1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Gosogliptin

Gosogliptin (Synonyms: PF-00734200; PF-734200)

目录号: HY-10287 纯度: 98.71%
产品使用指南

Gosogliptin 是一种有效的选择性二肽基肽酶IV (DPP-IV) 抑制剂。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Gosogliptin Chemical Structure

Gosogliptin Chemical Structure

CAS No. : 869490-23-3

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
1 mg ¥3000
In-stock
5 mg ¥6000
询价
10 mg ¥10200
询价
20 mg ¥18000
询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).

IC50 & Target

DPP-IV[1][2]

体外研究
(In Vitro)

Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates greater than 200-fold selectivity over other members of the DPP family (DPP-2, DPP-3, DPP-8, and DPP-9) and the related serine proteases, fibroblast activation protein, aminopeptidase P, and propyl oligopeptidase, enzymes that possess similar catalytic activities. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity when administered orally to rats, dogs, and monkeys. In various nonclinical models, Gosogliptin stimulates insulin secretion and improves glucose tolerance[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

The objectives of the present study are to characterize the metabolism, pharmacokinetics, and excretion of [14C] Gosogliptin in Sprague-Dawley (SD) rats, beagle dogs, and humans. A single dose of [14C] Gosogliptin is administered orally to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg). After a single oral dose of [14C] Gosogliptin to SD rats, an overall mean of 97.1% of the administered radioactivity is recovered in the urine, feces, and cage wash over a period of 168 h postdose. The mean cumulative dose recovered in feces is 66.0%. The mean cumulative excretion in the urine is 30.8%. Approximately 95% of the excreted radioactivity recovery occurred in the first 48 h. Mean total recoveries of dosed radioactivity from bile duct-cannulated rats are 29.5% in urine and 62.0% in bile. No gender-related differences are observed in the excretion pattern of radioactivity[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

366.41

Formula

C17H24F2N6O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
Kinase Assay
[2]

Studies to identify the P450 isoform(s) responsible for formation of M5 are conducted using chemical inhibition and incubation in recombinant P450 isozymes. Inhibition studies are performed with each of the following inhibitors: Furafylline (10 μM for CYP1A2), Sulfaphenazole (10 μM for CYP2C9), Quinidine (10 μM for CYP2D6), (+)N-3-benzylnirvanol (10 μM for CYP2C19), and Ketoconazole (1 μM for CYP3A4). Incubations (1 ml) are performed in duplicate with NADPH (1.3 mM) in 1.5 mL plastic Eppendorf tubes open to air at 37°C in a shaking water bath. Samples are preincubated at 37°C for 5 min before the addition of NADPH. Each incubation contains microsomes (2 mg/mL protein), 100 mM potassium phosphate buffer (pH 7.4), 10 mM MgCl2, 10 μM Gosogliptin (PF-00734200), and one of the above inhibitors. A control sample is also prepared without inhibitor. Additional controls using marker substrates (each at 10 μM), in the presence and absence of P450-specific inhibitors, are used to confirm inhibition results and included Phenacetin (CYP1A2), Tolbutamide (CYP2C9), (S)-Mephenytoin (CYP2C19), Dextromethorphan (CYP2D6), and Testosterone (CYP3A4). At 0 and 30 min, incubations are quenched with an equal volume of ice-cold acetonitrile. Samples are then placed on ice for 15 min to allow precipitation of protein and subsequently centrifuged at 1800g for 5 min. An aliquot is removed from each sample and injected onto the HPLC/MS system[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Rats[2]
A group of SD rats (n=3/gender) is administered a single 5 mg/kg oral dose of [14C] Gosogliptin for the mass balance study. For biliary excretion experiments, another group of two male and two female bile duct-cannulated rats is administered a single 5 mg/kg oral dose of [14C] Gosogliptin in similar fashion. The dose is formulated as a suspension in 0.5% methyl cellulose on the day before dose administration. Each rat received an approximate dose of ∼60 μCi of radiolabeled material. Urine and feces are collected from intact animals for 7 days at 0 to 8, 8 to 24, 24 to 48, 48 to 72, 72 to 96, 96 to 120, 120 to 144, and 144- to 168-h intervals after the dose. The first feces sample is collected at 0 to 24 h after the dose. Bile and urine samples are collected from bile duct-cannulated animals at 0- to 8-, 8- to 24-, and 24- to 48-h intervals after the dose. The volumes of urine and bile samples are recorded, and all of the biological samples are stored at -20°C until analysis. For determination of pharmacokinetic parameters and identification of circulating metabolites, a third group of jugular vein-cannulated rats (n=10/gender) is given an oral dose of 5 mg/kg [14C] Gosogliptin. Blood from two animals per gender is collected at 0.5, 1, 2, 4, and 8 h postdose in heparinized (lithium heparin anticoagulant) tubes. The blood samples are centrifuged at 1000g for 10 min to obtain the plasma. Plasma is transferred to clean tubes and stored at -20°C until analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
Gosogliptin
目录号:
HY-10287
需求量: