ACY-1083
Based on 1 publication(s) in Google Scholar
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.54%
- CAS. Nr.: 1708113-43-2
- Formel: C17H18F2N4O2
- Molecular Weight:348.35
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Speicherung:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Publications Citing Use of MedChemExpress (MCE) ACY-1083
More
Biologische Aktivität
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HDAC6 3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| THP-1 | IC50 |
94 μM
Compound: 1
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Cytotoxicity against human THP-1 cells assessed as reduction in cell viability by alamar blue staining based assay
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability by alamar blue staining based assay
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[PMID: 37797307] |
Treatment with ACY-1083 (30 and 300 nM) significantly improves cell viability in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse hippocampal (HT22) cells
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Concentration:30 and 300 nM
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Incubation Time:
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Result:Significant improvement in cell viability.
ACY-1083 (oral doses of 3 mg/kg ACY-1083 for 7 days) reverses Paclitaxel-induced mechanical allodynia in adult male SD rats.
Mice dosed with 5 mg/kg ACY-1083 by intraperitoneal (i.p.) injection have a maximum plasma concentration (Cmax) of 936 ng/mL, a half-life (T1/2) of 3.5 hours, and a biologically active plasma exposure of 8 hours after dosing.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male C57BL/6J mice of 8-10 weeks of age[1]
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Dosage:3 or 10 mg/kg
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Administration:Administered i.p. injection; daily; for 7 days
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Result:The 10 mg/kg relieved Cisplatin (2.3 mg/kg)-induced mechanical allodynia, whereas the 3 mg/kg dose did not.
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Animal Model:Adult male Sprague Dawley rats[1]
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Dosage:3 mg/kg
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Administration:Two daily doses were given orally for 7 days.
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Result:Reversed Paclitaxel (6 mg/kg or 12 mg/kg)-induced mechanical allodynia.
Chemical Information
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CAS. Nr. 1708113-43-2
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Appearance Solid
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Molecular Weight 348.35
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Formel C17H18F2N4O2
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Color White to off-white
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SMILES
FC(CC1)(F)CCC1(NC2=NC=C(C(NO)=O)C=N2)C3=CC=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (287.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (14.35 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (14.35 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Krukowski K, et al. HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy. Pain. 2017 Jun;158(6):1126-1137. [Content Brief]
[2]. Vahagn C Nikolian, et al. Isoform 6-selective histone deacetylase inhibition reduces lesion size and brain swelling following traumatic brain injury and hemorrhagic shock. J Trauma Acute Care Surg. 2019 Feb;86(2):232-239. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8707 mL | 14.3534 mL | 28.7068 mL | 71.7669 mL |
| 5 mM | 0.5741 mL | 2.8707 mL | 5.7414 mL | 14.3534 mL | |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8707 mL | 7.1767 mL | |
| 15 mM | 0.1914 mL | 0.9569 mL | 1.9138 mL | 4.7845 mL | |
| 20 mM | 0.1435 mL | 0.7177 mL | 1.4353 mL | 3.5883 mL | |
| 25 mM | 0.1148 mL | 0.5741 mL | 1.1483 mL | 2.8707 mL | |
| 30 mM | 0.0957 mL | 0.4784 mL | 0.9569 mL | 2.3922 mL | |
| 40 mM | 0.0718 mL | 0.3588 mL | 0.7177 mL | 1.7942 mL | |
| 50 mM | 0.0574 mL | 0.2871 mL | 0.5741 mL | 1.4353 mL | |
| 60 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1961 mL | |
| 80 mM | 0.0359 mL | 0.1794 mL | 0.3588 mL | 0.8971 mL | |
| 100 mM | 0.0287 mL | 0.1435 mL | 0.2871 mL | 0.7177 mL |
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