Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
HDAC6 0.019 μM (IC50) HDAC3 1.03 μM (IC50) HDAC1 1.53 μM (IC50) HDAC2 2.06 μM (IC50)
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ln Vitro |
Compared to class I HDACs, HDAC6-IN-13 (Compound 35m) (0.1–1 μM; 24 h) exhibits a significant degree of selectivity for HDAC6[1]. HDAC6-IN-13 demonstrates fast-on qualities for HDAC1, 2, and 3, while it is a slow-on and slow-off tight-binding HDAC6 inhibitor[1]. In vitro, HDAC6-IN-13 (5–20 μM; 8 h) has anti-inflammatory activity[1].
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ln Vivo |
HDAC6-IN-13 (Compound 35m) (20 mg/kg; po and ip; once) inhibits LPS-induced inflammation in mice in a remarkable way[1]. In mice, HDAC6-IN-13 (20 mg/kg; po; once) exhibits a notable BBB permeability and a very high oral bioavailability (F% = 93.4%)[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: MV4−11 and J774A.1 Tested Concentrations: 0.1, 0.2, 0.5 and 1 μM Incubation Duration: 24 h Experimental Results: Concentration-related accumulation of acetylated tubulin (Ac-Tubulin) was observed, while upregulation of acetylated histone H3 (AcHH3) and acetylated histone H4 (AcHH4) was not apparent even at the concentration of 1 μM. Western Blot Analysis[1] Cell Types: J774A.1 cells Tested Concentrations: 5, 10 and 20 μM Incubation Duration: 8 h Experimental Results: Inhibited the cleavage of pro-caspase 1 to p20 in a dose-dependent manner, inhibited the interaction between HDAC6 and dynein. |
Animal Protocol |
Animal/Disease Models: Male C57BL/6 WT mice, LPS-induced endotoxic shock model[1]
Doses: 20 mg/kg Route of Administration: PO and IP, immediately after the LPS injection Experimental Results: Dramatically diminished the serum IL-1β levels in LPS-induced mice via both ip and po administration. Animal/Disease Models: Male CD-1 mice[1] Doses: 5 mg/kg or 20 mg/kg Route of Administration: IV (5 mg/kg) or PO (20 mg/kg) (pharmacokinetic/PK Study) Experimental Results: pharmacokinetic/PKs Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral Administrationa[1] PK parameters HDAC6- IN-13 HDAC6-IN-13 administered dose (mg/kg) iv at 5 mg/kg oral at 20 mg/kg Cmax (ng/mL) 4604 ± 551 5570 ± 551 t1/2 (h) 7.95 ± 0.370 6.80 ± 0.145 AUC0−inf (ng·h/mL) 2755 ± 395 10292 ± 1385 F% n/a 93.4 ± 12.6 aHDAC6-IN-13 was administered via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calcula |
References |
[1]. Yue K, et al. First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation. J Med Chem. 2022 Sep 8.
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Molecular Formula |
C23H22N4O
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Molecular Weight |
370.45
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CAS # |
2837128-41-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6994 mL | 13.4971 mL | 26.9942 mL | |
5 mM | 0.5399 mL | 2.6994 mL | 5.3988 mL | |
10 mM | 0.2699 mL | 1.3497 mL | 2.6994 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.