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| 25mg |
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Purity: ≥98%
LY2183240 is a novel, potent and highly potent inhibitor of FAAH (fatty acid amide hydrolase) and a blocker of anandamide uptake with IC50 of 270 pM. LY2183240 inhibits the reuptake of the endocannabinoid anandamide and also acts as an inhibitor of fatty acid amide hydrolase (FAAH), the primary enzyme responsible for degrading anandamide. LY-2183240 has been shown to produce both analgesic and anxiolytic effects in animal models. LY-2183240 has relatively poor selectivity and also inhibits several other enzyme side targets. Consequently, it was never developed for clinical use, though it remains widely used in research, and has also been sold as a designer drug.
| ln Vivo |
LY2183240 (3-30 mg/kg; ip) dose-dependently reduced formalin-induced painful paw-licking behavior in a model of persistent pain mechanisms involving formalin [1].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (formalin pain model) [1]
Doses: 3, 10, 30 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: In the formalin model of persistent pain, Formalin-induced paw licking pain behavior is attenuated in a dose-dependent manner. |
| References |
[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]. 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. [3]. 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. [4]. 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. [5]. 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. [6]. 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. |
| Molecular Formula |
C17H17N5O
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| Molecular Weight |
307.35000
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| CAS # |
874902-19-9
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| SMILES |
O=C(N1N=NN=C1CC2=CC=C(C3=CC=CC=C3)C=C2)N(C)C
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| InChi Key |
CUCQDDZYZNBQFE-KUNNFNOCSA-N
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| InChi Code |
InChI=1S/C12H10ClN5O5S2/c13-3-1-24-10-6(9(20)18(10)7(3)11(21)22)16-8(19)5(17-23)4-2-25-12(14)15-4/h2,6,10,23H,1H2,(H2,14,15)(H,16,19)(H,21,22)/b17-5-/t6-,10-/m1/s1
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| Chemical Name |
5-([1,1'-biphenyl]-4-ylmethyl)-N,N-dimethyl-1H-tetrazole-1-carboxamide
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| Synonyms |
LY2183240; LY-2183240; LY 2183240.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~162.68 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2536 mL | 16.2681 mL | 32.5362 mL | |
| 5 mM | 0.6507 mL | 3.2536 mL | 6.5072 mL | |
| 10 mM | 0.3254 mL | 1.6268 mL | 3.2536 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Mean (±SEM) % FPS in male and female HAP mice in each LY2183240 dose group during the first (test 1) and second (test 2) FPS test.
Mean (±SEM) % FPS in male and female LAP mice for each LY2183240 dose group during the first (test 1) and second (test 2) FPS test.Psychopharmacology (Berl). 2010 Dec;212(4):571-83. |
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 Mean (±SEM) alcohol (g/kg;a) and total fluid (ml/kg;b) intake in HAP mice within each LY2183240 dose group during the 2-h limited access session on the first (drug day 1) and second (drug day 2) drug testing days.Psychopharmacology (Berl). 2010 Dec;212(4):571-83. |
 Mean (±SEM) second per minute (s/min) on alcohol-paired floor (post-test–pre-test difference score) in male and female HAP mice in each LY2183240 dose group during the first and last 30 min of each of the three preference tests.Psychopharmacology (Berl). 2010 Dec;212(4):571-83. |
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