VU6015929
|
|
|
- CAS号:
- 英文名:
- VU6015929
- 英文别名:
- VU6015929
- 中文名:
- VU6015929
- 中文别名:
- CBNumber:
- CB65833711
- 分子式:
- 分子量:
- 0
- MOL File:
- Mol file
|
|
|
VU6015929性质、用途与生产工艺
VU6015929 是一种选择性的 Discoidin Domain Receptor 1/2 (DDR1/2) 的抑制剂，对DDR1和DDR2的IC50值分别为4.67 nM和7.39 nM。VU6015929 可有效地抑制IV型胶原蛋白的产生。
| Target | Value |
DDR1
(Cell-free assay)
|
4.67 nM
|
DDR2
(Cell-free assay)
|
7.39 nM
|
VU6015929 (Compound 7e; 4-100 nM; 24 hours; HEK293-DDR1b cells) treatment inhibits collagen I-induced DDR1 phosphorylation in a dose dependent manner. Analysis of the phosphorylated DDR1/total DDR1 ratio reveals an
IC
50
for VU6015929 of 0.7078 nM.
Western Blot Analysis
|
Cell Line:
|
HEK293-DDR1b cells
|
|
Concentration:
|
4 nM, 20 nM, 100 nM
|
|
Incubation Time:
|
24 hours
|
|
Result:
|
Inhibited collagen I-induced DDR1 phosphorylation in a dose dependent manner. Significantly inhibited collagen IV production.
|
VU6015929 (Compound 7e) is further evaluated in a rat IV (0.5 mg/kg)/PO (3 mg/kg) PK study in a 10% EtOH/40% PEG400/50% saline vehicle. VU6015929 displays a good in vitro:in vivo correlation (IVIC), with moderate in vivo clearance (CL
p
= 34.2 mL/min/kg), an ~3 hour half-life, moderate volume of distribution at steady state (V
ss
= 4.3 L/kg) and 12.5% oral bioavailability with a rapid T
max
(0.75 hr).
VU6015929
上下游产品信息
上游原料
下游产品
VU6015929 试剂级价格
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-135401 | VU6015929 | | 1 mg | 1333元 |
| 2024/04/30 | HY-135401 | VU6015929
VU6015929 | | 5mg | 3500元 |