Queen's Award Received in 2021 ISO 9001 Certified Delivered over 1,000,000 bio-reagents to life science researchers Trusted by Life Science Communities
Cart summary

You have no items in your shopping cart.

Org 27569

SKU: orb1223804

Description

Org 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).

Images & Validation

−
Org 27569

Key Properties

−
CAS Number868273-06-7
MW409.95
Purity>98% (HPLC)
FormulaC24H28ClN3O
SMILESO=C(C(N1)=C(CC)C2=C1C=CC(Cl)=C2)NCCC3=CC=C(N4CCCCC4)C=C3
TargetCannabinoid Receptor
SolubilityDMSO: ≥ 52.2 mg/mL

Bioactivity

−
In Vivo
ORG 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.
In Vitro
Org 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.

Storage & Handling

−
StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

−
Org-27569 | Org27569

Similar Products

−

  • Org 27569 [orb1305237]

    98.00% (May vary between batches)

    868273-06-7

    409.95

    C24H28ClN3O

    2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO)
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Quick Database Links

Gene Symbol
Cannabinoid Receptor

Protocol Information

Find More Protocols

Available Sizes

Select a size below

1 g
Enquire
200 mg
Enquire
500 mg
Enquire
2 mg
$ 70.00
5 mg
$ 90.00
10 mg
$ 140.00
25 mg
$ 260.00
50 mg
$ 470.00
100 mg
$ 700.00
Bulk Enquiry
Need technical support? Find your Distributor Return and Tax Policy

Email

[email protected]

UK Office

+44 (0)1223 859353

US Office

+1 (415) 906-5211

CN Office

+86 (27)-87663101

Distributors

biorbyt.com/distributor