2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. ADX-47273

ADX-47273 是一种有效的，选择性和可透过血脑屏障的 mGluR5 阳性变构调节剂 (PAM)，增强谷氨酸 (50 nM) 反应的 EC50 值为 0.17 μM。 ADX-47273 具有抗精神病和增强认知的活性。

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ADX-47273 Chemical Structure

ADX-47273 Chemical Structure

CAS No. : 851881-60-2

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605
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5 mg ￥550
In-stock
10 mg ￥880
In-stock
50 mg ￥3300
In-stock
100 mg ￥5800
In-stock
200 mg   询价  
500 mg   询价  

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Other Forms of ADX-47273:

ADX-47273 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities[1][2].

IC50 & Target[1]

mGluR5

0.17 μM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
157 nM
Compound: 7, ADX-47273
Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
HEK293 EC50
199 nM
Compound: 2, ADX47273
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
[PMID: 23947773]
HEK293 EC50
55 nM
Compound: 7, ADX-47273
Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
[PMID: 24050755]
体外研究
(In Vitro)

ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5 without eliciting a response by itself[1].
ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 300 nM glutamate in primary astrocyte cultures, with an EC50 of 0.23 μM[1].
ADX47273 (0.01-10 μM; 60 min) inhibits [3H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a Ki of 4.3 μM[1].

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

ADX-47273 相关抗体:
体内研究
(In Vivo)

ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex[1].
ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats[1].
ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice[1].
ADX47273 (0.1-50 mg/kg; i.p.) increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats[1].
ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice[3].

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

Animal Model: Male Long-Evans rats[1]
Dosage: 1, 10 mg/kg
Administration: A single i.p.
Result: Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus.
分子量

369.36

Formula

C20H17F2N3O2
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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

Methanol 中的溶解度 : 105.5 mg/mL (285.63 mM; 超声加热助溶)

DMSO 中的溶解度 : ≥ 31 mg/mL (83.93 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7074 mL 13.5369 mL 27.0739 mL
5 mM 0.5415 mL 2.7074 mL 5.4148 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

纯度: 99.94%

COA (283 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

ADX-47273 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Methanol 1 mM 2.7074 mL 13.5369 mL 27.0739 mL 67.6846 mL
5 mM 0.5415 mL 2.7074 mL 5.4148 mL 13.5369 mL
10 mM 0.2707 mL 1.3537 mL 2.7074 mL 6.7685 mL
15 mM 0.1805 mL 0.9025 mL 1.8049 mL 4.5123 mL
20 mM 0.1354 mL 0.6768 mL 1.3537 mL 3.3842 mL
25 mM 0.1083 mL 0.5415 mL 1.0830 mL 2.7074 mL
30 mM 0.0902 mL 0.4512 mL 0.9025 mL 2.2562 mL
40 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6921 mL
50 mM 0.0541 mL 0.2707 mL 0.5415 mL 1.3537 mL
60 mM 0.0451 mL 0.2256 mL 0.4512 mL 1.1281 mL
80 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8461 mL
Methanol 100 mM 0.0271 mL 0.1354 mL 0.2707 mL 0.6768 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:

ADX-47273851881-60-2ADX47273ADX 47273mGluRMetabotropic glutamate receptorsmGluR5glutamateantipsychoticprocognitiveInhibitorinhibitorinhibit

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产品名称：
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目录号：
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