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668270-12-0 (Linagliptin)

1

Identification

Linagliptin Linagliptin
Name Linagliptin
Formula C25H28N8O2
MW 472.54
CAS No. 668270-12-0
EINECS
Smiles O=C1N(C2=C(C(N1CC3=NC(C)=C4C=CC=CC4=N3)=O)N(CC#CC)C(N5CCC[[email protected]@H](N)C5)=N2)C
Synonyms BI 1356;Tradjenta;BI-1356;BI1356; (R)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione
InChI InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1
2

Introduction

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. IC50 value: 1 nM [1] Target: DPP-4 in vitro: Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM) [1].

Background Information

A novel potent and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with potential use in the treatment of type 2 diabetes. ......by BOC Sciences
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. ......by MedChemexpress Co., Ltd.
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. ......by Selleck Chemicals LLC
Linagliptin is a DPP-4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes . Two pharmacological characteristics that sets linagliptin apart from other DPP-4 inhibitors is that it has a non-linear pharmacokinetic profile and is not primarily eliminated by the renal system. FDA approved on May 2, 2011. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Male db/db mice
Dosage ≤1 mg/kg
Formulation Linagliptin is dissolved in 0.1 N HCl and subsequently diluted with a 0.5% aqueous hydroxyethylcellulose solution (final HCl concentration 3 mM).
Administration Administered via p.o.
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000028529

Storage condition

Solubility

DMSO 17 mg/ml; Water <1 mg/ml by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 17 mg/mL (35.97 mM); Ethanol1 mg/mL (2.11 mM); Water<1 mg/mL (<1 mM); In vivo 0.5% hydroxyethyl cellulose30 mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Linagliptin Beth Israel Deaconess Medical Center Non-insulin dependent diabetes 2013/10/31 2015/3/31 Phase 4 Clinical
Linagliptin Boehringer Ingelheim Pharmaceuticals Inc Non-insulin dependent diabetes 2013/7/31 2018/1/31 Phase 4 Clinical
Linagliptin Profil Institut fur Stoffwechselforschung GmbH Renal failure 2013/5/31 2014/5/31 Phase 4 Clinical
Linagliptin Profil Institut fur Stoffwechselforschung GmbH Non-insulin dependent diabetes 2013/5/31 2014/5/31 Phase 4 Clinical
Linagliptin Boehringer Ingelheim Pharmaceuticals Inc Non-insulin dependent diabetes 2012/5/31 2013/9/30 Phase 4 Clinical
Linagliptin Eli Lilly & Co Non-insulin dependent diabetes 2013/2/28 2014/6/30 Phase 4 Clinical
Linagliptin - Launched
7

Safety Data of Linagliptin

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
Alfa Chemistry USA
BOC Sciences 2g/USD198(In stock)
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD60();10mg/USD84() USA
Cangzhou Senary Chemical S & T Co., Ltd. China
Changzhou Hi-tech Chemicals Ltd. China
Chengdu Miracle Chemicals Co., Ltd. China
Chengdu Yuyang High-tech Developing Co., Ltd. China
Lanzhou Boc Chemical Co., Ltd. China
MedChemexpress Co., Ltd. 5mg/USD60();10mg/USD84() USA
NOVASYNCS Co., Ltd. China
Selleck Chemicals LLC 5mg/USD170(In stock);10mg/USD270(In stock);10mM/1mLIn DMSO/USD320(In stock);100mg/USD1870(In stock);200mg/USD2770(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD60();10mg/USD84() China
Shanghai Pansopharm Technology Co., Ltd. China
Target Molecule Corp. 2mg/USD20();5mg/USD40();10mg/USD67();50mg/USD168();100mg/USD228() USA
10

Related Products

Other Forms of 668270-12-0

Name CAS No Formula MW
1H-Purine-2,6-dione, 8-[(3S)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]- 668270-11-9 C25H28N8O2 472.54

Recommended Compounds in Dipeptidyl Peptidase

Name CAS No Formula MW
Saxagliptin (hydrate) 945667-22-1 C18H27N3O3 333.43
Talabostat (mesylate) 150080-09-4 C10H23BN2O6S 310.18
Omarigliptin 1226781-44-7 C17H20F2N4O3S 398.43
Sitagliptin (phosphate) 654671-78-0 C16H18F6N5O5P 505.31
Sitagliptin 486460-32-6 C16H15F6N5O 407.31
Teneligliptin (hydrobromide) 906093-29-6 C44H65Br5N12O2S2 1257.72
Trelagliptin (succinate) 1029877-94-8 C22H26FN5O6 475.47
Trelagliptin 865759-25-7 C18H20FN5O2 357.38
Anagliptin 739366-20-2 C19H25N7O2 383.45
Teneligliptin 760937-92-6 C22H30N6OS 426.58
Vildagliptin 274901-16-5 C17H25N3O2 303.4
Talabostat 149682-77-9 C9H19BN2O3 214.07
Gosogliptin 869490-23-3 C17H24F2N6O 366.41
Dutogliptin 852329-66-9 C10H20BN3O3 241.1
Alogliptin 850649-61-5 C18H21N5O2 339.39
Alogliptin (Benzoate) 850649-62-6 C25H27N5O4 461.51
Saxagliptin 361442-04-8 C18H25N3O2 315.41
Sitagliptin (phosphate monohydrate) 654671-77-9 C16H20F6N5O6P 523.3241
DBPR108 1186426-66-3 C16H25FN4O2 324.39
UAMC00039 (dihydrochloride) 697797-51-6 C16H26Cl3N3O 382.75614

Recommended Compounds in Same Indication

Name CAS No Formula MW
Glibenclamide 10238-21-8 C23H28ClN3O5S 494.0
Mitiglinide (Calcium) 145525-41-3 C38H50CaN2O7 686.89
Teneligliptin 760937-92-6 C22H30N6OS 426.58
Empagliflozin 864070-44-0 C23H27ClO7 450.91
MK 0893 870823-12-4 C32H27Cl2N3O4 588.48
Canagliflozin 842133-18-0 C24H25FO5S 444.52
Manidipine (dihydrochloride) 89226-75-5 C35H40Cl2N4O6 683.62
Teneligliptin (hydrobromide) 906093-29-6 C44H65Br5N12O2S2 1257.72
Exendin-4 (Acetate) 914454-01-6 C186H286N50O62S 4246.62
Trelagliptin 865759-25-7 C18H20FN5O2 357.38
Bardoxolone (methyl) 218600-53-4 C32H43NO4 505.69
Saxagliptin 361442-04-8 C18H25N3O2 315.41
Alogliptin 850649-61-5 C18H21N5O2 339.39
Alogliptin (Benzoate) 850649-62-6 C25H27N5O4 461.51
Aleglitazar (racemate) 475479-24-4 C24H23NO5S 437.5081
Imeglimin (hydrochloride) 775351-61-6 C6H14ClN5 191.66
Imeglimin 775351-65-0 C6H13N5 155.2
Balaglitazone 199113-98-9 C20H17N3O4S 395.43
Vildagliptin 274901-16-5 C17H25N3O2 303.4
Taranabant 701977-09-5 C27H25ClF3N3O2 515.95
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Route of Synthesis

12

References

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More Information

Linagliptin

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