CN016
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.
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- CAS No.: 2902706-25-4
- Formule: C21H36N9O5P
- Masse moléculaire:525.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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IL-6 |
CN016 (10-1000 nM) significantly protects mouse primary DRG neurons against Paclitaxel (HY-B0015)-induced neurotoxic injury[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 |
CN016 (20 mg/kg; intraperitoneal injection; administered 1 h prior to each Oxaliplatin injection for 2 consecutive weeks) effectively protects BDNF Val/Val mice against Oxaliplatin (HY-17371)-induced peripheral neuropathy by regulating neuroinflammatory pathways, preserving sensory neuron integrity and improving sensory functional endpoints[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (7-week-old female; paclitaxel-induced peripheral neuropathy model)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; 1 hour prior to each of 4 paclitaxel injections on alternate days
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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.
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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]
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Dosage:5 mg/kg; 20 mg/kg
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Administration:i.p.; 1 hour before each oxaliplatin injection; 2 weeks
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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.
Chemical Information
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CAS No. 2902706-25-4
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Masse moléculaire 525.54
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Formule C21H36N9O5P
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SMILES
OCCCN1N=NC(CNC2=NC(N3CCOCC3)=CC(NC4CCN(CC4)CCP(O)(O)=O)=N2)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Chen YF, et al. Discovery of Potential Neuroprotective Agents against Paclitaxel-Induced Peripheral Neuropathy. J Med Chem. 2022;65(6):4767-4782. [Content Brief]
[2]. Chen LH, et al. BDNF Val66Met protects oxaliplatin-induced peripheral neuropathy in patients with colorectal cancer. Sci Transl Med. 2026;18(837):eadx1436. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CN016 Related Classifications
HY-181998 Related Classifications
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