2. Immunology/Inflammation
  3. Interleukin Related
  4. CN016

CN016 是一种神经保护剂。CN016 抑制 Oxaliplatin (HY-17371) 诱导的促炎细胞因子 G-CSF、GM-CSF 和 IL-6 的升高。CN016 抑制 Paclitaxel (HY-B0015) 诱导的炎症反应和免疫细胞向感觉神经元的浸润。CN016 保护神经元免受 Paclitaxel (HY-B0015) 诱导的神经毒性损伤。CN016 保护小鼠免受 Oxaliplatin 诱导的周围神经病变。

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CN016

CN016 Chemical Structure

CAS No. : 2902706-25-4

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CN016 相关抗体

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  • 生物活性

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生物活性

CN016 is a neuroprotective agent. CN016 inhibits the elevation of pro-inflammatory cytokines G-CSF, GM-CSF and IL-6 induced by Oxaliplatin (HY-17371). CN016 suppresses Paclitaxel (HY-B0015)-induced inflammatory responses and immune cell infiltration into sensory neurons. CN016 protects neurons from Paclitaxel (HY-B0015)-induced neurotoxic damage. CN016 protects mice against Oxaliplatin-induced peripheral neuropathy[1][2].

IC50 & Target[1]

IL-6

 

体外研究
(In Vitro)

CN016 (10-1000 nM) 可显著保护小鼠原代 DRG 神经元免受 Paclitaxel (HY-B0015) 诱导的神经毒性损伤[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CN016 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Clearance (CL) Vss AUC0-24
Mice[1] 5 mg/kg i.v. 12.8 ± 3.4 h 12.8 ± 2.9 mL/min/kg 0.8 ± 0.5 L/kg 6985 ± 1850 ng·h/mL
体内研究
(In Vivo)

CN016 (腹腔注射，剂量 5-20 mg/kg，在 4 次 Paclitaxel 隔日注射的每次注射前 1 h 给) 在 10 和 20 mg/kg 剂量下，可通过恢复感觉功能、保护神经结构和抑制神经炎症，显著缓解雌性 C57BL/6J 小鼠的紫杉醇诱导型周围神经病变[1]。
CN016 (20 mg/kg；腹腔注射；每次Oxaliplatin 注射前 1 h 给；持续 2 周) 可通过调控神经炎症通路、维持感觉神经元完整性并改善感觉功能终点指标，有效保护 BDNF Val/Val 小鼠免受 Oxaliplatin (HY-17371) 诱导的周围神经病变[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (7-week-old female; paclitaxel-induced peripheral neuropathy model)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.p.; 1 hour prior to each of 4 paclitaxel injections on alternate days
Result: Significantly alleviated paclitaxel-induced thermoanesthesia and mechanical allodynia at 10 and 20 mg/kg doses; moderately alleviated these symptoms at 5 mg/kg dose.
Rescued the reduced G-ratio in small sciatic nerve fibers (diameter <5 μm) caused by paclitaxel at 10 and 20 mg/kg doses.
Reduced the proportion of atypical axonal mitochondria by approximately 10-25% compared to paclitaxel-only treatment at 10 and 20 mg/kg doses.
Significantly restored the 25% myelinated fiber density loss caused by paclitaxel at 10 and 20 mg/kg doses, with 20 mg/kg showing the greatest recovery.
Significantly reduced paclitaxel-induced increases in plasma proinflammatory cytokines (GM-CSF, G-CSF, IFN-γ, IL-1α, IL-1β, TNF-α, IL-2, IL-3, IL-9) and chemokines (MCP-1, RANTES) at 10 and 20 mg/kg doses.
Diminished infiltration of M1 and M2 macrophages into DRG tissues at 10 and 20 mg/kg doses.
Suppressed activation of M1 microglia in DRG neurons at 10 and 20 mg/kg doses.
Animal Model: C57BL/6 background humanized BDNF Val/Val and Met/Met knockin mice (7-week-old; oxaliplatin-induced chemotherapy-induced peripheral neuropathy model)[2]
Dosage: 5 mg/kg; 20 mg/kg
Administration: i.p.; 1 hour before each oxaliplatin injection; 2 weeks
Result: Improved vibration sensitivity (P < 0.001), mechanical withdrawal thresholds (P < 0.001), and thermal withdrawal latency (P < 0.01) in oxaliplatin-treated BDNF Val/Val mice at 20 mg/kg.
Preserved Merkel cell density (P < 0.05) and intraepidermal nerve fiber (IENF) density (P < 0.001) in oxaliplatin-treated BDNF Val/Val mice at 20 mg/kg.
Prevented axonal degeneration and maintained normal myelin integrity in both Aβ (P < 0.01) and Aδ fibers (P < 0.01) in sciatic nerves from oxaliplatin-treated BDNF Val/Val mice at 20 mg/kg.
Modulated macrophage activation and suppressed oxaliplatin-induced elevations in proinflammatory cytokines G-CSF, GM-CSF, and IL-6 at 20 mg/kg.
分子量

525.54

Formula

C21H36N9O5P
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CN016 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CN0162902706-25-4CN 016CN-016Interleukin RelatedILAβ fibersMerkel cellsM1 phenotypesintraepidermal nerve fibersM2 phenotypesAδ fibersBDNF Val/Val micesensory neuronsproinflammatory cytokinesmacrophage activationInhibitorinhibitorinhibit

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目录号：
HY-181998
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