HDAC6-IN-80
HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy.
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- CAS. Nr.: 3118852-74-4
- Formel: C21H23N3O4
- Molecular Weight:381.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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HDAC6 8.5 nM (IC50) |
IL-6 |
iNOS |
HDAC6-IN-80 (Compound 36) (1-10 μg/mL; 6.5-24.5 h) inhibits LPS-induced inflammatory responses in BV2 microglial cells by reducing nitrite levels and the mRNA and protein expression of proinflammatory mediators (iNOS, COX-2, TNF-α, IL-6), and does not affect cell viability at concentrations up to 10 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HDAC6-IN-80 (15-60 mg/kg; p.o.; single administration) dose-dependently alleviates Paclitaxel (HY-B0015)-induced neuropathic pain in mice, with an ED50 of 37.89 mg/kg[1].
HDAC6-IN-80 (15-60 mg/kg; p.o.; single administration) exerts only extremely weak effects on motor coordination in mice at doses up to 30 mg/kg, and causes significant impairment only at the 60 mg/kg dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (male, 20-32 g)[1]
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Dosage:15 mg/kg; 30 mg/kg; 60 mg/kg
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Administration:p.o.; single dose
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Result:Produced a maximum possible effect (MPE) of 45.84% at 30 mg/kg.
Dose-dependently increased mechanical paw withdrawal thresholds (MWTs) across all tested doses.
Significantly elevated the area under the curve (AUC) of MWTs in a dose-related manner.
Achieved an ED50 value of 35.66 mg/kg for alleviating carrageenan-induced allodynia.
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Animal Model:ICR (male, 20-32 g)[1]
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Dosage:15 mg/kg; 30 mg/kg; 60 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently increased mechanical withdrawal thresholds (MWTs) in paclitaxel-treated mice.
Achieved an ED50 value of 37.89 mg/kg for alleviating paclitaxel-induced mechanical allodynia.
Significantly elevated the area under the curve (AUC) of MWTs in a dose-related manner.
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Animal Model:ICR (male, 20-32 g)[1]
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Dosage:15 mg/kg; 30 mg/kg; 60 mg/kg
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Administration:p.o.; single dose
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Result:Did not induce statistically significant motor impairment at 15 and 30 mg/kg.
Significantly reduced rotarod latency at 30, 60, and 90 minutes post-administration at 60 mg/kg (p < 0.01 vs vehicle).
Chemical Information
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CAS. Nr. 3118852-74-4
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Molecular Weight 381.43
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Formel C21H23N3O4
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SMILES
ONC(CCCCCOC1=CC=C(C2=NC(C3=CC=C(C)C=C3)=NO2)C=C1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
HDAC6-IN-80 Related Classifications
HY-182777 Related Classifications
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