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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
Alogliptin
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
850649-61-5
- 规格:
100mg/50mg/10mg/5mg
| 规格: | 100mg | 产品价格: | ¥2900.0 |
|---|---|---|---|
| 规格: | 50mg | 产品价格: | ¥2040.0 |
| 规格: | 10mg | 产品价格: | ¥1250.0 |
| 规格: | 5mg | 产品价格: | ¥800.0 |
是高活性DPP4选择性抑制剂。
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide-1 attenuates cardiac hypertrophy via the AngII/AT1R/ACE2 and AMPK/mTOR/p70S6K pathways
成员:Wang Jing, Fan Shaohua, Xiong Qianfeng, Niu Yu, Zhang Xin, Qin Junnan, Shi Yawei, Zhang Lihui
论文因子:3.848 发表期刊:ACTA BIOCHIMICA ET BIOPHYSICA SINICA pmid:34357376
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide 1 reverses myocardial hypertrophy through cAMP/PKA/RhoA/ROCK2 signaling
成员:Fan S, Xiong Q, Zhang X, Zhang L, Shi Y.
论文因子:3.7 发表期刊:Acta Biochim Biophys Sin pmid:32386193
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide-1 attenuates cardiac hypertrophy via the AngII/AT1R/ACE2 and AMPK/mTOR/p70S6K pathways
成员:Wang J; Fan S; Xiong Q; Niu Y; Zhang X; Qin J; Shi Y; Zhang L
论文因子:3.7 发表期刊:Acta Biochimica et Biophysica Sinica pmid:34357376
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide 1 reverses myocardial hypertrophy through cAMP/PKA/RhoA/ROCK2 signaling
成员:Fan S; Xiong Q; Zhang X; Zhang L; Shi Y.
论文因子:3.7 发表期刊:Acta Biochim Biophys Sin pmid:32386193
| 基本信息 | |
| CAS | No.850649-61-5 |
| 中文名称 | 阿洛利停 |
| 英文名称 | Alogliptin |
| 别名 | SYR 322 |
| 分子式 | C18H21N5O2 |
| 分子量 | 339.39 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| EC | EINECS 821-899-3 |
| MDL | MFCD09833196 |
| SMILES | O=C(C=C(N1C[C@H](N)CCC1)N(C2=O)CC3=C(C#N)C=CC=C3)N2C |
| 靶点 | Dipeptidyl Peptidase(DPP-4) |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | 是高活性DPP4选择性抑制剂。 |
| 生物活性 | Alogliptin (SYR-322) is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.[1-4] |
| In Vitro | Alogliptin is a potent(IC50 < 10 nM)inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9[1].Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM[2]. |
| 细胞实验 | Absolute oral bioavailability of alogliptin in rats,dogs,and monkeys is 45%,86%,and 72% to 88%,respectively. After a single oral dose of alogliptin,plasma DPP-4 inhibition is observed within 15 min and maximum inhibition is > 90% in rats,dogs,and monkeys; inhibition is sustained for 12 h in rats(43%)and dogs(65%)and 24 h in monkeys(> 80%). From Emax modeling,50% inhibition of DPP-4 activity is observed at a mean alogliptin plasma concentration(EC50)of 3.4 to 5.6 ng/ml(10.0 to 16.5 nM)in rats,dogs,and monkeys. In Zucker fa/fa rats,a single dose of alogliptin(0.3,1,3,and 10 mg/kg)inhibites plasma DPP-4(91% to 100% at 2 h and 20% to 66% at 24 h),increases plasma GLP-1(2- to 3-fold increase in AUC0–20 min)and increases early-phase insulin secretion(1.5- to 2.6-fold increase in AUC0-20 min)and reduces blood glucose excursion(31%–67% decrease in AUC0–90 min)after oral glucose challenge. Alogliptin(30 and 100 mg/kg)has no effect on fasting plasma glucose in normoglycemic rats.[3]. |
| 数据来源文献 | [1] Huan Y, et al.J Pharmacol Toxicol Methods. 2015;71:8-12. [2] Feng J, et al.J Med Chem. 2007,17;50(10):2297-300. [3] Lee B, et al.Eur J Pharmacol. 2008,28;589(1-3):306-14. |
| 单位 | 瓶 |
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文献和实验【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide-1 attenuates cardiac hypertrophy via the AngII/AT1R/ACE2 and AMPK/mTOR/p70S6K pathways
成员:Wang Jing, Fan Shaohua, Xiong Qianfeng, Niu Yu, Zhang Xin, Qin Junnan, Shi Yawei, Zhang Lihui
论文因子:3.848 发表期刊:ACTA BIOCHIMICA ET BIOPHYSICA SINICA pmid:34357376
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide 1 reverses myocardial hypertrophy through cAMP/PKA/RhoA/ROCK2 signaling
成员:Fan S, Xiong Q, Zhang X, Zhang L, Shi Y.
论文因子:3.7 发表期刊:Acta Biochim Biophys Sin pmid:32386193
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide-1 attenuates cardiac hypertrophy via the AngII/AT1R/ACE2 and AMPK/mTOR/p70S6K pathways
成员:Wang J; Fan S; Xiong Q; Niu Y; Zhang X; Qin J; Shi Y; Zhang L
论文因子:3.7 发表期刊:Acta Biochimica et Biophysica Sinica pmid:34357376
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Glucagon-like peptide 1 reverses myocardial hypertrophy through cAMP/PKA/RhoA/ROCK2 signaling
成员:Fan S; Xiong Q; Zhang X; Zhang L; Shi Y.
论文因子:3.7 发表期刊:Acta Biochim Biophys Sin pmid:32386193
磷酰胺(DEPC) (Sigma) 、30% 甘油及蛋白酶抑制剂 [ 含有 1 μg/ml 抑肽酶(aprotinin) 、1 μg/ml 胃蛋白酶抑制剂(pepstatin) 、1 μg/ml 亮抑酶肽(leupeptin) 、0.1 mmol/L PMSF ] ,所有药品都来自于 Sigma ( 见注释 1 和注释 2) 。注意:媒介中的两种成分—— DEPC 和 β-巯基乙醇是有毒的,需要在通风橱中进行准备,并需要戴化学防护手套。 2.2 细胞核的提纯 ( 1 ) 样品
to barley yellow dwarf virus. Y i C h u a n 29, 97-102. 36. Y a n , F . , Z h en g , Y. Y. , Z h a n g s W. W . , X ia o , H . , L i, S. F . a n d C h en g s Z . M . (2006) O b ta in ed transgeic w h ea t exp ressin
。它包括APC摄取抗原加工成多肽分子,MHCⅠ或MHCⅡ灯分子将抗原信息分别呈递给CD8或CD4细胞,激活特异性T细胞反应等一系列过程。该过程又分为MHCⅠ和MHCⅡ类分子限制性抗原呈递两条途径[4]。 1.MHCⅠ类分子限制性抗原呈递:MHCⅠ类分子限制的抗原加工和呈递是与胞生物合成MHCⅠ分子的转运相关联的。多数有核细胞都转录并表达MHCⅠ类基因,并预定方式将MHCⅠ类分子的重链和轻链(β2微球蛋白)转运入内质网腔。内源性和外源性蛋白经细胞质中蛋白酶降解形成的短多肽,被位于内质
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