NLG919

Catalog No.S7111

NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM in cell-free assays. Phase 1.

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NLG919 Chemical Structure

NLG919 Chemical Structure
Molecular Weight: 282.38

Validation & Quality Control

Customer Product Validation(1)

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM in cell-free assays. Phase 1.
Targets IDO [1]
(Cell-free assay)
IDO [1]
(Cell-free assay)
IC50 75 nM(EC50) 75 nM(EC50)
In vitro NLG919 potently blocks IDO-induced T-cell suppression and restored robust T-cell responses with ED50 of 80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, NLG919 abrogated IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED50 of 120 nM. [1]
In vivo In mice, a single oral administration of NLG919 reduces the concentration of plasma and tissue Kyn by ~ 50%. In mice bearing B16F10 tumors, NLG919 markedly enhances the antitumor responses of naive, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA.[1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] AACR Meeting, Poster 491, 2013.

Chemical Information

Download NLG919 SDF
Molecular Weight (MW) 282.38
Formula

C18H22N2O

CAS No. 1402836-58-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 15 mg/mL warmed (53.11 mM)
Ethanol 30 mg/mL (106.23 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5H-Imidazo[5,1-a]isoindole-5-ethanol, α-cyclohexyl-

Customer Product Validation (1)


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Rating
Source J Biomol Screen 2014 10.1177/1087057114536616. NLG919 purchased from Selleck
Method N-formylkynurenine (NFK) Green assay
Cell Lines A-172 glioblastoma cells
Concentrations 75 nM
Incubation Time 6 h
Results NCB024360 and S7111 potently inhibited TDO, which are close to literature values—that is, 67 nM for INCB0243609 and 75 nM for S7111.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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