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| 5mg |
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| 25mg |
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Purity: ≥98%
RG-2833 (formerly RGFP-109) is a potent, selective and brain-permeable inhibitor of HDAC (histone deacetylase) with potential neuroprotective effects. In cell-free assays, it inhibits HDAC1 and HDAC3 with IC50s of 60 nM and 50 nM, respectively. An experimental medication candidate called RG2833 is being researched to treat Parkinson's disease. It is being studied in phase I clinical trials after being granted orphan drug status. In an iPSC-derived neuronal cell model, FXN was upregulated and maximal deacetylase was inhibited by plasma RG2833 (5μM). The findings demonstrated a strong correlation between the downregulation of deacetylase activity and the increase in FXN (Friedreich Ataxia) transcript, indicating that deacetylation is the mechanism of action of RG2833.
| Targets |
HDAC3 ( IC50 = 50 nM ); HDAC1 ( IC50 = 60 nM ); HDAC1 ( Ki = 32 nM ); HDAC3 ( Ki = 5 nM )
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| ln Vitro |
In vitro activity: RG2833's Ki values for HDAC1 and HDAC3 are 32 nM and 5 nM, in that order. RG2833 demonstrates high activity throughout the entire tested concentration range of 1 to 10 µM. Frataxin protein increases more slowly in cells from patient P13 when RG2833 is continuously cultivated, but it increases quickly in the cells after the compound is removed[1]. In addition to reducing neuronal pathology of the dorsal root ganglia (DRG), RG2833 causes notable increases in brain aconitase enzyme activity[2]. |
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| ln Vivo |
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| Enzyme Assay |
Aconitase activities are measured by centrifuging mouse brain tissues at 800×g for 10 min at 4°C after homogenizing them on ice at 10% w/v in CellLytic MT Mammalian Tissue Lysis/Extraction buffer. After adding 50 μL of tissue lysates to 200 μL of substrate mix (which included 50 mM Tris/HCl pH7.4, 0.4 mM NADP, 5 mM Na citrate, 0.6 mM MgCl2, 0.1% (v/v) Triton X-100, and 1U isocitrate dehydrogenase), the reactions were incubated for 15 minutes at 37°C.The reaction slope was then determined by taking spectrophotometric absorbance measurements every minute for 15 minutes at 340 nm 37°C. Afterwards, using a citrate synthase assay kit, the aconitase activities of mouse brain tissues are normalized to citrate synthase activities.
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| Cell Assay |
RG2833's Ki values for HDAC1 and HDAC3 are 5.4 nM and 7.8 nM, in that order. RG2833 demonstrates high activity throughout the entire tested concentration range of 1 to 10 µM. Frataxin protein increases more slowly in cells from patient P13 when RG2833 is continuously cultivated; however, upon removal of the compound, frataxin protein levels rose quickly. In addition to reducing neuronal pathology in the dorsal root ganglia (DRG), RG2833 causes notable increases in brain aconitase enzyme activity.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C20H25N3O2
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| Molecular Weight |
339.43
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| Exact Mass |
339.195
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| Elemental Analysis |
C, 70.77; H, 7.42; N, 12.38; O, 9.43
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| CAS # |
1215493-56-3
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| Related CAS # |
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| PubChem CID |
56654642
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| Appearance |
White to off-white solid powder
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| LogP |
5.127
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1[H])=O)N([H])C1=C([H])C([H])=C([H])C([H])=C1N([H])[H]
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| InChi Key |
VOPDXHFYDJAYNS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25N3O2/c1-15-10-12-16(13-11-15)20(25)22-14-6-2-3-9-19(24)23-18-8-5-4-7-17(18)21/h4-5,7-8,10-13H,2-3,6,9,14,21H2,1H3,(H,22,25)(H,23,24)
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| Chemical Name |
N-[6-(2-aminoanilino)-6-oxohexyl]-4-methylbenzamide
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| Synonyms |
RGFP 109; RGFP-109; RGFP109; RG2833; RG 2833; RG-2833
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 5%DMSO Corn oil: 6.0mg/ml (17.68mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9461 mL | 14.7306 mL | 29.4612 mL | |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL | |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 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.
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