| Bioactivity | (Rac)-ZLc-002, an inhibitor of nNOS interaction with nitric oxide synthase 1 adaptor protein (NOS1AP), suppresses inflammatory nociception and chemotherapy-induced neuropathic pain and synergizes with Paclitaxel (HY-B0015) to reduce tumor cell viability[1][2]. | ||||||||||||
| Target | nNOS/NOS1AP interaction | ||||||||||||
| Invitro | (Rac)-ZLc-002 (10 μM) 可降低原代培养皮层神经元 NOS1AP 与 nNOS 免疫共沉淀。(Rac)-ZLc-002 在 AlphaScreen 体外结合实验中未能破坏 nNOS-NOS1AP 蛋白-蛋白相互作用。在无细胞检测中无活性[1]。(Rac)-ZLc-002 (10 μM) 可降低共表达全长 nNOS 的 HEK293T 细胞中全长 NOS1AP 的共免疫沉淀，但不能降低 PSD95-PDZ2 的共免疫沉淀[1]。(Rac)-ZLc-002 (0-50 μM; 72 h) 与 Paclitaxel (HY-B0015) 协同降低肿瘤细胞活力[1]。 Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | (Rac)-ZLc-002 (10 mg/kg; i.p.; once or daily for 8 days) 减轻 Paclitaxel (HY-B0015) 引起的机械性和冷性异位痛，抑制 Paclitaxel 诱导的小鼠模型神经性疼痛[1]。(Rac)-ZLc-002 (4 and 10 mg/kg; i.p.; once) 降低大鼠脊髓背角福尔马林诱发的痛觉行为和福尔马林样免疫反应性[1]。(Rac)-ZLc-002 (40 mg/kg/day; i.v.; 7 days) 减弱 ICR 小鼠慢性轻度应激 (CMS) 诱导的焦虑行为[2]。(Rac)-ZLc-002 (10 μM; 1 μl; 30 min after Corticosterone, HY-B1618) 海马体注射 7 天逆转糖皮质激素对小鼠的行为影响[2]。 Animal Model: | ||||||||||||
| Name | (Rac)-ZLc-002 | ||||||||||||
| Formula | C10H17NO5 | ||||||||||||
| Molar Mass | 231.25 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Lee WH, Carey LM, Li LL, et al. ZLc002, a putative small-molecule inhibitor of nNOS interaction with NOS1AP, suppresses inflammatory nociception and chemotherapy-induced neuropathic pain and synergizes with paclitaxel to reduce tumor cell viability. Mol Pain. 2018;14:1744806918801224. [2]. Zhu LJ, Shi HJ, Chang L, et al. nNOS-CAPON blockers produce anxiolytic effects by promoting synaptogenesis in chronic stress-induced animal models of anxiety. Br J Pharmacol. 2020;177(16):3674-3690. |