021-51111890
购物车（0）
sales@molnova.cn
Sitagliptin phosphate monohydrate
CAS No. 654671-77-9
Sitagliptin phosphate monohydrate ( —— )
产品货号. M15489 CAS No. 654671-77-9
Sitagliptin 磷酸盐一水合物是一种有效的 DPP4 抑制剂，在 Caco-2 细胞提取物中 IC50 为 19 nM
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 100MG | ￥405 | 有现货 |
|
| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
-
产品名称Sitagliptin phosphate monohydrate
-
注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
-
产品简述Sitagliptin 磷酸盐一水合物是一种有效的 DPP4 抑制剂，在 Caco-2 细胞提取物中 IC50 为 19 nM
-
产品描述Sitagliptin phosphate monohydrate is a potent inhibitor of?DPP4?with?IC50?of 19 nM in Caco-2 cell extracts.
-
体外实验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.?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.
-
体内实验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.
-
同义词——
-
通路Autophagy
-
靶点Other Targets
-
受体IC50: 19 nM (DPP4, in Caco-2 cell extracts)
-
研究领域Metabolic Disease
-
适应症——
化学信息
-
CAS Number654671-77-9
-
分子量523.32
-
分子式C??H??F?N?O?P
-
纯度>98% (HPLC)
-
溶解度H2O: ≥ 33 mg/mL
-
SMILES[H]O[H].O=C(N1CC2=NN=C(C(F)(F)F)N2CC1)C[C@H](N)CC3=CC(F)=C(F)C=C3F.O=P(O)(O)O
-
化学全称——
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
参考文献
1. Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of acti
2. Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51.
3. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73.
4. Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9.
5. Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32.
产品手册
关联产品
-
Rhein
大黄酸是一种广泛存在于草药中的亲脂性蒽醌，具有多种药理作用，包括胃肠保护、肾保护、抗炎、抗氧化、抗癌和抗菌活性。
-
Sitagliptin phosphat...
Sitagliptin 磷酸盐一水合物是一种有效的 DPP4 抑制剂，在 Caco-2 细胞提取物中 IC50 为 19 nM
