VU0357017
产品编号: DC9255
Featured
我们的合作伙伴:
中国地区超过5000个高品质化合物库存
应用领域
VU0357017盐酸盐是一种高度选择性M1受体激动剂, 作用于变构位点, 激活受体（EC50=477 ± 172 nM, pEC50=6.37 ± 0.15）。
| Cas No.: |
1135242-13-5 |
| 名称: |
|
| 别名: |
VU0-357017,VU 0357017,CID-25010775; VU-0357017 hydrochloride; VU 0357017 hydrochloride |
| SMILES: |
CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C.Cl |
| 分子式: |
C18H28ClN3O3 |
| 分子量: |
369.89 |
| 纯度: |
|
| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
|
| In Vivo: |
|
| In Vitro: |
|
| References: |
VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
in vitro: VU0357017 is a M1-selective agonists that appear to activate M1 through actions at an allosteric site. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. VU0357017 is a potent and efficacious M1 agonist, selective versus M2?M5 family members and allosteric agonist. VU0357017 is a highly selective M1 agonist suggests that these compounds are unlikely to act at the highly conserved orthosteric site on M1 and are more likely to act as allosteric agonists.VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 significantly enhances threshold Θ-burst LTP and VU0364572 induces LTD at the Schaffer collateral-CA1 synapse of rodent hippocampal slices.
in vivo: VU0357017 has robust efficacy in improving hippocampal-dependent learning in rats. VU0357017 enhances performance in Morris water maze and contextual fear conditioning in rats. |
| Kinase Assay: |
|
| Cell Assay: |
|
| Animal Administration: |
|
| References: |
|
MSDS
COA
| LOT NO. |
DOWNLOAD |
|
|
| 2018-0101 |
|
询盘
