2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Epigenetics
  3. Epoxide Hydrolase HDAC
  4. 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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sEH/HDAC6-IN-1 Chemical Structure

sEH/HDAC6-IN-1 Chemical Structure

CAS No. : 2847838-67-7

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sEH/HDAC6-IN-1 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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[1].

IC50 & Target

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)

In Vitro

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.

sEH/HDAC6-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: THP-1
Concentration: 1-2 μM
Incubation Time: 24 h
Result: Increased the levels of acetylated α-tubulin
In Vivo

sEH/HDAC6-IN-1 reveals a plasma protein binding (PBB) percentage of 81.40% in SD rats[1].
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.

Animal Model: alleviating spared nerve injury (SNI)-induced neuropathic pain in C57BL/6 mice[1]
Dosage: 100 mg/kg
Administration: oral administration for 7 days
Result: decreased PWT values.
Animal Model: LPS induced acute inflammation in C57BL/6 mice[1]
Dosage: 5 mg/kg
Administration: i.p., 4-12 h
Result: Survived 66.7% mice at 28 h, 44.44% mice at 35 h, 22.22% mice at 72 h.
Molecular Weight

484.63

Formula

C27H40N4O4
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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sEH/HDAC6-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

sEH/HDAC6-IN-12847838-67-7Epoxide HydrolaseHDACHistone deacetylasesanalgesicanti-neuropathicanti-inflammatory,THP-1SD ratsC57BL/6 miceSNI miceInhibitorinhibitorinhibit

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