| CAS NO: | 1375465-91-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 270.29 |
|---|---|
| Formula | C14H14N4O2 |
| CAS No. | 1375465-91-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 32 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: | |
| SMILES Code | O=C(C1=CN=C(NC2(C3=CC=CC=C3)CC2)N=C1)NO |
| Synonyms | ACY738; ACY 738; ACY-738 |
| In Vitro | In vitro activity: ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228 Kinase Assay: ACY-738 is a novel, potent, selective, brain penetrable and orally-bioavailable HDAC6 inhibitor with an IC50s of 1.7 nM; it also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM. Cell Assay: ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells. |
|---|---|
| In Vivo | ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation, but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels.ACY-738 (5 mg/kg) leads to significant increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50 mg/kg) fails to produce an enhancement of locomotor activity in WT mice tested in a home cage environment |
| Animal model | Mice |
| Formulation & Dosage | 5, 20, 50 mg/kg; i.p. and p.o. |
| References | Neuropsychopharmacology. 2014 Jan;39(2):389-400.Br J Haematol. 2013 Aug;162(4):559-62.Clin Immunol. 2016 Jan;162:58-73. |
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