| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87924-2mg买3赠1 |
98.00% | ￥345.00 |
9 | - | - | - | - |
|
S87924-5mg买3赠1 |
98.00% | ￥410.00 |
6 | - | - | - | - |
|
S87924-10mg买3赠1 |
98.00% | ￥630.00 |
6 | - | - | - | - |
|
S87924-25mg促销 |
98.00% | ￥1180.00 ￥944.00 |
4 | - | - | - | - |
|
S87924-50mg促销 |
≥98% | ￥1650.00 ￥1320.00 |
货期：2-3天 | - | - | - | - |
|
S87924-100mg促销 |
≥98% | ￥2650.00 ￥2120.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM). It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively). | ||||||||||||||||||||
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| 靶点： | Cannabinoid Receptor;CannabinoidReceptor | ||||||||||||||||||||
| 体外研究： | In vitro, LY2828360 was a slowly acting but efficacious G protein-biased CB2 agonist, inhibiting cAMP accumulation and activating extracellular signal-regulated kinase 1/2 signaling while failing to recruit arrestin, activate inositol phosphate signaling, or internalize CB2 receptors. | ||||||||||||||||||||
| 体内研究： | In wild-type (WT) mice, LY2828360 (3 mg/kg per day × 12 days) suppressed chemotherapy-induced neuropathic pain produced by paclitaxel without producing tolerance. Antiallodynic efficacy of LY2828360 was absent in CB2 knockout (KO) mice. Morphine (10 mg/kg per day × 12 days) tolerance developed in CB2KO mice but not in WT mice with a history of LY2828360 treatment (3 mg/kg per day × 12 days). LY2828360-induced antiallodynic efficacy was preserved in WT mice previously rendered tolerant to morphine (10 mg/kg per day × 12 days), but it was absent in morphine-tolerant CB2KO mice. Coadministration of LY2828360 (0.1 mg/kg per day × 12 days) with morphine (10 mg/kg per day × 12 days) blocked morphine tolerance in WT but not in CB2KO mice. WT mice that received LY2828360 coadministered with morphine exhibited a trend (P = 0.055) toward fewer naloxone-precipitated jumps compared with CB2KO mice. LY2828360 is a slowly signaling, G protein-biased CB2 agonist that attenuates chemotherapy-induced neuropathic pain without producing tolerance and may prolong effective opioid analgesia while reducing opioid dependence. LY2828360 may be useful as a first-line treatment in chemotherapy-induced neuropathic pain and may be highly efficacious in neuropathic pain states that are refractive to opioid analgesics. | ||||||||||||||||||||
| 参考文献： | 1. Lin X , Dhopeshwarkar A S , Huibregtse M , et al. The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained efficacy and attenuates morphine tolerance and dependence[J]. Molecular Pharmacology, 2017:mol.117.109355. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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