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- 保存条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
- 英文名:
(Rac)-MK-0431
- 库存:
货期:询盘
- 供应商:
MedChemExpress LLC
- CAS号:
823817-56-7
- 规格:
5 mg/10 mg/25 mg/50 mg/100 mg
| 规格: | 5 mg | 产品价格: | ¥540.0 |
|---|---|---|---|
| 规格: | 10 mg | 产品价格: | ¥855.0 |
| 规格: | 25 mg | 产品价格: | ¥1575.0 |
| 规格: | 50 mg | 产品价格: | ¥2520.0 |
| 规格: | 100 mg | 产品价格: | ¥4050.0 |
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(Rac)-Sitagliptin
CAS No. : 823817-56-7
MCE 国际站:(Rac)-Sitagliptin
产品活性:(Rac)-Sitagliptin 是 Sitagliptin (HY-13749) 的一种异构体。Sitagliptin (MK-0431) 是一种有效的,具有口服活性的 DPP4 抑制剂,在 Caco-2 细胞中,IC50 值为 19 nM。
研究领域:Autophagy | Metabolic Enzyme/Protease
作用靶点:Autophagy | Dipeptidyl Peptidase
In Vitro: Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. Stagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It reduces the effect of autoimmunity on graft survival.
In Vivo: In vivo, the ED50 value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats. The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival. The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs.
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文献和实验Rac and Rap GTPase Activation Assays
of Rac/Cdc42 and Rap activity in stimulated neutrophils.
因为自己实验后期需要使用这方面的技术,所以最近在查阅这方面的资料,想拿出来和大家一起分享.后期会把更详细的东西贴出来.英文水平一般,所以翻译的有点差,请海涵. Rac1 Activation Assay Kit被设计来鉴定贴壁细胞或非贴壁细胞的细胞裂解液中Rac活性数量(i.e. Rac-GTP, rather than the inactive Rac-GDP). 使用的glutathione (GST) pull-down方法,采用GST-agarose beads与有的包含74
Ubiquitination of Rac1 by Inhibitors of Apoptosis (IAPs)
that inhibitors of apoptosis (IAPs) function as direct E3 ubiquitin ligases for Rho GTPase Rac1 and target it for proteasomal degradation. Here, we describe in vitro and in vivo ubiquitination assays for detecting the conjugation
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