sEH/HDAC6-IN-2
sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain.
For research use only. We do not sell to patients.
- CAS No.: 3009011-58-6
- Formula: C27H32ClF2N5O5
- Molecular Weight:580.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC6 0.008 μM (IC50) |
Human sEh 0.0009 μM (IC50) |
Mouse sEh 0.0468 μM (IC50) |
HDAC8 0.062 μM (IC50) |
HDAC11 0.464 μM (IC50) |
HDAC2 0.492 μM (IC50) |
HDAC1 1.151 μM (IC50) |
HDAC3 1.276 μM (IC50) |
sEH/HDAC6-IN-2 has significant selectivity on the inhibitory activity of HDAC6 (selectivity Index: HDAC1/HDAC6 = 144, HDAC2/HDAC6 = 62, HDAC3/HDAC6 = 160, HDAC8/HDAC6 = 8, HDAC11/HDAC6 = 58)[1].
sEH/HDAC6-IN-2 (compound 28g; 1-2 μM; 24 h) induces an increase in acetylation of α-tubulin without affecting histone H3, indicating the selective inhibition of HDAC6[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:1 μM, 2 μM
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Incubation Time:24 h
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Result:Induced acetylation of α-tubulin and histone H3.
Pharmacokinetics of sEH/HDAC6-IN-2 in SD rats Following Intravenous and Oral Administration[1].
| parameter | iv (10 mg/kg) | ig (50 mg/kg) |
| Tmax (h) | 0.08 | 0.50 |
| Cmax (μM) | 7.87 | 6.63 |
| t1/2 (h) | 5.43 | 3.55 |
| CL (L/h) | 0.16 | 0.82 |
| Vz (L) | 1.28 | 4.20 |
| AUC0-12h (μM·h) | 12.29 | 15.01 |
| AUC0-∞ (μM·h) | 21.16 | 21.22 |
| F (%) | 24.42 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming mice (male, weighing 20-22 g) injected with 5% Formalin solution[1].
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Dosage:30 mg/kg
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Administration:ip; once
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Result:Exhibited an effective analgesic activity.
Chemical Information
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CAS No. 3009011-58-6
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Molecular Weight 580.02
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Formula C27H32ClF2N5O5
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SMILES
O=C([C@@H]1CN(C(C2=CC=C(NC(NC3=CC=C(Cl)C(F)=C3)=O)C(F)=C2)=O)CCC1)NCCCCCCC(NO)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
sEH/HDAC6-IN-2 Related Classifications
HY-159171 Related Classifications
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