LY2183240
Based on 3 publication(s) in Google Scholar
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 .
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- Purity: 98.00%
- CAS No.: 874902-19-9
- 화학식: C17H17N5O
- 분자량:307.35
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LY2183240
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Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
26.9 μM
Compound: 1, LY2183240
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Agonist activity at rat TRPA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ concentration by spectrofluorimetric analysis
Agonist activity at rat TRPA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ concentration by spectrofluorimetric analysis
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[PMID: 23474898] |
| HEK293 | IC50 |
>100 μM
Compound: 1, LY2183240
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Antagonist activity at human TRPV1 receptor expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular Ca2+ elevation incubated for 5 mins prior to capsaicin-stimulation by spectrofluorimetric analysis
Antagonist activity at human TRPV1 receptor expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular Ca2+ elevation incubated for 5 mins prior to capsaicin-stimulation by spectrofluorimetric analysis
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[PMID: 23474898] |
| HEK293 | IC50 |
49.4 μM
Compound: 1, LY2183240
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Antagonist activity at rat TRPA1 receptor expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular Ca2+ elevation incubated for 5 mins prior to allyl isothiocyanate-stimulation by spectrofluorimetric analysis
Antagonist activity at rat TRPA1 receptor expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular Ca2+ elevation incubated for 5 mins prior to allyl isothiocyanate-stimulation by spectrofluorimetric analysis
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[PMID: 23474898] |
| RBL-2H3 | IC50 |
0.015 μM
Compound: 1, LY-2183240
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Inhibition of [14C]anandamide uptake in rat RBL-2H3 cells preincubated 10 mins before addition of [14C]anandamide
Inhibition of [14C]anandamide uptake in rat RBL-2H3 cells preincubated 10 mins before addition of [14C]anandamide
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[PMID: 17452063] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (Formalin Pain Model)[1]
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Dosage:3, 10, 30 mg/kg
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Administration:I.p.
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Result:Dose-dependently attenuated formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms.
Chemical Information
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CAS No. 874902-19-9
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Appearance Solid
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분자량 307.35
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화학식 C17H17N5O
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Color White to yellow
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SMILES
O=C(N(C)C)N1N=NN=C1CC(C=C2)=CC=C2C3=CC=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
FAAH served a key membrane-anchoring and stabilizing role for NLRP3 protein independently of the endocannabinoid system. [Abstract]2023 Jan;30(1):168-183. PMID: 36104448 -
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Eur J Pain
Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. [Abstract]2017 May;21(5):804-814. PMID: 28107590
용액&용해도
In Vitro:
DMSO : 50 mg/mL (162.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2536 mL | 16.2681 mL | 32.5362 mL | 81.3405 mL |
| 5 mM | 0.6507 mL | 3.2536 mL | 6.5072 mL | 16.2681 mL | |
| 10 mM | 0.3254 mL | 1.6268 mL | 3.2536 mL | 8.1340 mL | |
| 15 mM | 0.2169 mL | 1.0845 mL | 2.1691 mL | 5.4227 mL | |
| 20 mM | 0.1627 mL | 0.8134 mL | 1.6268 mL | 4.0670 mL | |
| 25 mM | 0.1301 mL | 0.6507 mL | 1.3014 mL | 3.2536 mL | |
| 30 mM | 0.1085 mL | 0.5423 mL | 1.0845 mL | 2.7113 mL | |
| 40 mM | 0.0813 mL | 0.4067 mL | 0.8134 mL | 2.0335 mL | |
| 50 mM | 0.0651 mL | 0.3254 mL | 0.6507 mL | 1.6268 mL | |
| 60 mM | 0.0542 mL | 0.2711 mL | 0.5423 mL | 1.3557 mL | |
| 80 mM | 0.0407 mL | 0.2034 mL | 0.4067 mL | 1.0168 mL | |
| 100 mM | 0.0325 mL | 0.1627 mL | 0.3254 mL | 0.8134 mL |
LY2183240 Related Classifications
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