Org 27569 is a potentCB1receptorallosteric modulator, which increases agonist binding, yet blocks agonist-inducedCB1signaling.

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^[2]. 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 pEC₅₀and E_maxbeing 8.66±0.11 and 77% (95% confidence limits, 70.6-82.7), respectively^[4]. 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 E_maxof 19% and pEC₅₀value of 8.55±0.99^[5].

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^[1]. 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^[3].

409.95

Solid

C₂₄H₂₈ClN₃O

868273-06-7

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 52.2 mg/mL(127.33 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: 2.5 mg/mL (6.10 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.10 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 2.5 mg/mL (6.10 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.10 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。