Trelagliptin (SYR-472) is a potent, orally active and highly selectiveDPP-4inhibitor with anIC₅₀of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM)^[1].

IC50: 4 nM (DPP-4)^[1]

Dipeptidyl peptidase-4 (DPP-4) is one of the widely explored novel targets for type 2 diabetes mellitus (T2DM) strategy to preserve the endogenous glucagon like peptide (GLP)-1 activity by inhibiting the DPP-4 action^[1].
Trelagliptin exhibits potent inhibitory activity toward DPP-4 prepared from Caco-2 cells with an IC₅₀ value of 5.4 nM. Trelagliptin also inhibits human, dog, and rat plasma DPP-4 activity with IC₅₀ values of 4.2 nM, 6.2 nM, and 9.7 nM, respectively^[2].
Trelagliptin is highly selective for DPP-4 and displays IC₅₀ values >100,000 nM corresponding to >10,000-fold selectivity over DPP-2, DPP-8, DPP-9, PEP and FAPα activities. Trelagliptin shows DPP4 selective about 4- and 12-fold more potent than alogliptin (HY-A0023) and sitagliptin (HY-13749), respectively^[2].

Trelagliptin (oral gavage; 7 mg/kg; single dose) shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h^[1].
Trelagliptin (oral gavage; 3 mg/kg; single dose; 60 min prior to oral glucose) significantly improves the glucose tolerance capacity by decreasing the AUC_0–120minof 19.3% compared with the vehicle group in ob/ob mice^[3].
Trelagliptin (oral gavage; 10 mg/kg; once a week; 8 weeks) caused significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 16.8% compared to the control.It also increases insulin level and raised it by 1.7-fold in AUC_0–120minin ob/ob mice^[3].

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Solid

C₁₈H₂₀FN₅O₂

865759-25-7

曲格列汀

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL(139.91 mM)

*"≥" means soluble, but saturation unknown.

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请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
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• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.00 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.00 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。