ACY-775

ACY-775
Cat. No. : CS-7689 CAS No. : 1375466-18-4
M. Wt. : 330.36
Size Stock Price Quantity Add to Cart Quotation Online
2mg In-stock $90.0
5mg In-stock $120.0
10mg In-stock $190.0
25mg In-stock $290.0
50mg In-stock $490.0
100mg In-stock $690.0
Products are for research use only. Not for human use. We do not sell to patients.

Bulk Inquiry

Collapse
Your information is safe with us. * Required Fields
  Salutation:
  • Dr.
  • Prof.
  • Mr.
  • Ms.
  • Mrs.
  • Miss.
* Country:
  • United States
  • Canada
  • United Kingdom
  • Australia
  • China
  • Germany
  • France
  • Japan
  • Korea South
  • Switzerland
  • ----------------------------------
  • Albania
  • Algeria
  • Argentina
  • Armenia
  • Australia
  • Austria
  • Azerbaijan
  • Bahrain
  • Bangladesh
  • Barbados
  • Belarus
  • Belgium
  • Bolivia
  • Bosnia Herzegovina
  • Brazil
  • Bulgaria
  • Cameroon
  • Canada
  • Chile
  • China
  • Colombia
  • Croatia
  • Cyprus
  • Czech Republic
  • Denmark
  • Ecuador
  • Egypt
  • Estonia
  • Fiji
  • Finland
  • France
  • Georgia
  • Germany
  • Gibraltar
  • Greece
  • Hong Kong
  • Hungary
  • Iceland
  • India
  • Indonesia
  • Iran
  • Iraq
  • Ireland
  • Israel
  • Italy
  • Japan
  • Jordan
  • Kazakhstan
  • Kenya
  • Korea South
  • Kuwait
  • Latvia
  • Lebanon
  • Libya
  • Lithuania
  • Luxembourg
  • Macedonia
  • Malaysia
  • Malta
  • Mexico
  • Moldova
  • Monaco
  • Mongolia
  • Montenegro
  • Morocco
  • Nepal
  • Netherlands
  • New Zealand
  • Nigeria
  • Norway
  • Oman
  • Pakistan
  • Paraguay
  • Peru
  • Philippines
  • Poland
  • Portugal
  • Puerto Rico
  • Qatar
  • Republic of Benin
  • Romania
  • Russia
  • Saudi Arabia
  • Serbia
  • Singapore
  • Slovakia
  • Slovenia
  • South Africa
  • Spain
  • Sri Lanka
  • Suriname
  • Sweden
  • Switzerland
  • Syria
  • Taiwan
  • Thailand
  • Tunisia
  • Turkey
  • Ukraine
  • United Arab Emirates
  • United Kingdom
  • United States
  • Uruguay
  • Uzbekistan
  • Venezuela
  • Vietnam
  • Zambia
  • Zimbabwe
  • Other Countries
* Applicant name:
* Organization Name:
* Email address:
* Requested quantity:
  • g
  • kg
  • t
  • mL
  • L
* Phone number:
  Remarks:
 
Name, 
Organization Name, 
Email address, 
Requested quantity, 
Phone number, 
  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: ACY-775; 
Cat. No. : CS-7689
CAS No. : 1375466-18-4
Formula: C17H19FN4O2
M. Wt. : 330.36
Solubility: DMSO: 100 mg/mL

Activity:

ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6), with IC50 of 7.5 nM. IC50 & Target: IC50: 7.5 nM (HDAC6)[1] In Vitro: The HDAC6 inhibitors, ACY-775, hyperacetylate α-tubulin at a concentration of 1 μM. The histone acetylation is not affected. In vehicle-treated cells, α-tubulin is mainly present in the deacetylated form, while histone 3 is clearly acetylated. Upon treatment with ACY-775, a clear enhancement of the acetylation of α-tubulin is visible, while histone acetylation remained unaltered. Acetylation of α-tubulin is visualized by immunofluorescence and the intensity in the neurites of the neurons is quantified and normalized to the length of the fluorescent signal. In vehicle-treated DRG neurons, acetylated α-tubulin is already present. Upon treatment with ACY-775 the signal intensity of acetylated α-tubulin increase significantly. DRG neurons treat with vehicle ACY-775. Significant increase motility of mitochondria and also the total number of mitochondria within the neurites is observed compared with vehicle-treated DRG neurons. Interestingly, a significantly higher number of retrogradely transport mitochondria is observed in DRG neurons treated with ACY-775 compared with vehicle-treated cells[1]. In Vivo: In vivo biodistribution profiles of ACY-738, ACY-775, and tubastatin A are examined after acute dosing at 5 or 50 mg/kg over 2 h. At t=30 min after acute 50 mg/kg injection, respective plasma levels of ACY-738 and ACY-775 are 515 ng/ml (1.9 μM) and 1359 ng/ml (4.1 μM). Elimination from plasma is rapid, with plasmatic half-life of 12 min and concentration below 10 ng/ml after 2 h. Nevertheless, areas under concentration time curves for brain and plasma(AUCBrain/AUCPlasma) calculate over 2 h for both ACY-738 and ACY-775 lead to ratios >1. Taken together, these results suggest that despite their short half-life, ACY-738 and ACY-775 rapidly distribute to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues. When ACY-738 (5 mg/kg) or ACY-775 (50 mg/kg) are 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: cortex, F2, 7=582.5, P<0.0001; hippocampus, F2, 7=260.4, P<0.0001; DRN, F2, 7=54.00,P<0.0001; and cerebellum, F2, 7=136.2, P<0.0001[2].

Protocol:

Cell Assay: [2]Undifferentiated RN46A-B14 cells, a line of immortalized rat raphe neuronal precursors, are grown as previously described. They are treated with 2.5 μM ACY-738, ACY-775, tubastatin A, or 0.6 μM TSA, or vehicle (0.1% DMSO) for 4 h. Samples are processed using histone extraction kit and quantified using protein assay. Animal Administration: [2]Mice are tested for immobility in the TST using a rig from Med-Associates. At 30 min or 2 h after i.p. injection of ACY-738 (5, 50 mg/kg), ACY-775 (5, 50 mg/kg), and citalopram (0.5, 2, 20 mg/kg), a combination of the previous, or vehicle, mice are attached to the test rig and time immobile over 6 min is recorded. For open-field activity mice were injected with ACY-738 or ACY-775 at 5, 10, or 50 mg/kg or vehicle and allowed to explore. Activity was recorded using the Photobeam Activity System[2].

References:

Jeanine Jochems et al. Antidepressant-Like Properties of Novel HDAC6-Selective Inhibitors with Improved Brain Bioavailability. Neuropsychopharmacology. 2014 Jan; 39(2): 389–400. doi: 10.1038/npp.2013.207

Veronick Benoy, et al. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot–Marie–Tooth Disease. Neurotherapeutics. 2017 Apr; 14(2): 417–428. doi: 10.1007/s13311-016-0501-z

  • Select Batch :
Browsing History
Tags:ACY-775 supplier,ACY-775 purchase,ACY-775 manufacturer,ACY-775 sigma,ACY-775 distributor,cost,ACY-775 buy,ACY-775 for sale
Please enter your email address
Organization name: Email:

Submit success