Fig. 1 · Structure

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Org 27569

Cat. No. A11513 CAS 868273-06-7

CB1 modulator

Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24).

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Biological Activity

Target & Activity

Target Activity Value
CB1 pEC50 8.24

Cellular Effect

Cell Line Activity Value Description Reference
CHO EC50 83 nM Positive allosteric modulator activity at human CB1R expressed in CHO cells assessed as enhanced binding of [3H]CP55,940 after 60 mins by liquid scintillation spectrometric analysis [PMID: 26529344]
CHO-K1 IC50 2 nM Negative allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940 induced beta arrestin recruitment preincubated for 30 mins followed by addition of CP55940 for 90 mins by chemiluminescence assay [PMID: 27542310]
CHO-K1 EC50 324 nM Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte [PMID: 26529344]
CHO-K1 EC50 9.05 nM Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay [PMID: 26529344]
HEK293 EC50 0.64 μM Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins in presence of CP55,940 by cAMP BRET assay [PMID: 26203658]
HEK293 EC50 10.59 μM Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay [PMID: 26203658]
HEK293 EC50 2.09 μM Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 10 mins in presence of CP55,940 by cAMP BRET assay [PMID: 26203658]
HEK293 EC50 2.24 μM Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay [PMID: 26203658]

Specifications

Manufacturer Adooq Bioscience
Actions Modulator
CAS Number 868273-06-7
Applications CB1 modulator
Formula C24H28ClN3O
Molecular Weight 409.95
SMILES
CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 71 mg/mL (173.19 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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