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

LY-404187 是有效的,选择性和中枢活性的 AMPA 受体的正变构调节剂,作用于 GluR1iGluR2iGluR2oGluR3iGluR4iEC50 值分别为 5.65、0.15、1.44、1.66 和 0.21 µM。LY-404187 有潜力用于许多精神疾病和神经退行性疾病的研究。

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LY-404187 Chemical Structure

LY-404187 Chemical Structure

CAS No. : 211311-95-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1100
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1 mg ¥400
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5 mg ¥1000
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10 mg ¥1700
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25 mg ¥3400
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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]

体外研究
(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.

体内研究
(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 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
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (292.00 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 2.9200 mL 14.6002 mL 29.2005 mL
5 mM 0.5840 mL 2.9200 mL 5.8401 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

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

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 2.9200 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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产品名称:
LY-404187
目录号:
HY-13456
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