 
        
        
        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 +
 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+ | 
 
                                 
                                
                            

| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
| {[ item.pr_size ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} | 现货 | 1周 咨询 | - + | 
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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。 | |||||||||||||||||||
| 描述 | LY2183240 is a highly potent blocker of anandamide uptake (IC50 = 270 pM). | 
| 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 | 
| 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 | 
| 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 | |
| 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 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 
 
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