货号	规格	价格	上海	北京	珠海	重庆	武汉
S87697-5mg买3赠1	99.74%	￥500.00 S87697-5mg ￥500.00 现货（买3赠1）	3 3	-	-	-	-
S87697-10mg买3赠1	99.74%	￥800.00 S87697-10mg ￥800.00 现货（买3赠1）	4 4	-	-	-	-
S87697-25mg买3赠1	99.74%	￥1400.00 S87697-25mg ￥1400.00 现货（买3赠1）	5 5	-	-	-	-
S87697-50mg买3赠1	≥98%	￥2300.00 S87697-50mg ￥2300.00 现货（买3赠1）	2 2	-	-	-	-
S87697-100mg买3赠1	≥98%	￥4000.00 S87697-100mg ￥4000.00 现货（买3赠1）	1 1	-	-	-	-

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产品描述：

AZD7986 is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).

靶点：

Proteasome

体内研究：

AZD7986 shows good stability in plasma, with a half-life of >10 h. AZD7986 inhibits activation of Pr3 and NE, but not CatG, in bone marrow cell lysates in a dose-dependent manner in vivo.

细胞实验：

Cellular potency is studied using the DPP1-expressing monocytic U937 cell line. Briefly, cells grown in RPMI are plated on 384-well polypropylene v-bottom plates at a density of 5×10^5 cells/mL per well. Added to this is 10 μL of AZD7986 at 37°C for 60 min, followed by 350 μM Gly-Phe-AFC. The well fluorescence is read using a multilabel plate reader. Data are analyzed to calculate pIC50 values.

动物实验：

Rats are used for the in vivo study. Naive rats are dosed orally twice daily with AZD7986 at 0.2, 2, and 20 mg/kg/day for 8 days. At termination, bone marrow is taken by femural aspiration for neutrophil serine proteases activity analysis using commercial synthetic peptide substrates.

参考文献：

1. Doyle K, et al. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). J Med Chem. 2016 Oct 27;59(20):9457-9472.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.378 ml	11.892 ml	23.783 ml
5 mM	0.476 ml	2.378 ml	4.757 ml
10 mM	0.238 ml	1.189 ml	2.378 ml
50 mM	0.048 ml	0.238 ml	0.476 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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