashi K, Kushima H, Koshibu M, Saito T, Yashima H, Watanabe T, Hirano T. A Dipeptidyl Peptidase-4 Inhibitor Suppresses Macrophage Foam Cell Formation in Diabetic db/db Mice and Type 2 Diabetes Patients. Int J Endocrinol. 2018 Dec 9;2018:8458304. doi: 10.1155/2018/8458304. eCollection 2018. PubMed PMID: 30627161; PubMed Central PMCID: PMC6304851.