1. GPCR/G Protein Neuronal Signaling
  2. Somatostatin Receptor
  3. L-803087

L-803087 是一种有效的选择性的生长抑素 sst4 受体激动剂,Ki 为 0.7 nM,比其他生长抑素受体的选择性高 280 倍以上。L-803087 在体外促进 AMPA 介导的海马突触反应,在体内增加了海藻酸盐诱导的小鼠癫痫发作。

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L-803087 Chemical Structure

L-803087 Chemical Structure

CAS No. : 217480-26-7

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5 mg ¥3500
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10 mg ¥5600
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查看 Somatostatin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2].

IC50 & Target

Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)[1]

体外研究
(In Vitro)

L-803087 has Ki values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively[1].
L-803087 has a diamine moiety that maps to lysine on the phmacophore, but relation of this molecule to the aromatic and the Trp substituents of the phmacophore are not obvious. L-803087 does not inhibit secretion of growth hormone, insulin, or glucagon[1].

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

体内研究
(In Vivo)

L-803087 (5 nmol) is doubled seizure activity in wild-type mice on average. Interestingly, this effect is blocked by 3 nmol Octreotide. In hippocampal slices from wild-type mice, Octreotide (2 μM) does not modify AMPA-mediated synaptic responses while facilitation occurred with L-803087 (2 μM)[2].

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

分子量

485.53

Formula

C25H29F2N5O3

CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 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 : 250 mg/mL (514.90 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 2.0596 mL 10.2980 mL 20.5961 mL
5 mM 0.4119 mL 2.0596 mL 4.1192 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

纯度: ≥98.0%

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 2.0596 mL 10.2980 mL 20.5960 mL 51.4901 mL
5 mM 0.4119 mL 2.0596 mL 4.1192 mL 10.2980 mL
10 mM 0.2060 mL 1.0298 mL 2.0596 mL 5.1490 mL
15 mM 0.1373 mL 0.6865 mL 1.3731 mL 3.4327 mL
20 mM 0.1030 mL 0.5149 mL 1.0298 mL 2.5745 mL
25 mM 0.0824 mL 0.4119 mL 0.8238 mL 2.0596 mL
30 mM 0.0687 mL 0.3433 mL 0.6865 mL 1.7163 mL
40 mM 0.0515 mL 0.2575 mL 0.5149 mL 1.2873 mL
50 mM 0.0412 mL 0.2060 mL 0.4119 mL 1.0298 mL
60 mM 0.0343 mL 0.1716 mL 0.3433 mL 0.8582 mL
80 mM 0.0257 mL 0.1287 mL 0.2575 mL 0.6436 mL
100 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5149 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:
L-803087
目录号:
HY-108497
需求量: