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(±)-Sitagliptin-d4 (hydrochloride)

Katalog-Nr.GC46308

A neuropeptide with diverse biological activities

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(±)-Sitagliptin-d4 (hydrochloride) Chemische Struktur

Cas No.: 2749855-96-5

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500 μg
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1 mg
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Sample solution is provided at 25 µL, 10mM.

Description of (±)-Sitagliptin-d4 (hydrochloride)

(±)-Sitagliptin-d4 is intended for use as an internal standard for the quantification of sitagliptin by GC- or LC-MS. Sitagliptin is a mixture of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin and (+)-sitagliptin, also known as sitagliptin impurity E, a potential impurity found in commercial preparations of (-)-sitagliptin.1 (-)-Sitagliptin is a potent inhibitor of DPP-4 (IC50 = 18 nM).2 It is selective for DPP-4 over DPP-8 (IC50 = 48 µM) as well as several other peptidases, including DPP-9, DPP-2, and amino peptidase P.2,3 (-)-Sitagliptin improves glucose tolerance in insulin-resistant Zucker fatty and high-fat diet fed rats as well as ob/ob and high-fat diet fed mice.4 It also reduces hyperglycemia in mice fed a high-fat diet with diabetes induced by streptozotocin . Formulations containing (-)-sitagliptin have been used in the treatment of type 2 diabetes mellitus.

1.Kothari, H.M., Dave, M.G., Pandey, B., et al.Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-α]pyrazin-7(8H)-yl]-L-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof(2013) 2.Biftu, T., Feng, D., Qian, X., et al.(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetesBioorg. Med. Chem. Lett.17(1)49-52(2007) 3.Kim, D., Kowalchick, J.E., Edmondson, S.D., et al.Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIAT (sitagliptin phosphate)Bioorg. Med. Chem. Lett.17(12)3373-3377(2007) 4.AhrÉn, B.DPP-4 inhibitorsBest Pract.Res.Clin.Endocrinol.Metab.21(4)517-533(2007)

Chemical Properties of (±)-Sitagliptin-d4 (hydrochloride)

Cas No. 2749855-96-5 SDF
Canonical SMILES FC1=CC(CC(N)CC(N2CC3=NN=C(C(F)(F)F)N3C([2H])([2H])C2([2H])[2H])=O)=C(F)C=C1F.Cl
Formula C16H11D4F6N5O.HCl M.Wt 447.8
Löslichkeit Water: Soluble Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (±)-Sitagliptin-d4 (hydrochloride)

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1 mg 5 mg 10 mg
1 mM 2.2331 mL 11.1657 mL 22.3314 mL
5 mM 0.4466 mL 2.2331 mL 4.4663 mL
10 mM 0.2233 mL 1.1166 mL 2.2331 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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