| Size | Price | Stock | Qty |
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| Other Sizes |
| Targets |
NLG-1486 targets indoleamine 2,3-dioxygenase (IDO), an enzyme that catalyzes the rate-limiting step in the catabolism of tryptophan along the kynurenine pathway. IDO is a heme-containing enzyme that is induced by inflammatory cytokines such as IFN-gamma and plays a critical role in immune regulation. IDO-mediated tryptophan depletion and kynurenine production suppress T cell proliferation and promote immune tolerance, contributing to tumor immune escape. By inhibiting IDO with an IC50 of <1 microM, NLG-1486 restores tryptophan levels and reduces kynurenine production, thereby enhancing antitumor immune responses.
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| ln Vitro |
IDO-IN-6, also known as Compound 1486, is an inhibitor of indoleamine 2,3-dioxygenase (IDO) with an IC50 <1 μM, meaning that 50% of the enzyme activity concentration is inhibited by recombinant human IDO-IN-6 (International Data Organization) [1].
NLG-1486 demonstrates potent in vitro activity as an IDO inhibitor. The compound inhibits IDO with an IC50 of <1 microM. Its activity is concentration-dependent, with potent inhibition observed at nanomolar to micromolar concentrations. NLG-1486 has anticancer and immunomodulatory effects. The compound's ability to inhibit IDO activity has been characterized in enzymatic assays using recombinant IDO enzyme or cell-based assays measuring kynurenine production. NLG-1486 is extracted from patent WO WO2012142237A1, compound 1486. Its potency and selectivity for IDO make it a valuable tool for studying IDO biology and evaluating IDO inhibition as a therapeutic strategy for cancer immunotherapy. |
| ln Vivo |
In vivo, NLG-1486 has been studied for its potential to enhance antitumor immune responses. As an IDO inhibitor with an IC50 of <1 microM, the compound would be expected to restore tryptophan levels and reduce kynurenine production, thereby enhancing T cell proliferation and antitumor immunity. IDO inhibitors have been studied in various animal models of cancer, where they have demonstrated efficacy in enhancing antitumor immune responses and reducing tumor growth. NLG-1486's in vivo activity has been described in patent literature. The compound's immunomodulatory activity supports its potential for cancer immunotherapy research.
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| Enzyme Assay |
In vitro enzyme assays for NLG-1486 involve measuring the inhibition of IDO enzymatic activity. Recombinant human IDO is incubated with varying concentrations of the test compound, L-tryptophan, and appropriate cofactors (e.g., methylene blue, ascorbate, catalase). The production of kynurenine is quantified by measuring absorbance at 320 nm after deproteinization with trichloroacetic acid and reaction with Ehrlich's reagent. IC50 values are calculated by plotting percent inhibition against compound concentration using non-linear regression analysis. The compound has an IC50 of <1 microM. Each concentration is typically tested in duplicate or triplicate with appropriate positive controls (known IDO inhibitors) and vehicle controls.
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| Cell Assay |
In vitro cellular assays for NLG-1486 are performed using IDO-expressing cells, such as dendritic cells, macrophages, or cancer cells. Cells are stimulated with IFN-gamma to induce IDO expression and treated with varying concentrations of the compound. Kynurenine levels in the culture supernatant are measured by HPLC or by colorimetric assay after reaction with Ehrlich's reagent. Cell viability is assessed in parallel using standard viability assays such as MTT to ensure that observed effects are not due to cell death. The compound's ability to restore T cell proliferation in the presence of IDO-expressing cells can be assessed using T cell proliferation assays. IC50 values for inhibition of kynurenine production are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for NLG-1486 are conducted using mouse models of cancer. Immunocompetent mice are implanted with syngeneic tumor cells and treated with NLG-1486 via oral gavage or intraperitoneal injection at various doses and schedules. Tumor growth is measured using calipers. Immune cell infiltration into tumors is assessed by flow cytometry or immunohistochemistry. Tryptophan and kynurenine levels are measured in plasma and tumor tissues by LC-MS/MS. Cytokine levels are measured in serum and tumor tissues. Pharmacokinetic studies assess drug concentrations in plasma and tissues. Animals are monitored for clinical signs and body weight. Efficacy is expressed as tumor growth inhibition and immune activation compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NLG-1486 have been characterized in preclinical studies. The compound has a molecular formula of C18H21FN2O2 and a molecular weight of 316.37 g/mol. NLG-1486 is extracted from patent WO WO2012142237A1, compound 1486. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of cancer immunotherapy. Detailed pharmacokinetic data are available from research publications.
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| Toxicity/Toxicokinetics |
NLG-1486 is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As an IDO inhibitor that modulates immune function, the compound would be expected to have effects on immune regulation and could potentially cause immune-related adverse events. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has been conducted as part of preclinical development. The compound is not approved for human use and is strictly intended for research purposes.
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| References | |
| Additional Infomation |
NLG-1486 (IDO-IN-8) is a novel and potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of <1 microM. It is extracted from patent WO WO2012142237A1, compound 1486. NLG-1486 has anticancer and immunomodulatory effects. The compound has a molecular formula of C18H21FN2O2 and a molecular weight of 316.37 g/mol. NLG-1486 has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only.
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| Molecular Formula |
C18H21FN2O2
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|---|---|
| Molecular Weight |
316.369948148727
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| Exact Mass |
316.158
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| CAS # |
1402837-76-6
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| Related CAS # |
IDO-IN-5;1402837-79-9;Navoximod;1402837-78-8;IDO-IN-8;1402837-77-7
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| PubChem CID |
70914234
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
555.4±35.0 °C at 760 mmHg
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| Flash Point |
289.7±25.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.683
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| LogP |
1.28
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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 |
3
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| Heavy Atom Count |
23
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| Complexity |
416
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CC(CCC1[C@H](C[C@H]2C3=C(C=CC=C3F)C4=CN=CN24)O)O
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| InChi Key |
YGACXVRLDHEXKY-VDPJLGHJSA-N
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| InChi Code |
InChI=1S/C18H21FN2O2/c19-14-3-1-2-13-16-9-20-10-21(16)15(18(13)14)8-17(23)11-4-6-12(22)7-5-11/h1-3,9-12,15,17,22-23H,4-8H2/t11?,12?,15-,17-/m0/s1
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| Chemical Name |
4-[(1S)-2-[(5S)-6-fluoro-5H-imidazo[5,1-a]isoindol-5-yl]-1-hydroxyethyl]cyclohexan-1-ol
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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) |
DMSO : ~50 mg/mL (~158.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.90 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 (7.90 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 (7.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1609 mL | 15.8043 mL | 31.6086 mL | |
| 5 mM | 0.6322 mL | 3.1609 mL | 6.3217 mL | |
| 10 mM | 0.3161 mL | 1.5804 mL | 3.1609 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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