大麻素作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetAnandamideCat. No.: HY-10863CAS No.: 94421-68-8分式: CHNO分量: 347.53作靶點(diǎn): Cannabinoid Receptor; GPR55; Endogenous Metabolite作通路: GPCR/G Protein; Neuronal Signaling; Metabolic Enzyme/Protease儲(chǔ)存式: Solution, -20C, 2 years溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 250 mg/mL (719.36 mM)* means soluble, but saturatio

2、n unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.8774 mL 14.3872 mL 28.7745 mL5 mM 0.5755 mL 2.8774 mL 5.7549 mL10 mM 0.2877 mL 1.4387 mL 2.8774 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)

3、驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.99 mM); Clear solution此案可獲得 2.08 mg/mL (5.99 mM，飽和度未

4、知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.99 mM); Clear solution此案可獲得 2.08 mg/mL (5.99 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液

5、加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.99 mM); Clear solution此案可獲得 2.08 mg/mL (5.99 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Anandamide種中樞神經(jīng)系統(tǒng)的免疫

6、調(diào)節(jié)劑，不僅通過(guò)素受體 (CB1 和 CB2) 且通過(guò)其他靶點(diǎn) (如 GPR18/GPR55) 起作。IC & Target Human Endogenous CB1 CB2 GPR18/GPR55Metabolite體外研究 Anandamide, acting via CB2 receptors, alleviates lipopolysaccharide (LPS)-induced neuroinflammation in rat primarymicroglial cultures. The endocannabinoid system modulates both neuronal

7、and immune functions through twoprotein-coupled cannabinoid receptors (CB1 and CB2), although endocannabinoids, especially Anandamide (AEA), canactivate numerous other receptors like PPARS, TRPV1, and GPR18/GPR551.體內(nèi)研究 Anandamide is an endocannabinoid binding both CB1R and CB2R. To evaluate the impa

8、ct of CBR activation onwhole-body glucose homeostasis, glucose tolerance is assessed after a single intraperitoneal Anandamide injection (10 mg/kg). The increase in glycemia in response to glucose ingestion is considerably smaller in mice treated withAnandamide compared with control, and this is ass

9、ociated with an improvement of glucose tolerance as illustrated bythe AUC0-2h calculations2.PROTOCOLAnimal Mice2Administration 2 Eleven-week-old C57BL/6J male mice and global CB1R-/- mice are housed individually on a 12/12-h light/darkschedule at 22-23C with ad libitum access to water and food. A gr

10、oup of mice is subject to a high-fat diet (30% lard).After 16 weeks of diet, animals with a weight gain less than +10 g compared with controls are excluded from thestudy. Diet-induced obesity (DIO) mice (39.11.1 vs. 27.30.9 g, DIO vs. control) are glucose intolerant and insulinresistant. On the day

11、of each experiment, food is removed from the cages for 6 h (from 8:00 A.M. to 2:00 P.M.).Anandamide is administered intraperitoneally at 10 mg/kg. In control experiments, animals are injected with vehicle(4% DMSO/1% Tween 80)2.MCE has not independently confirmed the accuracy of these methods. They a

12、re for reference only.REFERENCES1. Malek N, et al. Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures. Neural Plast.2015;2015:130639.2. Troy-Fioramonti S, et al. Acute activation of cannabinoid receptors by Anandamide reduces gastrointestinal motility and improves postprandial glycemiain mice. Diabetes. 2015 Mar;64(3):808-18.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not