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 No.: 3118852-74-4
- Formule: C21H23N3O4
- Masse moléculaire:381.43
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
HDAC6 8.5 nM (IC50) |
IL-6 |
iNOS |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
In Vivo
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 No. 3118852-74-4
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Masse moléculaire 381.43
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Formule 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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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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC6-IN-80 Related Classifications
HY-182777 Related Classifications
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