Linagliptin - CAS 668270-12-0
Catalog number: B0084-461855
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C25H28N8O2
Molecular Weight:
472.553
COA:
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Targets:
DPP4
Description:
A novel potent and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with potential use in the treatment of type 2 diabetes.
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Catalog Number Size Price Stock Quantity
B0084-461855 2.5 g $198 In stock
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Brife Description:
DPP-4 inhibitor, type 2 diabetes
Purity:
0.99
Synonyms:
Tradjenta; BI-1356; Ondero; Trajenta
MSDS:
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Application:
the treatment of type 2 diabetes
InChIKey:
LTXREWYXXSTFRX-QGZVFWFLSA-N
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
Canonical SMILES:
CC4=NC5=CC=CC=C5C(=N4)C)C
1.Empagliflozin/Linagliptin: Combination therapy in patients with type 2 diabetes.
Tan X1, Hu J2. Ann Endocrinol (Paris). 2016 Apr 6. pii: S0003-4266(15)01131-2. doi: 10.1016/j.ando.2015.11.003. [Epub ahead of print]
Glyxambi® (empagliflozin/linagliptin) is a fixed-dose, once-daily tablet combining a sodium glucose co-transporter-2 (SGLT2) inhibitor with a dipeptidyl peptidase-4 (DPP-4) inhibitor. Glyxambi® is served as an adjuvant to diet and exercise to improve glycemic control in adults with type 2 diabetes when both empagliflozin and linagliptin are appropriate treatments. Glyxambi® combines 10mg or 25mg empagliflozin with 5mg linagliptin, with different, complementary mechanisms of action to improve glycemic control in patients with type 2 diabetes. Empagliflozin removes glucose through the urine by blocking blood glucose re-absorption in the kidney, and linagliptin exerts glucose-lowering activity by increasing hormones that stimulate the pancreas to produce more insulin and decreasing the levels of glucagon in the circulation. In addition, this combination therapy modestly reduces body weight and blood pressure without significant safety issues.
2.The dipeptidyl peptidase inhibitor linagliptin and the angiotensin II receptor blocker telmisartan show renal benefit by different pathways in rats with 5/6 nephrectomy.
Tsuprykov O1, Ando R2, Reichetzeder C1, von Websky K1, Antonenko V1, Sharkovska Y3, Chaykovska L4, Rahnenführer J1, Hasan AA5, Tammen H6, Alter M7, Klein T8, Ueda S9, Yamagishi S10, Okuda S2, Hocher B11. Kidney Int. 2016 May;89(5):1049-61. doi: 10.1016/j.kint.2016.01.016. Epub 2016 Mar 24.
Dipeptidyl peptidase (DPP)-4 inhibitors delay chronic kidney disease (CKD) progression in experimental diabetic nephropathy in a glucose-independent manner. Here we compared the effects of the DPP-4 inhibitor linagliptin versus telmisartan in preventing CKD progression in non-diabetic rats with 5/6 nephrectomy. Animals were allocated to 1 of 4 groups: sham operated plus placebo; 5/6 nephrectomy plus placebo; 5/6 nephrectomy plus linagliptin; and 5/6 nephrectomy plus telmisartan. Interstitial fibrosis was significantly decreased by 48% with linagliptin but a non-significant 24% with telmisartan versus placebo. The urine albumin-to-creatinine ratio was significantly decreased by 66% with linagliptin and 92% with telmisartan versus placebo. Blood pressure was significantly lowered by telmisartan, but it was not affected by linagliptin. As shown by mass spectrometry, the number of altered peptide signals for linagliptin in plasma was 552 and 320 in the kidney.
3.Hypoglycemia Incidence Rates and Associated Health Care Costs in Patients with Type 2 Diabetes Mellitus Treated with Second-Line Linagliptin or Sulfonylurea After Metformin Monotherapy.
Raju A1, Shetty S2, Cai B2, D'Souza AO1. J Manag Care Spec Pharm. 2016 May;22(5):483-92. doi: 10.18553/jmcp.2016.22.5.483.
BACKGROUND: Hypoglycemia poses a significant clinical and economic burden to patients with type 2 diabetes mellitus (T2DM). Minimizing the risk of hypoglycemia is an important component when managing patients with T2DM. Understanding hypoglycemia rates and the associated economic consequences can help to inform health care decision makers.
4.Acute Kidney Injury Associated with Linagliptin.
Nandikanti DK1, Gosmanova EO2, Gosmanov AR3. Case Rep Endocrinol. 2016;2016:5695641. doi: 10.1155/2016/5695641. Epub 2016 Feb 14.
Linagliptin is a dipeptidyl peptidase-IV (DPP-IV) inhibitor that is approved for the treatment of type 2 diabetes mellitus. About 5% of linagliptin is eliminated by the kidneys and no dose adjustment is recommended in kidney impairment. We report a first case of linagliptin-associated acute kidney injury (AKI) in a patient with preexisting chronic kidney disease (CKD). We hypothesize that AKI was due to renal hypoperfusion from linagliptin-induced natriuresis and intravascular volume contraction in the setting of concomitant lisinopril use, which is known to impair autoregulation and potentiate hypotension-induced AKI. It may be prudent to exert caution and closely monitor kidney function when initiating linagliptin in combination with ACE-inhibitors in CKD patients.
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CAS 668270-12-0 Linagliptin

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