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

ADX-47273 是一種有效的，選擇性和可透過血腦屏障的 mGluR5 陽性變構(gòu)調(diào)節(jié)劑 (PAM)，增強谷氨酸 (50 nM) 反應的 EC50 值為 0.17 μM。 ADX-47273 具有抗精神病和增強認知的活性。

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ADX-47273 Chemical Structure

ADX-47273 Chemical Structure

CAS No. : 851881-60-2

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規(guī)格 價格 是否有貨 數(shù)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
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50 mg ￥3300
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100 mg ￥5800
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200 mg   詢價  
500 mg   詢價  

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Other Forms of ADX-47273:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

細胞效力
(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]
體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗： 

Methanol 中的溶解度 : 105.5 mg/mL (285.63 mM; 超聲加熱助溶)

DMSO 中的溶解度 : ≥ 31 mg/mL (83.93 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.94%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
ADX-47273
目錄號：
HY-13058
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