- JNJ-1661010
- URB597
- PF-3845
| LY2183240Blocker of anandamide uptake,highly potent |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | LY2183240 is a novel and highly potent inhibitor of anandamide uptake with an IC50 value of 270 pM. | |||||
| Targets | anandamide uptake | fatty acid amide hydrolase (FAAH) | ||||
| IC50 | 270 pM | 12.4 nM | ||||
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| Cas No. | 874902-19-9 | SDF | Download SDF |
| Synonyms | LY 2183240; LY-2183240 | ||
| Chemical Name | N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide | ||
| Canonical SMILES | CN(C)C(=O)N1C(=NN=N1)CC2=CC=C(C=C2)C3=CC=CC=C3 | ||
| Formula | C17H17N5O | M.Wt | 307.35 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
LY2183240 is a highly potent blocker of anandamide uptake with IC50 value of 270 pM, and an inhibitor of fatty acid amide hydrolase (FAAH) activity with IC50 value of 12.4 nM [1].
Fatty acid amide hydrolase (FAAH) belongs to the family of serine hydrolase, which is an integral membrane enzyme. It has esterase and amidase activity that are responsive for the uptake of fatty acid amide (FAA) family signaling lipids, including anandamide. The uptake and metabolic process of anandamide is mainly achieved by FAAH, therefore the inhibition of FAAH may result in the blockage of anadaminde uptake.
LY2183240 is a potent and covalent inhibitor of FAAH, with the effect of blocking anandamide uptake. Biochemical research had identified that LY2183240 inactivate FAAH via carbamylation of the serine nucleophile of FAAH [2]. In RBL cell line containing FAAH, radioactive labeled 3H-LY2183240 exhibited strong binding to FAAH, inhibition of FAAH and thus blockage of anandamide uptake. However, in HeLa cells lacking FAAH, 3H-LY2183240 was less bound, and the blockage of anandamide uptake was very weak. It suggested that the direct interaction between LY2183240 and FAAH was required to block the anandamide uptake. However, it also indicated that there might be uncharacterized pathways of anandamide uptake regulated by LY2183240, independent from FAAH [1]. However, FAAH is not the sole target for LY2183240. Several uncharacterized brain serine hydrolases were also identified as the target of LY2183240, and these might be additional pathway for anandamide uptake [2].
In mouse model, 10 mg/kg injection of LY2183240 would produce analgesic effects in the formalin test of noxious pain which is a phenotype associated with elevated level of anandamide in brain. It indicated LY2183240 might inhibit FAAH in vivo [2]. When mice were administrated with LY2183240 (10 mg/kg, ip) for 90 min, characterization of brain tissues revealed that LY2183240 inactivated FAAH and other brain serine hydrolases ranging from 25-35 kDa [2].
References:[1] Dickason-Chesterfield A K et al., Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol Neurobiol. 2006, 26(4-6): 407-23.[2] Alexander J P, Cravatt B F. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. J Am Chem Soc. 2006, 128(30): 9699-9704.
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实验需要请问有没有养THP-1细胞的同仁？能否寄一皿我，我在广州南方医科大学，不胜感激！
激光共聚焦的看活细胞皿哪里买呢
想问下各位大神，本人用皿养的PC-9GR细胞突然有大片飘起，也并没有成团状飘起，求解决方法？
如题~
已经基本养好了贴壁的原代细胞了，准备鉴定了，看到好多都在说细胞爬片的问题，我可以不做爬片直接在皿里操作吗？具体需要注意些什么呢？感谢各位大神
ps：大皿和6孔板里细胞密度、培养条件等等都几乎一样。
我看园子里有人提过类似的问题，但还没人给出答案，希望有经验或有想法的战友帮忙分析分析啊~谢谢！
同学说传代必须是一皿传多皿，一皿传一皿就不算传代~求高手指点~~
传代后5天，依然没有长满，怕影响活力，想传代和冻存，不知这样是否可以？？
做细胞实验快半年了，一直都还挺顺的，这次五一放完假回来，复苏一支HK2，操作都跟以前一样，没想到出了好多问题：
冻存方法：包裹棉花直接-80℃过夜，第二天转移到液氮
冻存时间：1个半月前冻存的细胞，密度保证没问题，冻存前状态也好
复苏方法：液氮取出后37℃水浴，约2分钟溶解，加入6倍体积的完全培养基，800转离心5分钟，弃去上清，1ml完全培养基重悬，转移入培养皿（进口一次性塑料培养大皿），补足完全培养基，培养箱培养
第二天看细胞全都没贴壁，但是也没死，聚集成团装飘着，没有污染。不想重新离心加重机械损伤，就一直试试看的心态放在培养箱里养着了。又重新复苏一支，还是一样的结果，全飘着没贴壁。不死心，就往前面复苏的那一皿里直接加了1ml的血清，相当于18%的血清比例，过了一天去看，这下细胞都贴壁了。没有另外添加血清的那一皿就还是没贴壁。
另外还有一支以前复苏的HK2，也是一样的方法复苏的，那次复苏很好，细胞基本没什么死的，也都贴壁了，养在皿里状态也不错，但是拿来铺板就还是不贴壁，同样的培基（10%血清），铺板就一个不贴，皿里就都可以贴上。
求助各位战友：
1、复苏不贴壁是为什么？
2、增加血清比例能使复苏的细胞贴壁，这样的细胞是不是可以认为状态并不好，以后的培养是不是要一直这么高比例的血清？还是可以培养一段时间逐步减少血清比例？
3、仍然是10%血清，为什么铺板就不贴壁，而皿里的就没事？是不是铺板的时候也要增加血清比例呢？那在板里干预的过程中是不是要一直保持高比例的血清培养？
4、我的冻存及复苏方法是否有错？我觉得我的HK2从形态、生长速度上来说状态应该是不错的，而且我已经更换了全新的培基、血清和双抗，重新配置了完全培养基，不知道为什么会出现这种不贴壁的问题
拜托各位集思广益，细胞实验已经为了这个不贴壁的问题停滞快2周，心急如焚啊，拜托各位！
