2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU0448088

VU0448088  (Synonyms: ML253)

目录号: HY-162663 纯度: 98.67%
COA 产品使用指南

摩尔计算器

VU0448088 (ML253) 是一种有效的、可穿过血脑屏障的三环毒蕈碱乙酰胆碱受体亚型 4 (tricyclic muscarinic acetylcholine receptor subtype 4 (M4)) 正变构调节剂，对人和大鼠的 EC50 值分别为 56, 176 nM。VU0448088 具有用于精神病研究的潜力。

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VU0448088 Chemical Structure

VU0448088 Chemical Structure

CAS No. : 1417616-42-2

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规格 价格 是否有货 数量
5 mg ￥1100
In-stock
10 mg ￥1750
In-stock
25 mg ￥3300
In-stock
50 mg ￥5300
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

VU0448088 相关抗体

Top Publications Citing Use of Products

查看 mAChR 亚型特异性产品:

查看所有亚型
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic[1][2].

IC50 & Target[1]

mAChR4

56 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 EC50
> 30 μM
Compound: 4, ML253 (VU0448088)
Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
[PMID: 23177787]
CHO-K1 EC50
> 30 μM
Compound: 4, ML253 (VU0448088)
Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
[PMID: 23177787]
CHO-K1 EC50
> 30 μM
Compound: 4, ML253 (VU0448088)
Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
[PMID: 23177787]
CHO-K1 EC50
> 30 μM
Compound: 4, ML253 (VU0448088)
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
[PMID: 23177787]
CHO-K1 EC50
56 nM
Compound: 4, ML253 (VU0448088)
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
[PMID: 23177787]
体内研究
(In Vivo)

VU0448088 (3, 10, 30, 56.6, 100 mg/kg; i.p.) 以剂量依赖性方式逆转苯丙胺引起的运动亢进[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat (amphetamine-induced hyperlocomotion)[1]
Dosage: 3, 10, 30, 56.6, 100 mg/kg
Administration: IP
Result: Reversed amphetamine-induced hyperlocomotion in a dose-dependent manner, showed a modest reduction of 26% at a dose of 10 mg/kg; at the three highest doses (30, 56.6 and 100 mg/kg), showed significant reductions of 47.9%, 53.7% and 57.3%, respectively.
分子量

346.83

Formula

C16H15ClN4OS
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 5 mg/mL (14.42 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8833 mL 14.4163 mL 28.8326 mL
5 mM 0.5767 mL 2.8833 mL 5.7665 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

VU0448088 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8833 mL 14.4163 mL 28.8326 mL 72.0814 mL
5 mM 0.5767 mL 2.8833 mL 5.7665 mL 14.4163 mL
10 mM 0.2883 mL 1.4416 mL 2.8833 mL 7.2081 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU04480881417616-42-2ML253VU 0448088VU-0448088ML 253ML-253mAChRMuscarinic acetylcholine receptorblood-brain barrierpsychoticamphetamineInhibitorinhibitorinhibit

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目录号：
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