sEH/HDAC6-IN-1
sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC50s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects.
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- No. CAS: 2847838-67-7
- Fòrmula: C27H40N4O4
- Peso molecular:484.63
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
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murine sEH 0.72 nM (IC50) |
human sEH 2 nM (IC50) |
HDAC6 5 nM (IC50) |
HDAC1 0.2731 μM (IC50) |
HDAC2 0.8 μM (IC50) |
HDAC3 0.49 μM (IC50) |
HDAC11 0.3142 μM (IC50) |
sEH/HDAC6-IN-1 (1-2 μM, 24 h) inhibits cell growth of THP-1 with IC50 of 3.2 μM[1].
sEH/HDAC6-IN-1 (100 μM) reveals microsomal stability in human, rat and mouse liver microsomes, with half-times of 4.07, 1.76 and 1.39 h[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
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Concentration:1-2 μM
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Incubation Time:24 h
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Result:Increased the levels of acetylated α-tubulin
sEH/HDAC6-IN-1 (p.o., 100 mg/kg, 7 days) reveals analgesic effects in SNI mice[1].
sEH/HDAC6-IN-1 (5 mg/kg, i.p., 4-12 h) inhibits LPS induced inflammation and the release of IL-6, TNF-α and MCP-5 in C57BL/6 mice[1].
sEH/HDAC6-IN-1 (i.v.:10 mg/kg, p.o.:100 mg/kg) reveals a pharmacokinetics profils in SD rats[1]:
Pharmacokinetic Analysis of sEH/HDAC6-IN-1 in SD rats[1]
| route | Dose (mg/kg) | Tmax (h) | Cmax (μM) | T1/2 (h) | CL (L/h/kg) | VZ (L/kg) | AUC0-8 (μM·h) | AUC0-∞ (μM·h) | F (%) |
| iv | 10 | 0.03 | 261.20 | 1.58 | 0.21 | 0.43 | 36.76 | 38.10 | 10.82 |
| po | 100 | 0.50 | 13.09 | 1.31 | 1.80 | 3.43 | 19.89 | 22.85 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:alleviating spared nerve injury (SNI)-induced neuropathic pain in C57BL/6 mice[1]
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Dosage:100 mg/kg
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Administration:oral administration for 7 days
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Result:decreased PWT values.
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Animal Model:LPS induced acute inflammation in C57BL/6 mice[1]
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Dosage:5 mg/kg
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Administration:i.p., 4-12 h
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Result:Survived 66.7% mice at 28 h, 44.44% mice at 35 h, 22.22% mice at 72 h.
Chemical Information
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No. CAS 2847838-67-7
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Peso molecular 484.63
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Fòrmula C27H40N4O4
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SMILES
O=C(NC(C=C1)=CC=C1C(NCCCCCCC(NO)=O)=O)N[C@@](C[C@]2(C3)C)(C[C@H]3C4)C[C@]4(C2)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
sEH/HDAC6-IN-1 Related Classifications
HY-163207 Related Classifications
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