Linrodostat (BMS-986205) - 98%, high purity , CAS No.1923833-60-6, Inhibitor of indoleamine 2;3-dioxygenase 1

Item Number
L414088
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L414088-5mg
5mg
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$64.90
L414088-10mg
10mg
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L414088-25mg
25mg
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$195.90
L414088-50mg
50mg
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100mg
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IDO/TDO Inhibitors

Basic Description

SynonymsONO7701 | ONO-7701 | ONO 7701 | s8629 | 1-(6-Amino-9H-purin-9-yl)-1-deoxy-N-ethyl-?-D-ribofuranuronamide | Linrodostat | SCHEMBL21374258 | (R)-N-(4-chlorophenyl)-2-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide;(R)-N-(4-chlorophenyl)-2-((1s,4S)-
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsLinrodostat (BMS-986205, ONO-7701) is an irreversible inhibitor of IDO1 with an IC50 of 1.7 nM. It inhibits kynurenine production with IC50 values of 1.7, 1.1 and > 2000 in human HeLa, HEK293 expressing human IDO-1 and tryptophan-2, 3-dioxygenase cell-
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of indoleamine 2;3-dioxygenase 1
Product Description

Information

Linrodostat (BMS-986205) Linrodostat (BMS-986205, ONO-7701) is an irreversible inhibitor of IDO1 with an IC50 of 1.7 nM. It inhibits kynurenine production with IC50 values of 1.7, 1.1 and > 2000 in human HeLa, HEK293 expressing human IDO-1 and tryptophan-2, 3-dioxygenase cell-based assays.


Targets

IDO1 (Cell-free assay) 1.7 nM


In vitro

BMS-986205 exhibits potent inhibition of kynurenine (kyn) production in IDO1-HEK293 cells (IC50 = 1.1 nM) but not in TDO-HEK293 cells. It is an irreversible suicide inhibitor.


Product description:

BMS-986205 is a selective indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor.

Associated Targets(Human)

IDO1 Tchem Indoleamine 2,3-dioxygenase 1 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name (2R)-N-(4-chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide
INCHI InChI=1S/C24H24ClFN2O/c1-15(24(29)28-20-9-6-18(25)7-10-20)16-2-4-17(5-3-16)21-12-13-27-23-11-8-19(26)14-22(21)23/h6-17H,2-5H2,1H3,(H,28,29)/t15-,16?,17?/m1/s1
InChi Key KRTIYQIPSAGSBP-KLAILNCOSA-N
Canonical SMILES CC(C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)C(=O)NC4=CC=C(C=C4)Cl
Isomeric SMILES C[C@H](C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)C(=O)NC4=CC=C(C=C4)Cl
Alternate CAS 1923833-60-6
PubChem CID 121328278
MeSH Entry Terms (2R)-N-(4-Chlorophenyl)-2-(cis-4-(6-fluoro-4-quinolinyl)cyclohexyl)propanamide;BMS-986205;Cyclohexaneacetamide, N-(4-chlorophenyl)-4-(6-fluoro-4-quinolinyl)-\u03b1-methyl-, cis-;linrodostat
Molecular Weight 410.91

Certificates

Certificate of Analysis(COA)

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3 results found

Lot NumberCertificate TypeDateItem
G2216554Certificate of AnalysisJun 07, 2022 L414088
G2216555Certificate of AnalysisJun 07, 2022 L414088
G2216556Certificate of AnalysisJun 07, 2022 L414088

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 82 mg/mL (199.55 mM); Ethanol: 82 mg/mL (199.55 mM); Water: Insoluble;

Related Documents

References

1. Li F, Zhang R, Li S, Liu J.  (2017)  IDO1: An important immunotherapy target in cancer treatment..  Int Immunopharmacol,  47  (13): (70-77).  [PMID:28365507] [10.1021/op500134e]
2. Nelp MT, Kates PA, Hunt JT, Newitt JA, Balog A, Maley D, Zhu X, Abell L, Allentoff A, Borzilleri R et al..  (2018)  Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form..  Proc Natl Acad Sci USA,  115  (13): (3249-3254).  [PMID:29531094] [10.1021/op500134e]

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