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
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
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) |
In Vitro
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. Further protocols information, click here.
-
Cell Line:THP-1 cells
-
Concentration:1 μM, 2 μM
-
Incubation Time:24 h
-
Result:Induced acetylation of α-tubulin and histone H3.
In Vivo
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.
-
Animal Model:Kunming mice (male, weighing 20-22 g) injected with 5% Formalin solution[1].
-
Dosage:30 mg/kg
-
Administration:ip; once
-
Result:Exhibited an effective analgesic activity.
Chemical Information
-
CAS No. 3009011-58-6
-
Molecular Weight 580.02
-
Formula C27H32ClF2N5O5
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
sEH/HDAC6-IN-2 Related Classifications
HY-159171 Related Classifications
Powered by Bioz