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NVP DPP 728 dihydrochloride Sale

目录号 : GC14126

NVP DPP 728 dihydrochloride 是一种有效的、可逆的和腈依赖性二肽基肽酶 IV (DPP-IV) 抑制剂。

NVP DPP 728 dihydrochloride Chemical Structure

Cas No.:247016-69-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,124.00
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10mg
¥1,418.00
现货
50mg
¥6,447.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

NVP DPP 728 dihydrochloride
Description:
Ki: Inhibit human DPP-IV amidolytic activity with a Ki of 11 nM [1]
Inhibitors of dipeptidyl peptidase 4, also known as DPP-4 inhibitors or gliptins, are a class of oral hypoglycemics that can be used to treat diabetes mellitus type 2. NVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV.
In vitro: NVP-DPP728 was found to inhibit human DPP-IV amidolytic activity with a Ki of 11 nM, a kon value of 1.3 x 105 M-1 s-1, and a koff of 1.3 x 10-3 s-1. NVP-DPP728 inhibited DPP-IV in a manner consistent with a two-step inhibition mechanism. Taken together, these data suggest that NVP-DPP728 inhibits DPP-IV through formation of a novel, reversible, nitrile-dependent complex with transition state characteristics [1].
In vivo: Aging caused a decrease in early insulin response after an oral glucose challenge in aged Wistar or DPP-IV(+) F344 rats, but not in aged DPP-IV(-) F344 rats, compared with young control groups. Glucose tolerance after an oral glucose challenge in aged DPP-IV(-) F344 rats was better than in aged DPP-IV(+) F344 and Wistar rats associated with the preservation of the early insulin response. NVP-DPP728 improved the glucose tolerance after an oral glucose challenge by potentiating the early insulin response throughout the inhibition of plasma DPP-IV activity in aged DPP-IV(+) Wistar andF34 4 rats. In contrast, NVP-DPP728 did not affect the glucose tolerance after an oral glucose challenge in aged DPP-IV(-) F344 rats. These results indicate that treatment with NVP-DPP728 ameliorated glucose tolerance in aged rats by the direct inhibition of plasma DPP-IV activity and presumably the subsequent increase in endogenous incretin action [2].
Clinical trial: NVP-DPP728 is currently in the preclinical development and no clinical trial is ongoing.
Reference:
[1] Hughes TE, Mone MD, Russell ME, Weldon SC, Villhauer EB. NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)-pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV. Biochemistry. 1999;38(36):11597-603.
[2] Mitani H, Takimoto M, Kimura M. Dipeptidyl peptidase IV inhibitor NVP-DPP728 ameliorates early insulin response and glucose tolerance in aged rats but not in aged Fischer 344 rats lacking its enzyme activity. Jpn J Pharmacol. 2002;88(4):451-8.

Chemical Properties

Cas No. 247016-69-9 SDF
化学名 6-[2-[[2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl]amino]ethylamino]pyridine-3-carbonitrile;dihydrochloride
Canonical SMILES C1CC(N(C1)C(=O)CNCCNC2=NC=C(C=C2)C#N)C#N.Cl.Cl
分子式 C15H18N6O.2HCl 分子量 371.27
溶解度 ≥ 17.75mg/mL in DMSO with gentle warming, ≥ 81 mg/mL in EtOH, ≥ 82 mg/mL in Water 储存条件 Desiccate at RT
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6935 mL 13.4673 mL 26.9346 mL
5 mM 0.5387 mL 2.6935 mL 5.3869 mL
10 mM 0.2693 mL 1.3467 mL 2.6935 mL
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