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PF-06882961
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-06882961图片
CAS NO:2230198-02-2
包装:5mg, 10mg, 25mg
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品名称
Danuglipron
PF06882961
产品介绍

生物活性

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R) agonist. PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. PF-06882961 shows mild to moderate damage to the heart, moderate to severe effects on the thymus gland (which helps with managing infection), mild to moderate stomach ulcers at the highest dose level given in the rat.


化学数据

分子量555.6
分子式C31H30FN5O4
CAS号2230198-02-2
纯度>99%
溶解性(25°C)DMSO 100 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系HEK293 cells
方法HEK293 cells stably expressing hGLP-1R fused to green fluorescent protein (GFP) (400,000 cells per well) are cultured onto 6 well plates for 24 hours and stimulated with PF-06882961 for 30 minutes. An agonist concentration of 1 μM shown to induce maximal internalization is chosen for these studies. In selected wells, cells are washed three times with PBS containing 0.1 % BSA and incubated at 37 °C for an additional 2 hours to assess reversibility of the endocytosis process. Cells are then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS containing 0.1% BSA.
浓度1 μM
处理时间30 minutes

动物实验
动物模型cynomolgus monkeys
配制-
剂量1 mg/kg iv; 5 mg/kg, 100 mg/kg PO
给药处理iv, PO

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM1.7999 mL8.9993 mL17.9986 mL
5 mM0.36 mL1.7999 mL3.5997 mL
10 mM0.18 mL0.8999 mL1.7999 mL