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LY2183240 {[allProObj[0].p_purity_real_show]}

货号:A702851

LY2183240是一种强效的内源性大麻素吸收抑制剂,IC50 为 270 pM,同时也是脂肪酸酰胺水解酶(FAAH)的共价抑制剂(IC50 = 12.4 nM),并抑制其他多种丝氨酸水解酶。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
LY2183240 化学结构 CAS号:874902-19-9
LY2183240 化学结构
CAS号:874902-19-9
LY2183240 3D分子结构
CAS号:874902-19-9
LY2183240 化学结构 CAS号:874902-19-9
LY2183240 3D分子结构 CAS号:874902-19-9
规格 价格 会员价 库存 数量
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LY2183240 纯度/质量文件 产品仅供科研

货号:A702851 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 FAAH 其他靶点 纯度
URB-597 ++++

FAAH, IC50: 4.6 nM

99%
JNJ-1661010 +++

FAAH (human), IC50: 12 nM

FAAH (rat), IC50: 10 nM

99%
Biochanin A +

FAAH (human), IC50: 1.4 μM

FAAH (mouse), IC50: 1.8 μM

EGFR 98+%
PF-3845 ++

FAAH, Ki: 230 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

95%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 HCl ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

99%
Lys05 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

LY2183240 生物活性

描述 LY2183240 is a highly potent blocker of anandamide uptake (IC50 = 270 pM).

LY2183240 细胞实验

Cell Line
Concentration Treated Time Description References
HeLa cells 10 μM 20–40 hours Measure inhibition of [14C]-anandamide uptake Cell Mol Neurobiol. 2006 Jul-Aug;26(4-6):407-23
mouse primary cortical neurons 10 μM 24 and 72 hours To investigate the effect of LY-2183240 on cell death and morphology, results showed that LY-2183240 induces neuronal death with an IC50 of 6.9 μM and significantly reduced the total DAPI number, DAPI + NeuN number, and MAP2 intensity. iScience. 2024 Sep 30;27(11):111069
rat primary cortical neurons 10 μM To ascertain whether the rise in APs induced by LY-2183240 is linked to an elevation in intracellular Ca2+ level, results showed no discernible calcium response by LY-2183240. iScience. 2024 Sep 30;27(11):111069
mouse cortical neurons 10 μM To evaluate the effect of LY-2183240 on the intrinsic excitability of neurons, results showed that LY-2183240 increased the number of spontaneous action potentials (sAPs) and elevated the resting membrane potential (RMP). iScience. 2024 Sep 30;27(11):111069
chick embryo spinal motoneurons 1 μM 20-40 minutes LY2183240 significantly reduced AMPA miniature postsynaptic current frequency without affecting amplitude. J Neurosci. 2012 Sep 26;32(39):13597-607
RBL-2H3 cells 10 μM 16–20 hours Measure inhibition of [14C]-anandamide uptake Cell Mol Neurobiol. 2006 Jul-Aug;26(4-6):407-23

LY2183240 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Formalin-induced inflammatory pain model Intraperitoneal injection 2.5-5 mg/kg Single dose, 15 min before formalin injection LY2183240 significantly inhibited the second phase of formalin-induced nocifensive response, which was fully antagonized by CB1 receptor antagonists Br J Pharmacol. 2008 Nov;155(5):775-82
Mice High alcohol-preferring (HAP) and low alcohol-preferring (LAP) mice Intraperitoneal injection 10 and 30 mg/kg Administered 30 min prior to testing, lasting 48 hours To assess the effects of LY2183240 on fear-potentiated startle (FPS) and alcohol-seeking behaviors in high alcohol-preferring (HAP) and low alcohol-preferring (LAP) mice. Results showed that LY2183240 (30 mg/kg) reduced the expression of FPS in HAP mice during the second FPS test but had no effect in LAP mice. Additionally, LY2183240 enhanced alcohol-induced conditioned place preference (CPP) but did not significantly alter limited-access alcohol drinking behavior. Psychopharmacology (Berl). 2010 Dec;212(4):571-83
C57BL/6 mice Conditioned place preference (CPP) and self-administration (SA) models Intraperitoneal (i.p.) injection (CPP), intravenous (i.v.) injection (SA) 0.05 mg/10 μL/kg CPP: every other day for 4 times; SA: once daily for 12 days To evaluate the effect of LY-2183240 on reward-seeking behavior, results showed that LY-2183240 increased the lever pressing in SA tests and altered dwelling times in CPP tests, indicating its potential for abuse. iScience. 2024 Sep 30;27(11):111069

LY2183240 参考文献

[1]Dickason-Chesterfield AK, Kidd SR, et al. Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol Neurobiol. 2006 Jul-Aug;26(4-6):407-23.

[2]Alexander JP, Cravatt BF. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. J Am Chem Soc. 2006 Aug 2;128(30):9699-704.

LY2183240 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.54mL

6.51mL

3.25mL

LY2183240 技术信息

CAS号874902-19-9
分子式C17H17N5O
分子量 307.35
SMILES Code O=C(N1N=NN=C1CC2=CC=C(C3=CC=CC=C3)C=C2)N(C)C
MDL No. MFCD08703123
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(162.68 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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