Teneligliptin HBr | CAS#760937-92-6 | 906093-29-6 | DPP-4 inhibitor

MedKoo Cat#: 319879 | Name: Teneligliptin HBr

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Teneligliptin is a pharmaceutical drug for the treatment of type 2 diabetes mellitus. It belongs to the class of anti-diabetic drugs known as dipeptidyl peptidase-4 inhibitors or "gliptins". It is approved for use in Japan.

Chemical Structure

Teneligliptin HBr

CAS#906093-29-6 (HBr)

Theoretical Analysis

MedKoo Cat#: 319879

Name: Teneligliptin HBr

CAS#: 906093-29-6 (HBr)

Chemical Formula: C44H65Br5N12O2S2

Exact Mass: 426.2202

Molecular Weight: 1257.73

Elemental Analysis: C, 42.02; H, 5.21; Br, 31.77; N, 13.36; O, 2.54; S, 5.10

Price and Availability

Size	Price	Availability
100mg	USD 250.00	2 Weeks
250mg	USD 450.00	2 Weeks
500mg	USD 750.00	2 Weeks

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Related CAS #

760937-92-6 (free base) 906093-29-6 (HBr) 1572583-29-9 (HBr hydrate)

Synonym

Teneligliptin. trade name Tenelia; Teneligliptin HBr; Teneligliptin hydrobromide;

IUPAC/Chemical Name

((2S,4S)-4-(4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl)pyrrolidin-2-yl)(thiazolidin-3-yl)methanone; hydrobromide (2:5)

InChi Key

LUXIOMHUGCXFIU-MAYGPZJUSA-N

InChi Code

InChI=1S/2C22H30N6OS.5BrH/c2*1-17-13-21(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*2-6,13,19-20,23H,7-12,14-16H2,1H3;5*1H/t2*19-,20-;;;;;/m00...../s1

SMILES Code

O=C([C@H]1NC[C@@H](N2CCN(C3=CC(C)=NN3C4=CC=CC=C4)CC2)C1)N5CSCC5.O=C([C@H]6NC[C@@H](N7CCN(C8=CC(C)=NN8C9=CC=CC=C9)CC7)C6)N%10CSCC%10.[H]Br.[H]Br.[H]Br.[H]Br.[H]Br

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, not in water

Shelf Life

>2 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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 1,257.73 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.

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

1: Nakamaru Y, Akahoshi F, Iijima H, Hisanaga N, Kume T. Tissue distribution of teneligliptin in rats and comparisons with data reported for other dipeptidyl peptidase-4 inhibitors. Biopharm Drug Dispos. 2016 Jan 8. doi: 10.1002/bdd.2003. [Epub ahead of print] PubMed PMID: 26749565. 2: Hong S, Park CY, Han KA, Chung CH, Ku BJ, Jang HC, Ahn CW, Lee MK, Moon MK, Son HS, Lee CB, Cho YW, Park SW. Efficacy and safety of teneligliptin, a novel dipeptidyl peptidase-4 inhibitor, in Korean patients with type 2 diabetes mellitus: A 24-week multicenter, randomized, double-blind, placebo-controlled phase III trial. Diabetes Obes Metab. 2016 Jan 9. doi: 10.1111/dom.12631. [Epub ahead of print] PubMed PMID: 26749529. 3: Ideta T, Shirakami Y, Miyazaki T, Kochi T, Sakai H, Moriwaki H, Shimizu M. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18. doi: 10.3390/ijms161226156. PubMed PMID: 26670228; PubMed Central PMCID: PMC4691103. 4: Scott LJ. Teneligliptin: a review in type 2 diabetes. Clin Drug Investig. 2015 Nov;35(11):765-72. doi: 10.1007/s40261-015-0348-9. PubMed PMID: 26475720. 5: Shantikumar S, Satheeshkumar N, Srinivas R. Pharmacokinetic and protein binding profile of peptidomimetic DPP-4 inhibitor - Teneligliptin in rats using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:194-200. doi: 10.1016/j.jchromb.2015.08.023. Epub 2015 Aug 24. PubMed PMID: 26340762. 6: Wada N, Mori K, Nakagawa C, Sawa J, Kumeda Y, Shoji T, Emoto M, Inaba M. Improved glycemic control with teneligliptin in patients with type 2 diabetes mellitus on hemodialysis: Evaluation by continuous glucose monitoring. J Diabetes Complications. 2015 Nov-Dec;29(8):1310-3. doi: 10.1016/j.jdiacomp.2015.07.002. Epub 2015 Jul 3. PubMed PMID: 26298521. 7: Hashikata T, Yamaoka-Tojo M, Kakizaki R, Nemoto T, Fujiyoshi K, Namba S, Kitasato L, Hashimoto T, Kameda R, Maekawa E, Shimohama T, Tojo T, Ako J. Teneligliptin improves left ventricular diastolic function and endothelial function in patients with diabetes. Heart Vessels. 2015 Aug 13. [Epub ahead of print] PubMed PMID: 26266630. 8: Sameshima A, Wada T, Ito T, Kashimura A, Sawakawa K, Yonezawa R, Tsuneki H, Ishii Y, Sasahara M, Saito S, Sasaoka T. Teneligliptin improves metabolic abnormalities in a mouse model of postmenopausal obesity. J Endocrinol. 2015 Oct;227(1):25-36. doi: 10.1530/JOE-15-0239. Epub 2015 Aug 11. PubMed PMID: 26264980. 9: Ito R, Fukui T, Hayashi T, Osamura A, Ohara M, Hara N, Higuchi A, Yamamoto T, Hirano T. Teneligliptin, a Dipeptidyl Peptidase-4 Inhibitor, Improves Early-Phase Insulin Secretion in Drug-Naïve Patients with Type 2 Diabetes. Drugs R D. 2015 Sep;15(3):245-51. doi: 10.1007/s40268-015-0096-6. PubMed PMID: 26224337; PubMed Central PMCID: PMC4561050. 10: Nakamaru Y, Hayashi Y, Davies M, Jürgen Heuer H, Hisanaga N, Akimoto K. Investigation of Potential Pharmacokinetic Interactions Between Teneligliptin and Metformin in Steady-state Conditions in Healthy Adults. Clin Ther. 2015 Sep;37(9):2007-18. doi: 10.1016/j.clinthera.2015.06.012. Epub 2015 Jul 23. PubMed PMID: 26212570. 11: Nagai H, Fujiwara S, Takahashi Y, Nishigori C. Ameliorating effect of the novel dipeptidyl peptidase-4 inhibitor teneligliptin on psoriasis: A report of two cases. J Dermatol. 2015 Nov;42(11):1094-7. doi: 10.1111/1346-8138.12955. Epub 2015 May 28. PubMed PMID: 26031638. 12: Oguma T, Kuriyama C, Nakayama K, Matsushita Y, Yoshida K, Kiuchi S, Ikenaga Y, Nakamaru Y, Hikida K, Saito A, Arakawa K, Oka K, Ueta K, Shiotani M. The effect of combined treatment with canagliflozin and teneligliptin on glucose intolerance in Zucker diabetic fatty rats. J Pharmacol Sci. 2015 Apr;127(4):456-61. doi: 10.1016/j.jphs.2015.03.006. Epub 2015 Mar 28. PubMed PMID: 25892328. 13: Kadowaki T, Marubayashi F, Yokota S, Katoh M, Iijima H. Safety and efficacy of teneligliptin in Japanese patients with type 2 diabetes mellitus: a pooled analysis of two Phase III clinical studies. Expert Opin Pharmacother. 2015 May;16(7):971-81. doi: 10.1517/14656566.2015.1032249. Epub 2015 Apr 10. PubMed PMID: 25861982. 14: Moroi M, Kubota T. Diuretic and Natriuretic Effects of Dipeptidyl Peptidase-4 Inhibitor Teneligliptin: The Contribution of Glucagon-like Peptide-1. J Cardiovasc Pharmacol. 2015 Aug;66(2):159-64. doi: 10.1097/FJC.0000000000000258. PubMed PMID: 25853991. 15: Morishita R, Nakagami H. Teneligliptin : expectations for its pleiotropic action. Expert Opin Pharmacother. 2015 Feb;16(3):417-26. doi: 10.1517/14656566.2015.1000301. Review. PubMed PMID: 25597385. 16: Kim MK, Rhee EJ, Han KA, Woo AC, Lee MK, Ku BJ, Chung CH, Kim KA, Lee HW, Park IB, Park JY, Chul Jang HC, Park KS, Jang WI, Cha BY. Efficacy and safety of teneligliptin, a dipeptidyl peptidase-4 inhibitor, combined with metformin in Korean patients with type 2 diabetes mellitus: a 16-week, randomized, double-blind, placebo-controlled phase III trial. Diabetes Obes Metab. 2015 Mar;17(3):309-12. doi: 10.1111/dom.12424. Epub 2015 Jan 18. PubMed PMID: 25475929. 17: Nakamaru Y, Emoto C, Shimizu M, Yamazaki H. Human pharmacokinetic profiling of the dipeptidyl peptidase-IV inhibitor teneligliptin using physiologically based pharmacokinetic modeling. Biopharm Drug Dispos. 2015 Apr;36(3):148-62. doi: 10.1002/bdd.1928. Epub 2015 Jan 28. PubMed PMID: 25450725. 18: Kinoshita S, Kondo K. Evaluation of pharmacokinetic and pharmacodynamic interactions of canagliflozin and teneligliptin in Japanese healthy male volunteers. Expert Opin Drug Metab Toxicol. 2015 Jan;11(1):7-14. doi: 10.1517/17425255.2015.982531. Epub 2014 Nov 26. PubMed PMID: 25424014. 19: Kusunoki M, Sato D, Nakamura T, Oshida Y, Tsutsui H, Natsume Y, Tsutsumi K, Miyata T. DPP-4 Inhibitor Teneligliptin Improves Insulin Resistance and Serum Lipid Profile in Japanese Patients with Type 2 Diabetes. Drug Res (Stuttg). 2015 Oct;65(10):532-4. doi: 10.1055/s-0034-1390419. Epub 2014 Nov 4. PubMed PMID: 25368904. 20: Tsuchimochi W, Ueno H, Yamashita E, Tsubouchi C, Sakoda H, Nakamura S, Nakazato M. Teneligliptin improves glycemic control with the reduction of postprandial insulin requirement in Japanese diabetic patients. Endocr J. 2015;62(1):13-20. doi: 10.1507/endocrj.EJ14-0393. Epub 2014 Sep 25. PubMed PMID: 25252844.