KM 233 是一种经典的大麻素，具有良好的血脑屏障渗透性。相对于 THC，KM 233 对 CB2 受体具有选择性亲和力。 KM 233 可有效降低 U87 胶质瘤肿瘤负担，可用于胶质瘤研究。
| Cas No. | 628263-22-9 |
| Canonical SMILES | CC(C1=CC=CC=C1)(C)C2=CC(O)=C3C(OC(C)(C)[C@H]4[C@H]3CC(C)=CC4)=C2 |
| 分子式 | C25H30O2 |
| 分子量 | 362.5 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 20 mg/ml,Ethanol: 3 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Because selective activation of peripheral cannabinoid (CB2) receptors in rat C-6 glioma cells has been shown to induce apoptosis through enhanced ceramide synthesis de novo, CB2 agonists present potential as anti glioma agents. KM 233 is a δ8-tetrahydrocannabinol analog with a dimethyl substitution that exhibits high binding affinity for both the CB1 and CB2 receptors with 13-fold selectivity for the CB2 receptor (Kis = 12.3 and 0.91 nM, respectively). Demonstrating good lipophilicity and ability to penetrate the blood brain barrier, KM 233 inhibits human U87 glioma cell proliferation in vitro with an IC50 value of 1.4 μM and significantly reduces U87 glioma tumor size in vivo at a dose of 2 mg/kg in a SCID mouse xenograft side-pocket model. |
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