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  2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. LY-404187

LY-404187 是有效的，選擇性和中樞活性的 AMPA 受體的正變構(gòu)調(diào)節(jié)劑，作用于 GluR1i，GluR2i，GluR2o，GluR3i 和 GluR4i 的 EC50 值分別為 5.65、0.15、1.44、1.66 和 0.21 μM。LY-404187 有潛力用于許多精神疾病和神經(jīng)退行性疾病的研究。

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LY-404187 Chemical Structure

LY-404187 Chemical Structure

CAS No. : 211311-95-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1100
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1 mg ￥400
In-stock
5 mg ￥1000
In-stock
10 mg ￥1700
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25 mg ￥3400
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Customer Review

查看 iGluR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 μM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases[1][2].

IC50 & Target

EC50: 5.65 μM (GluR1i), 0.15 μM (GluR2i), 1.44 μM (GluR2o), 1.66 μM (GluR3i), 0.21 μM (GluR4i)[2]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
1061 nM
Compound: 5b
Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
[PMID: 16879964]
HEK293 EC50
1905 nM
Compound: 5b
Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
[PMID: 16879964]
HEK293 EC50
290 nM
Compound: 3a
Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors.
Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors.
[PMID: 11985477]
HEK293 EC50
420 nM
Compound: 5b
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
[PMID: 16879964]
HEK293 EC50
559 nM
Compound: 5b
Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
[PMID: 16879964]
體外研究
(In Vitro)

LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells[2].
LY-404187 (0.03-10 μM) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC50=1.3±0.3 μM) and efficacy (Emax=45.3±8.0-fold increase) [3].
LY-404187 does not affect the magnitude or time course of wholecell K+ or Na+ currents in pre frontal cortex (PFC) pyramidal neurons at concentrations of 10 μM[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent MPTP-induced neurotoxicity in mice[4].
LY-404187 (0.5 mg/kg; s.c. for 28 days) attenuates apomorphine-induced contraversive rotations and affords significant protection against the loss of tyrosine hydroxylase positive nigral cell bodies[4].
LY-404187 (0.1 or 0.5 mg/kg; s.c. for 14 days) affords functional, neurochemical and histological protection after infusion of 6-hydroxydopamine into the substantia nigra in rats[4].
LY-404187 (0.5 mg/kg; s.c. for 14 days) delayed treatment provides functional and histological improvement, suggesting a trophic action as administration is initiated after cell death[4].
LY-404187 (0.1 and 0.5 mg/kg; s.c. for 14 days) increases GAP-43 immunoreactivity in the striatum in a dose-dependent manner[4].

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

Animal Model: Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8[4]
Dosage: 0.5 mg/kg
Administration: S.c; twice daily on weekdays and once daily at weekends for 11 days
Result: Attenuated the loss of tyrosine hydroxylase immunoreactivity in the substantia nigra.
No significant change in tyrosine hydroxylase immunoreactivity in the dorsal and ventral striatum.
分子量

342.46

Formula

C19H22N2O2S
CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (292.00 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.9200 mL 14.6002 mL 29.2005 mL
5 mM 0.5840 mL 2.9200 mL 5.8401 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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 1 mM 2.9200 mL 14.6002 mL 29.2005 mL 73.0012 mL
5 mM 0.5840 mL 2.9200 mL 5.8401 mL 14.6002 mL
10 mM 0.2920 mL 1.4600 mL 2.9200 mL 7.3001 mL
15 mM 0.1947 mL 0.9733 mL 1.9467 mL 4.8667 mL
20 mM 0.1460 mL 0.7300 mL 1.4600 mL 3.6501 mL
25 mM 0.1168 mL 0.5840 mL 1.1680 mL 2.9200 mL
30 mM 0.0973 mL 0.4867 mL 0.9733 mL 2.4334 mL
40 mM 0.0730 mL 0.3650 mL 0.7300 mL 1.8250 mL
50 mM 0.0584 mL 0.2920 mL 0.5840 mL 1.4600 mL
60 mM 0.0487 mL 0.2433 mL 0.4867 mL 1.2167 mL
80 mM 0.0365 mL 0.1825 mL 0.3650 mL 0.9125 mL
100 mM 0.0292 mL 0.1460 mL 0.2920 mL 0.7300 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：
LY-404187
目錄號(hào)：
HY-13456
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