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ACY-775

Cat. No. M10079
ACY-775 Structure
Synonym:

ACY775

Size Price Availability Quantity
10mg USD 190  USD190 In stock
25mg USD 395  USD395 In stock
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Quality Control & Documentation
Biological Activity

ACY-775 is a potent and selective HDAC6 inhbiitor with IC50 of 7.5 nM. ACY-775 inhibits HDAC6 with low nanomolar potency and a selectivity of 60- to 1500-fold over class I HDACs. ACY-775 shares the antidepressant-like properties of other HDAC inhibitors, such as SAHA and MS-275. ACY-775 (50 mg/kg) administered repeatedly in wild-type mice at 24 h, 4 h, and 30 min before killing significant increases in α-tubulin acetylation are observed in all tested brain regions.

Chemical Information
Molecular Weight 330.36
Formula C17H19FN4O2
CAS Number 1375466-18-4
Solubility (25°C) DMSO ≥ 89 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Veronick Benoy, et al. Neurotherapeutics. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease

[2] Jeanine Jochems, et al. Neuropsychopharmacology. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability

[3] Sridurga Mithraprabhu, et al. Br J Haematol. Histone deacetylase (HDAC) inhibitors as single agents induce multiple myeloma cell death principally through the inhibition of class I HDAC

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Keywords: ACY-775, ACY775 supplier, HDAC, inhibitors, activators


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