LY2183240

ArtNr	HY-10865-5mg
Hersteller	MedChem Express
CAS-Nr.	874902-19-9
Menge	5 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 1 mg 25 mg 50 mg 5 mg
Kategorie	Inhibitors & Compound Libraries Small Molecules
Typ	Inhibitors
Specific against	other
Purity	98.01
Citations	[1]Moore SA, et al. Identification of a high-affinity binding site involved in the transport of endocannabinoids. Proc Natl Acad Sci U S A. 2005;102(49):17852-17857.\|[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.\|[3]Maione S, et al. Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor-mediated mechanisms. Br J Pharmacol. 2008 Nov;155(5):775-82.\|[4]Pelorosso FG, et al. The endocannabinoid anandamide inhibits kinin B1 receptor sensitization through cannabinoid CB1 receptor stimulation in human umbilical vein. Eur J Pharmacol. 2009 Jan 5;602(1):176-9.\|[5]Powers MS, et al. Effects of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seeking behaviors in mice selectively bred for high alcohol preference. Psychopharmacology (Berl). 2010 Dec;212(4):571-83.\|[6]Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814.
Smiles	O=C(N(C)C)N1N=NN=C1CC(C=C2)=CC=C2C3=CC=CC=C3
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Versandbedingung	Raumtemperatur
Lieferbar
Manufacturer - Type	Reference compound
Manufacturer - Applications	Neuroscience-Neuromodulation
Manufacturer - Targets	Autophagy; FAAH
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	307.35
Product Description	LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively[1][2] [3].
Manufacturer - Research Area	Neurological Disease
Solubility	DMSO: 50 mg/mL (ultrasonic)
Manufacturer - Pathway	Autophagy; Metabolic Enzyme/Protease; Neuronal Signaling
Clinical information	No Development Reported

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