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Org 27569
CAS No. 868273-06-7
Org 27569( Org-27569 | Org27569 )
Catalog No. M16306 CAS No. 868273-06-7
Org 27569 is a potent, selective, allosteric modulator of cannabinoid CB1 receptor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 46 | In Stock |
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| 2MG | 29 | In Stock |
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| 5MG | 46 | In Stock |
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| 10MG | 77 | In Stock |
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| 25MG | 151 | In Stock |
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| 50MG | 276 | In Stock |
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| 100MG | 412 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameOrg 27569
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NoteResearch use only, not for human use.
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Brief DescriptionOrg 27569 is a potent, selective, allosteric modulator of cannabinoid CB1 receptor.
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DescriptionOrg 27569 is a potent, selective, allosteric modulator of cannabinoid CB1 receptor, significantly increases the binding of the CB1 receptor agonist [3H]CP 55,940 with pKb of 5.67; reduces food consumption in rats, produces CB1-independent hypophagic effects and does not affect the discriminative stimulus effects of anandamide (AEA).
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In VitroOrg 27569 enhances agonist (CP55940) binding, promotes agonist binding to CB1 yet inhibits agonist-induced G protein activation and blocks the agonist-induced conformational changes in TM6. Org 27569 inhibits agonist-induced TM6 movement in CB1 detected by a fluorescent probe on site 342. Org 27569 produces a significant, but saturable, increase in the level of specific [3H]CP 55,940 binding. Org 27569 (1 μM) inhibits electrically evoked contractions of the mouse vas deferens with the pEC50 and Emax being 8.66±0.11 and 77% (95% confidence limits, 70.6-82.7), respectively. In hCB1R cells, Org 27569 (1 and 10 μM) behaves as a weak inverse agonist producing a small but significant decrease in basal [35S]GTPγS binding. Org 27569 is less effective as an inhibitor of WIN55212-mediated inhibition of forskolin-stimulated cAMP production. Org 27569 induces a small but significant level of ERK1/2 phosphorylation with an Emax of 19% and pEC50 value of 8.55±0.99.
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In VivoORG 27569 (3.2 and 5.6 mg/kg, i.p.) significantly attenuates cocaine associated cue-induced reinstatement, cocaine priming-induced reinstatement, methamphetamine associated cue-induced reinstatement and methamphetamine priming-induced reinstatement in rat. Org27569 (30 mg/kg, i.p.) produces CB1-independent hypophagic effects and does not affect the discriminative stimulus effects of anandamide (AEA). Org27569 (100 μg intracerebroventricularly) does not affect the pharmacologic effects of systemically administered CP55,940 compared with vehicle.
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SynonymsOrg-27569 | Org27569
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PathwayGPCR/G Protein
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TargetCannabinoid Receptor
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RecptorCB1
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Research AreaNeurological Disease
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Indication——
Chemical Information
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CAS Number868273-06-7
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Formula Weight409.95
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Molecular FormulaC24H28ClN3O
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 52.2 mg/mL
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SMILESO=C(C(N1)=C(CC)C2=C1C=CC(Cl)=C2)NCCC3=CC=C(N4CCCCC4)C=C3
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Chemical Name1H-Indole-2-carboxamide, 5-chloro-3-ethyl-N-[2-[4-(1-piperidinyl)phenyl]ethyl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Price MR, et al. Mol Pharmacol. 2005 Nov;68(5):1484-95.
2. Erdozain AM, et al. Biochem Pharmacol. 2012 Jan 15;83(2):260-8.
3. Fay JF, et al. J Biol Chem. 2012 Sep 28;287(40):33873-82.
4. Gamage TF, et al. Behav Pharmacol. 2014 Apr;25(2):182-5.
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