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1.13.11-双加氧酶
Linrodostat (BMS-986205)

Linrodostat (BMS-986205)

IDO/TDO 抑制剂

规格或纯度: 98%

CAS编号: 1923833-60-6
分子式: C₂₄H₂₄ClFN₂O
分子量: 410.91
PubChem编号: 121328278

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货号 (SKU)	包装规格	是否现货
L414088-5mg	5mg	期货
L414088-10mg	10mg	现货
L414088-25mg	25mg	期货
L414088-50mg	50mg	现货
L414088-100mg	100mg	现货

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indoleamine 2，3-dioxygenase 1 Inhibitor

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基本描述

规格或纯度	98%
英文名称	Linrodostat (BMS-986205)
别名	ONO-7701Cyclohexaneacetamide?,N-?(4-?chlorophenyl)?-?4-?(6-?fluoro-?4-?quinolinyl)?-?α-?methyl-?,cis-?(αR)?-；ONO-7701
英文别名	ONO-7701Cyclohexaneacetamide?,N-?(4-?chlorophenyl)?-?4-?(6-?fluoro-?4-?quinolinyl)?-?α-?methyl-?,cis-?(αR)?-；ONO-7701
生化机理	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.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	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.

名称和标识符

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
分子式	C₂₄H₂₄ClFN₂O
关联CAS	1923833-60-6
UNII	0A7729F42K
PubChem CID	121328278
分子量	410.91

化学和物理性质

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

靶标

Target ID

2829

名称

indoleamine 2,3-dioxygenase 1

缩写名

IDO1

家族

1.13.11.- Dioxygenases

别名

V₃

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	403	8p11.21	IDO1	indoleamine 2,3-dioxygenase 1
Mouse	2	407	8 A2	Ido1	indoleamine 2,3-dioxygenase 1
Rat	2	407	16q12.5	Ido1	indoleamine 2,3-dioxygenase 1

Entrez Gene

3620 (Hs) , 15930 (Mm) , 66029 (Rn)

RefSeq Nucleotide

NM_002164 (Hs) , NM_008324 (Mm) , NM_001293690 (Mm) , NM_023973 (Rn)

RefSeq Protein

NP_002155 (Hs) , NP_032350 (Mm) , NP_001280619 (Mm) , NP_076463 (Rn)

Protein GI

4504577 (Hs) , 6680347 (Mm) , 13027384 (Rn)

OMIM

147435 (Hs)

UniProtKB

P14902 (Hs) , P28776 (Mm) , Q9ERD9 (Rn)

Ensembl Gene

ENSMUSG00000031551 (Mm) , ENSG00000131203 (Hs) , ENSRNOG00000031189 (Rn)

ChEMBL Target

CHEMBL4685 (Hs) , CHEMBL4523451 (Rn) , CHEMBL1075294 (Mm)

关联配体

Ligand ID	9707
名称	linrodostat
别名	BMS986205
类别	Synthetic organic
学名	(2R)-N-(4-chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	Linrodostat (BMS-986205) is a potent and selective, orally available indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor , being investigated as an immuno-therapeutic for various malignancies. The INN for linrodostat specifies the (R) stereoisomer. The chemical structure is claimed as example 19 in Flexus Bioscience's patent US2016137652 and the compound is being taken through clinical development by Bristol-Myers Squibb. Mechanistically, linrodostat competes with the heme cofactor for binding to the apo-form of the enzyme, and once bound prevents heme from rebinding .
临床描述	The purpose of this study is to see if BMS-986205 combined with nivolumab, compared to nivolumab by itself, is more effective in treating Melanoma that has spread or is unable to be removed by surgery, and has not previously been treated
来源公司	Bristol-Myers Squibb

参考文献

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]
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]