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| Targets |
NCGC607 targets glucocerebrosidase (GCase), a lysosomal enzyme that catalyzes the hydrolysis of glucocerebroside to glucose and ceramide. It acts as a noninhibitory chaperone, binding to mutant GCase and facilitating proper protein folding and trafficking to the lysosome. This restores GCase activity and protein levels without inhibiting enzyme function. The compound also reduces α-synuclein levels, linking GCase dysfunction to Parkinson's disease pathology.
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| ln Vitro |
In vitro, NCGC607 successfully assists mutant enzyme, restoring glucocerebrosidase activity and protein levels in cellular models. It reduces glycolipid storage in both iPSC-derived macrophages and dopaminergic neurons. The compound increases GCase activity and decreases glycolipid levels in cell-based assays. It shows potential for treating neuronopathic Gaucher disease. Detailed in vitro data are available in the primary literature.
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| ln Vivo |
In vivo, NCGC607 has demonstrated efficacy in preclinical models of Gaucher disease. It reduces glycolipid storage and improves GCase activity in vivo. The compound shows potential for treating neuronopathic Gaucher disease. Its ability to reduce α-synuclein levels suggests possible application in Parkinson's disease research. Further in vivo studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro GCase activity assays for NCGC607 typically use recombinant GCase enzyme or cell lysates with fluorogenic substrate (4-methylumbelliferyl-β-D-glucopyranoside). The compound is dissolved in DMSO and diluted in assay buffer (0.1 M citrate-phosphate buffer, pH 5.5, 0.1% Triton X-100). Reactions are incubated at 37°C for 60 minutes and terminated by adding glycine-NaOH buffer (pH 10.5). Fluorescence (excitation 365 nm, emission 445 nm) is measured. Chaperone activity is assessed by measuring increased GCase activity in mutant GCase-expressing cells. IC₅₀ and EC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
For cell-based assays, iPSC-derived macrophages and dopaminergic neurons are cultured in appropriate media. Cells are seeded in multi-well plates and treated with NCGC607 at various concentrations (0.1-100 μM) for 24-72 hours. GCase activity is measured using fluorogenic substrate in cell lysates. Glycolipid levels are quantified by mass spectrometry or thin-layer chromatography. α-Synuclein levels are assessed by Western blotting or ELISA. Cell viability is assessed by standard assays. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, NCGC607 is typically administered to rodent models of Gaucher disease or Parkinson's disease via intraperitoneal (IP) or oral routes. Dosing regimens may involve daily administration at various concentrations for 1-4 weeks. Endpoints include GCase activity measurement in brain and peripheral tissues, glycolipid quantification, and α-synuclein level assessment. Behavioral tests may be performed in Parkinson's disease models. Tissue collection and analysis are conducted at specified time points post-treatment. All procedures follow institutional animal care guidelines.
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| ADME/Pharmacokinetics |
NCGC607 (MW 543.35, C₂₄H₂₂IN₃O₄) is soluble in DMSO and has a purity of ≥98% by HPLC. The compound is a salicylic acid derivative with an iodine substituent. Detailed pharmacokinetic parameters (bioavailability, half-life, clearance) are not extensively reported in publicly available sources. The compound is typically stored at 2-8°C. Further ADME studies are needed to fully characterize its pharmacokinetic profile.
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| Toxicity/Toxicokinetics |
NCGC607 is a research-grade compound and is not a therapeutic agent. It is for research use only and not intended for human therapeutic applications. The compound has shown promising results in preclinical models of Gaucher disease and Parkinson's disease. Standard safety pharmacology and toxicology studies would be required for therapeutic development. The compound should be handled with standard laboratory safety precautions.
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| References | |
| Additional Infomation |
A molecular chaperone for glucocerebroside lipase; structure described in the first article.
NCGC607 is a research-grade chemical probe for studying glucocerebrosidase (GCase) function in Gaucher disease and Parkinson's disease. Its primary applications include lysosomal storage disorder research, neurodegenerative disease research, and drug discovery. The compound is not approved for clinical use and has not entered clinical trials. It is commercially available from various chemical suppliers for research purposes only. Its mechanism involves chaperone-mediated restoration of mutant GCase activity and reduction of α-synuclein levels. |
| Molecular Formula |
C24H22IN3O4
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|---|---|
| Molecular Weight |
543.36
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| Exact Mass |
543.065
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| CAS # |
1462267-07-7
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| PubChem CID |
46943210
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
734.5±60.0 °C at 760 mmHg
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| Flash Point |
398.0±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.679
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
633
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C1=CC=CC=C1)C(=O)CNC(=O)C2=CC=CC=C2OCC(=O)NC3=CC=C(C=C3)I
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| InChi Key |
HFVDMJQQAKLUSN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H22IN3O4/c1-28(19-7-3-2-4-8-19)23(30)15-26-24(31)20-9-5-6-10-21(20)32-16-22(29)27-18-13-11-17(25)12-14-18/h2-14H,15-16H2,1H3,(H,26,31)(H,27,29)
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| Chemical Name |
2-[2-(4-iodoanilino)-2-oxoethoxy]-N-[2-(N-methylanilino)-2-oxoethyl]benzamide
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| Synonyms |
NCGC-607; NCGC 607; NCGC607
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~62.5 mg/mL (~115.03 mM)
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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 | 1.8404 mL | 9.2020 mL | 18.4040 mL | |
| 5 mM | 0.3681 mL | 1.8404 mL | 3.6808 mL | |
| 10 mM | 0.1840 mL | 0.9202 mL | 1.8404 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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