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T0901317,非LXR激动剂

强大的非选择性LXR激动剂
规格或纯度: ≥98%
有货

库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
T129709-25mg 25mg 现货 Stock Image
T129709-100mg 100mg 期货 Stock Image

基本描述

规格或纯度 ≥98%
英文名称 T0901317
别名 T 0901317; T-0901317
英文别名 T 0901317; T-0901317; N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide;N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2, 2-trifluoroethyl)benzenesulfonamide;
生化机理 T 0901317 is a cell-permeable, nonsterol, benzenesulfonamide compound that acts as a highly selective and potent liver X receptor (LXR) agonist (EC50 of 20 nM for LXRα). T 0901317 is reported to induce the expression of genes associated with fatty acid biosynthesis and raise both the levels of serum HDL cholesterol and triglyceride.Potent, non-selective LXR agonist (EC 50 = 50 nM). Increases ABCA1 expression associated with cholesterol efflux regulation and HDL metabolism. Increases muscle expression of PPAR-δ. Shows antiobesogenic effects in vivo.
储存温度 -20°C储存
运输条件 超低温冰袋运输
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产品介绍

T0901317是一个强的和选择性的LXR和FXR激动剂,EC50分别是50 nM和5 μM,能够抑制核里的NF/κB。A cell-permeable, nonsterol compound that acts as a highly potent LXR activator

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively.
A cell-permeable, nonsterol compound that acts as a highly potent LXR activator

名称和标识符

IUPAC Name N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
INCHI InChI=1S/C17H12F9NO3S/c18-14(19,20)10-27(31(29,30)13-4-2-1-3-5-13)12-8-6-11(7-9-12)15(28,16(21,22)23)17(24,25)26/h1-9,28H,10H2
InChi Key SGIWFELWJPNFDH-UHFFFAOYSA-N
Canonical SMILES C1=CC=C(C=C1)S(=O)(=O)N(CC(F)(F)F)C2=CC=C(C=C2)C(C(F)(F)F)(C(F)(F)F)O
分子式

C17H12F9NO3S

关联CAS 293754-55-9
UNII A07663A39I
PubChem CID 447912
分子量 481.33

化学和物理性质

溶解性 DMSO 96 mg/mL Water <1 mg/mL Ethanol 96 mg/mL
密度 1.55
沸点 470.55° C at 760 mmHg
熔点 116-122°C
折光率 1.49

靶标

Target ID 598
名称 RAR-related orphan receptor-α
缩写名 SHP2
家族 1F. Retinoic acid-related orphans
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 523 15q22.2 RORA RAR related orphan receptor A
Mouse 2 523 9 37.45 cM Rora RAR-related orphan receptor alpha
Rat 2 309 8q24 Rora RAR-related orphan receptor A
Entrez Gene 6095 (Hs) , 19883 (Mm) , 300807 (Rn)
OMIM 600825 (Hs)
UniProtKB P35398 (Hs) , P51448 (Mm)
RefSeq Nucleotide NM_134260 (Hs) , NM_013646 (Mm)
RefSeq Protein NP_599023 (Hs) , NP_038674 (Mm) , NP_599022 (Hs) , NP_002934 (Hs) , NP_599024 (Hs)
Ensembl Gene ENSG00000069667 (Hs) , ENSMUSG00000032238 (Mm) , ENSRNOG00000027145 (Rn)
Protein GI 7305439 (Mm) , 19743905 (Hs)
NURSA Receptor 10.1621/DSPDOWHBAX (Hs)
CATH/Gene3D 3.30.50.10 (N/A)
ChEMBL Target CHEMBL5868 (Hs) , CHEMBL3217403 (Mm)
Target ID 600
名称 RAR-related orphan receptor-γ
缩写名 SHP2
家族 1F. Retinoic acid-related orphans
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 518 1q21 RORC RAR related orphan receptor C
Mouse 2 516 3 F2.1 Rorc RAR-related orphan receptor gamma
Rat 2 147 2q34 Rorc RAR-related orphan receptor C
Entrez Gene 6097 (Hs) , 19885 (Mm) , 368158 (Rn)
OMIM 602943 (Hs)
UniProtKB P51449 (Hs) , P51450 (Mm)
RefSeq Nucleotide NM_001001523 (Hs) , NM_011281 (Mm) , NM_005060 (Hs)
RefSeq Protein NP_005051 (Hs) , NP_035411 (Mm) , NP_001001523 (Hs)
Ensembl Gene ENSG00000143365 (Hs) , ENSMUSG00000028150 (Mm) , ENSRNOG00000020836 (Rn)
Protein GI 48255918 (Hs) , 188536040 (Mm) , 109467161 (Rn)
NURSA Receptor 10.1621/SQN2V3ZKEV (Hs)
CATH/Gene3D 3.30.50.10 (N/A)
ChEMBL Target CHEMBL1741186 (Hs) , CHEMBL1293231 (Mm)
Target ID 601
名称 Liver X receptor-β
缩写名 SHP2
家族 1H. Liver X receptor-like receptors
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 460 19q13.3 NR1H2 nuclear receptor subfamily 1 group H member 2
Mouse 2 446 7 B3 Nr1h2 nuclear receptor subfamily 1, group H, member 2
Rat 2 446 1q22 Nr1h2 nuclear receptor subfamily 1, group H, member 2
Entrez Gene 7376 (Hs) , 58851 (Rn) , 22260 (Mm)
OMIM 600380 (Hs)
UniProtKB P55055 (Hs) , Q62755 (Rn) , Q60644 (Mm)
RefSeq Nucleotide NM_007121 (Hs) , NM_031626 (Rn) , NM_009473 (Mm)
RefSeq Protein NP_009052 (Hs) , NP_033499 (Mm) , NP_113814 (Rn)
Ensembl Gene ENSG00000131408 (Hs) , ENSMUSG00000060601 (Mm) , ENSRNOG00000019812 (Rn)
Protein GI 375331888 (Hs) , 13928862 (Rn) , 6678507 (Mm)
NURSA Receptor 10.1621/4Y2DTEP5D8 (Hs)
CATH/Gene3D 3.30.50.10 (N/A)
ChEMBL Target CHEMBL4105785 (Rn) , CHEMBL2417346 (Mm) , CHEMBL4093 (Hs)
Target ID 602
名称 Liver X receptor-α
缩写名 SHP2
家族 1H. Liver X receptor-like receptors
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 447 11p11.2 NR1H3 nuclear receptor subfamily 1 group H member 3
Mouse 2 445 2 50.52 cM Nr1h3 nuclear receptor subfamily 1, group H, member 3
Rat 2 445 3q24 Nr1h3 nuclear receptor subfamily 1, group H, member 3
Entrez Gene 10062 (Hs) , 22259 (Mm) , 58852 (Rn)
OMIM 602423 (Hs)
UniProtKB Q13133 (Hs) , Q62685 (Rn) , Q9Z0Y9 (Mm)
RefSeq Nucleotide NM_001130102 (Hs) , NM_031627 (Rn) , NM_013839 (Mm) , NM_001177730 (Mm)
RefSeq Protein NP_005684 (Hs) , NP_038867 (Mm) , NP_113815 (Rn)
Ensembl Gene ENSG00000025434 (Hs) , ENSMUSG00000002108 (Mm) , ENSRNOG00000013172 (Rn)
Orphanet 123908 (Hs)
Protein GI 295148193 (Mm) , 353731060 (Hs) , 145279192 (Rn)
NURSA Receptor 10.1621/WD46UVPRKT (Hs)
CATH/Gene3D 3.30.50.10 (N/A)
ChEMBL Target CHEMBL2808 (Hs) , CHEMBL2189152 (Mm) , CHEMBL4523336 (Rn)

关联配体

Ligand ID 2755
名称 T0901317
别名 T-0901317
类别 Synthetic organic
学名 N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
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 T0901317 is a synthetic agonist of the liver X receptors (LXRs), equipotent at the α and β receptor isoforms. T0901317-induced repression of the gluconeogenic enzyme glucose-6-phosphatase is is ROR-dependent and is not associated with the ligand's LXR activity .

参考文献

1. Han S, Zhuang H, Shumyak S, Wu J, Xie C, Li H, Yang LJ, Reeves WH.  (2018)  Liver X Receptor Agonist Therapy Prevents Diffuse Alveolar Hemorrhage in Murine Lupus by Repolarizing Macrophages..  Front Immunol,  (13):  (135).  [PMID:29456535]
2. Wang J, Xiao C, Wei Z, Wang Y, Zhang X, Fu Y.  (2018)  Activation of liver X receptors inhibit LPS-induced inflammatory response in primary bovine mammary epithelial cells..  Vet Immunol Immunopathol,  197  (13):  (87-92).  [PMID:29475512]
3. Zhang CJ et al..  (2021)  Celastrol induces lipophagy via the LXRα/ABCA1 pathway in clear cell renal cell carcinoma..  Acta Pharmacol Sin,  42  (9):  (1472-1485).  [PMID:33303989]
4. Wu D et al..  (2021)  Dichlorodiphenyltrichloroethane Impairs Amyloid Beta Clearance by Decreasing Liver X Receptor a Expression..  Front Aging Neurosci,  13  ():  (634948).  [PMID:34045954]

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