西格列汀|T0242

價(jià)格	￥515	￥722	￥996
包裝	50mg	100mg	200mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:西格列汀	英文名稱:Sitagliptin
CAS:486460-32-6	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.4%	產(chǎn)品類別: 抑制劑
貨號(hào): T0242

Product Introduction

Bioactivity

名稱	Sitagliptin
描述	Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein/enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.
細(xì)胞實(shí)驗(yàn)	CD4T-cells are plated on membrane inserts in serum-free RPMI 1640, and cell migration is assayed using Transwell chambers (Corning), in the presence or absence of purified porcine kidney DPP-4 (32.1 units/mg; 100 mU/mL final concentration) and DPP-4 inhibitor (100 μM). After 1 hour, cells on the upper surface are removed mechanically, and cells that have migrated into the lower compartment are counted. The extent of migration is expressed relative to the control sample.
激酶實(shí)驗(yàn)	DPP-4 is extracted from confluent Caco-2 cells. After 5 minutes of incubation at room temperature with lysis buffer (10 mM Tris-HCl, 150 mM NaCl, 0.04 U/mL aprotinin, 0.5% Nonidet P40, pH 8.0), cells are centrifuged at 35,000 g at 4°C for 30 minutes, and the supernatant is stored at -80°C. Assays are performed by mixing 20 μL of appropriate compound dilutions with 50 μL of the substrate for the DPP-4 enzyme, H-Ala-Pro-7-amido-4-trifluoromethylcoumarin (final concentration in the assay, 100 μM) and 30 μL of the Caco-2 cell extract (diluted 1000-fold with 100 mM Tris-HCl, 100 mM NaCl, pH 7.8). Plates are incubated at room temperature for 1 hour, and fluorescence is measured at excitation/emission wavelengths of 405/535 nm using a SpectraMax GeminiXS. Dissociation kinetics of inhibitors from the DPP-4 enzyme is determined after a 1-hour preincubation of Caco-2 cell extracts with high inhibitor concentrations (30 nM for BI 1356, 3 μM for vildagliptin). The enzymatic reaction is started by adding the substrate H-Ala-Pro-7-amido-4-trifluoromethylcoumarin after a 3000-fold dilution of the preincubation mixture with assay buffer. Under these conditions, the difference in DPP-4 activity at a certain time point in the presence or absence of an inhibitor reflects the amount of this inhibitor still bound to the DPP-4 enzyme. Maximal reaction rates (fluorescence units/seconds ×1000) at 10-minute intervals are calculated using the SoftMax software of the SpectraMax and corrected for the rate of an uninhibited reaction [(vcontrol-vinhibitor)/vcontrol].
體外活性	Sitagliptin phosphate 對 DPP-4 具有強(qiáng)效抑制作用，從 Caco-2 細(xì)胞提取物中提取的 IC50 為 19 nM[1]。Sitagliptin phosphate 通過 cAMP/PKA/Rac1 激活途徑減少離體脾臟 CD4 T 細(xì)胞的體外遷移[2]。Sitagliptin phosphate 通過一種不依賴于 DPP-4、蛋白激酶 A 和 MEK-ERK1/2 的途徑發(fā)揮一種新的直接作用，刺激腸 L 細(xì)胞分泌 GLP-1。Sitagliptin phosphate 能降低自身免疫對移植物存活率的影響[3]。
體內(nèi)活性	Sitagliptin phosphate 對自由采食的漢-Wistar 大鼠血漿中 DPP-4 活性的抑制 ED50 值為劑量后 7 小時(shí) 2.3 mg/kg和劑量后 24 小時(shí) 30 mg/kg[1]。鏈脲佐菌素誘導(dǎo)的 1 型糖尿病小鼠模型顯示血漿中的 DPP-4 水平升高，而Sitagliptin phosphate 飲食可大幅抑制這種升高。這可能是通過延長胰島移植存活時(shí)間對高血糖的調(diào)節(jié)產(chǎn)生積極影響而實(shí)現(xiàn)的[4]。Sitagliptin phosphate 在大鼠體內(nèi)的血漿清除率和分布容積（40-48 mL/min/kg，7-9 L/kg）高于狗（9 mL/min/kg，3 L/kg）；在大鼠體內(nèi)的半衰期為 2 小時(shí)，短于狗的 4 小時(shí)[5]。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 16.67 mg/mL (40.92 mM) H2O : ＜1 mg/mL (Insoluble)
關(guān)鍵字	Dipeptidyl Peptidase \| MK-0431 \| inhibit \| Autophagy \| Sitagliptin \| MK 0431 \| Inhibitor \| DPP
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Curcumin \| Stavudine \| Salicylic acid \| Paeonol \| Sodium 4-phenylbutyrate
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌上市藥物庫 \| 已知活性化合物庫 \| EMA 上市藥物庫 \| 高選擇性抑制劑庫 \| FDA 上市藥物庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字：西他列汀|||西格列汀|||MK0431|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號(hào)4樓

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