计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Sitagliptin(MK 0431)是DPP4高效抑制剂，在Caco-2细胞中IC50值为19nM。A potent, active inhibitor of DPP-IV
Information
Sitagliptin phosphate monohydrate Sitagliptin phosphate monohydrate (MK-0431) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.
In vitro
As an orally active agent, Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts. MK0431 reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. A recent study demonstrates that sitagliptin 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 therefore 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.
Cell Data
cell lines：Namru murine mammary gland (NMuMG), MDA-MB-231, renal cell carcinoma (RCC)4, and U2OS cells
Concentrations：100 μM
Incubation Time：1 hour
Powder Purity:≥99%
规格
英文别名
MK-0431 | (R)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one phosphate monohydrate
规格或纯度
10mM in DMSO
英文名称
Sitagliptin phosphate monohydrate
生化机理
磷酸西他列汀一水合物（MK-0431）是一种强效的 DPP-IV 抑制剂，在 Caco-2 细胞提取物中的 IC50 为 19 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
二肽基肽酶 IV 抑制剂
名称和识别符
EC号
682-492-2
分子类型
小分子
Isomeric SMILES
C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)C[C@@H](CC3=CC(=C(C=C3F)F)F)N.O.OP(=O)(O)O
PubChem CID
分子量
523.32
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 100 mg/mL (123.38 mM); Ethanol: 100 mg/mL (123.38 mM); Water: Insoluble;
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H319: 引起严重眼睛刺激
预防措施声明
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2201175 |
分析证书 | S408605 |
溶液计算器
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