製品番号: HY-10626

T0901317

45 Cited Publications

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Based on 45 publication(s) in Google Scholar

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

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純度: 99.85%
CAS 番号: 293754-55-9
分子式: C₁₇H₁₂F₉NO₃S
分子量:481.33

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

T0901317 構造式

CAS 番号: 293754-55-9

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製品説明

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα^[1]. T0901317 activates FXR with an EC₅₀ of 5 μM^[2]. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively^[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice^[4]^[5].

IC₅₀ & Target

EC50: 20 nM (LXRα) and 5 μM (FXR)^[1]^[2]
Ki: 132 nM (RORα) and 51 nM (RORγ)^[3]

ROR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	16 nM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay	[PMID: 19853462]
CHO	EC₅₀	16 nM Compound: 3, TO901317	Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay	[PMID: 17034119]
CHO-K1	EC₅₀	0.41 μM Compound: 1, T0901317	Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
CHO-K1	EC₅₀	0.41 μM Compound: T0901317	Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27283790]
CHO-K1	EC₅₀	0.49 μM Compound: 1, T0901317	Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
CHO-K1	EC₅₀	0.49 μM Compound: T0901317	Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27283790]
COS-7	EC₅₀	0.011 μM Compound: T0901317	Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay	[PMID: 17416521]
COS-7	EC₅₀	0.011 μM Compound: T0901317	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay	[PMID: 17587573]
COS-7	EC₅₀	84 % Compound: T0901317	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-3965 Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-3965	[PMID: 17587573]
CV-1	EC₅₀	0.03 μM Compound: 1, T0901317	Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay	[PMID: 26238323]
CV-1	EC₅₀	0.13 μM Compound: 1, T0901317	Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay	[PMID: 26238323]
CV-1	EC₅₀	140 nM Compound: 1a, TO-091317	Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
CV-1	EC₅₀	28 nM Compound: 1a, TO-091317	Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
H4	EC₅₀	0.02 μM Compound: 1; TO-091317	Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay	[PMID: 27011007]
H4	EC₅₀	3.6 μM Compound: 4, TO901317	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay	[PMID: 17723298]
H4	IC₅₀	>40 μM Compound: 4, TO901317	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay	[PMID: 17723298]
H4	IC₅₀	4.5 μM Compound: 4, TO901317	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay	[PMID: 17723298]
HEK293	EC₅₀	0.01 μM Compound: T0901317	Activity against LXR alpha transiently transfected in HEK293 cells Activity against LXR alpha transiently transfected in HEK293 cells	[PMID: 16386417]
HEK293	EC₅₀	0.019 μM Compound: 1a	Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation	[PMID: 20350005]
HEK293	EC₅₀	0.036 μM Compound: 8, T0901317	Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.053 μM Compound: 1a	Agonist activity at human LXRalpha in HEK293 cells assessed as Gal4 transactivation Agonist activity at human LXRalpha in HEK293 cells assessed as Gal4 transactivation	[PMID: 20350005]
HEK293	EC₅₀	0.066 μM Compound: 3, T0901317	Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 26288691]
HEK293	EC₅₀	0.09 μM Compound: 3, T1317	Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay	[PMID: 22873709]
HEK293	EC₅₀	0.12 μM Compound: T0901317	Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	0.16 μM Compound: 8, T0901317	Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.21 μM Compound: 3, T0901317	Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 26288691]
HEK293	EC₅₀	0.23 μM Compound: 5; T0901317	Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.27 μM Compound: 5; T0901317	Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.29 μM Compound: T0901317	Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	0.34 μM Compound: 3, T1317	Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay	[PMID: 22873709]
HEK293	EC₅₀	0.37 μM Compound: 8, T0901317	Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.4 μM Compound: 5; T0901317	Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.46 μM Compound: 8, T0901317	Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	1.3 μM Compound: 8, T0901317	Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	3.4 μM Compound: 5; T0901317	Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	5 μM Compound: 8, T0901317	Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	6 μM Compound: 8, T0901317	Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	85 nM Compound: T0901317	Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 25305688]
HEK293	IC₅₀	>20 μM Compound: T0901317	Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	IC₅₀	3 μM Compound: 5; T0901317	Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay	[PMID: 26905831]
HEK293	IC₅₀	6.5 μM Compound: T0901317	Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK-293T	EC₅₀	0.036 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.156 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.25 μM Compound: T0901317	Agonist activity at GAL4-fused LXR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Agonist activity at GAL4-fused LXR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK-293T	EC₅₀	0.373 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.463 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.8 μM Compound: 4; T0901317	Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	0.94 μM Compound: 4; T0901317	Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	1 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	5 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	6 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	IC₅₀	1.7 μM Compound: T0901317	Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK-293T	IC₅₀	2 μM Compound: T0901317	Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HeLa	EC₅₀	17 nM Compound: 1a, TO-091317	Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay	[PMID: 25435151]
HepG2	EC₅₀	0.02 μM Compound: 1; TO-091317	Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay	[PMID: 27011007]
HepG2	EC₅₀	0.137 μM Compound: 1 (TO901317)	Effect on triglyceride accumulation in human HepG2 cells Effect on triglyceride accumulation in human HepG2 cells	[PMID: 19962892]
HepG2	EC₅₀	0.137 μM Compound: 1, T0901317	Increase in cellular triglyceride level in human HepG2 cells Increase in cellular triglyceride level in human HepG2 cells	[PMID: 20005711]
HepG2	EC₅₀	0.14 μM Compound: 1a	Induction of [3H]cholesterol efflux in human HepG2 cells loaded with ac-LDL assessed as lipid accumulation Induction of [3H]cholesterol efflux in human HepG2 cells loaded with ac-LDL assessed as lipid accumulation	[PMID: 20350005]
HepG2	EC₅₀	104 nM Compound: 1, T0901317	Increase in cellular triglyceride level in human HepG2 cells Increase in cellular triglyceride level in human HepG2 cells	[PMID: 20006495]
HepG2	EC₅₀	107 nM Compound: 1, T0901317	Increase in triglyceride level in human HepG2 cells Increase in triglyceride level in human HepG2 cells	[PMID: 20382019]
HepG2	EC₅₀	137 nM Compound: 3, TO901317	Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days	[PMID: 18023179]
HepG2	EC₅₀	137 nM Compound: 1, T0901317	Effect on triglyceride accumulation in human HepG2 cells Effect on triglyceride accumulation in human HepG2 cells	[PMID: 18973288]
HepG2	EC₅₀	190 nM Compound: 6, GW3965	Agonist activity at Homo sapiens (human) LXRalpha expressed in HepG2 cells assessed as transactivation of CYP7A1 gene expression after 48 hr by luciferase reporter gene assay Agonist activity at Homo sapiens (human) LXRalpha expressed in HepG2 cells assessed as transactivation of CYP7A1 gene expression after 48 hr by luciferase reporter gene assay	10.1007/s00044-012-0359-5
HepG2	EC₅₀	61 nM Compound: 1, T0901317	Effect on SREBP1c gene expression in human HepG2 cells Effect on SREBP1c gene expression in human HepG2 cells	[PMID: 18973288]
HepG2	EC₅₀	67 nM Compound: 3, TO901317	Effect on SREBP1c gene expression in human HepG2 cells Effect on SREBP1c gene expression in human HepG2 cells	[PMID: 18023179]
Huh-7	EC₅₀	0.067 μM Compound: 3, TO901317	Induction of SREBP-1C mRNA expression in human HuH7 cells after 18 hrs by RT-PCR Induction of SREBP-1C mRNA expression in human HuH7 cells after 18 hrs by RT-PCR	[PMID: 19394832]
Huh-7	EC₅₀	0.135 μM Compound: 1, T0901317	Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay	[PMID: 20005711]
Huh-7	EC₅₀	0.135 μM Compound: 3, TO901317	Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay	[PMID: 19394832]
Huh-7	EC₅₀	0.14 μM Compound: 1 (TO901317)	Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
Huh-7	EC₅₀	0.14 μM Compound: 1, T0901317	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	0.14 μM Compound: 1a	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 20350005]
Huh-7	EC₅₀	0.17 μM Compound: 1 (TO901317)	Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
Huh-7	EC₅₀	0.17 μM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	0.17 μM Compound: 1, T0901317	Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay	[PMID: 20005711]
Huh-7	EC₅₀	0.17 μM Compound: 1a	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 20350005]
Huh-7	EC₅₀	0.178 μM Compound: 3, TO901317	Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay	[PMID: 19394832]
Huh-7	EC₅₀	135 nM Compound: 3, TO901317	Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay	[PMID: 18023179]
Huh-7	EC₅₀	170 nM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay	[PMID: 20382019]
Huh-7	EC₅₀	178 nM Compound: 3, TO901317	Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay	[PMID: 18023179]
Huh-7	EC₅₀	36 nM Compound: 1, T0901317	Upregulation of SREB1c mRNA level in human HuH7 cells Upregulation of SREB1c mRNA level in human HuH7 cells	[PMID: 20382019]
J774	EC₅₀	27 nM Compound: 1, T0901317	Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression	[PMID: 19853462]
J774	EC₅₀	35 nM Compound: 1, T0901317	Upregulation of ABCA1 mRNA level in mouse J774 cells Upregulation of ABCA1 mRNA level in mouse J774 cells	[PMID: 20382019]
J774	EC₅₀	35 nM Compound: 3, TO901317	Effect on ABCA1 gene expression in mouse J774 cells Effect on ABCA1 gene expression in mouse J774 cells	[PMID: 18023179]
J774.A1	EC₅₀	0.034 μM Compound: 3, TO901317	Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR	[PMID: 19394832]
J774.A1	EC₅₀	35 nM Compound: 1	Induction of ABCA1 mRNA expression in mouse J774A1 cells Induction of ABCA1 mRNA expression in mouse J774A1 cells	[PMID: 19932617]
L02	EC₅₀	0.53 μM Compound: TO901317	Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay	[PMID: 31095389]
LS180	IC₅₀	>50 μM Compound: 6; T0901317	Cytotoxicity against human LS180 cells assessed as effect on cell viability measured after 24 hrs by MTT assay Cytotoxicity against human LS180 cells assessed as effect on cell viability measured after 24 hrs by MTT assay	[PMID: 27497733]
PBMC	EC₅₀	>20 μM Compound: 1, T0901317	Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay	[PMID: 24239186]
PBMC	EC₅₀	>20 μM Compound: 1, T0901317	Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA	[PMID: 24239186]
PBMC	EC₅₀	3 μM Compound: 1, T0901317	Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA	[PMID: 24239186]
Platelet	IC₅₀	>50 nM Compound: T0901317	Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay	[PMID: 32463237]
SH-SY5Y	EC₅₀	0.075 μM Compound: 2, T0901317	Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
SH-SY5Y	EC₅₀	0.085 μM Compound: 2, T0901317	Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
SH-SY5Y	IC₅₀	>50 μM Compound: 6; T0901317	Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability measured after 24 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability measured after 24 hrs by MTT assay	[PMID: 27497733]
THP-1	EC₅₀	0.033 μM Compound: T0901317	Induction of cholesterol efflux in THP1 cells after 18 hrs Induction of cholesterol efflux in THP1 cells after 18 hrs	[PMID: 17416521]
THP-1	EC₅₀	0.033 μM Compound: T0901317	Induction of cholesterol efflux in THP1 cells Induction of cholesterol efflux in THP1 cells	[PMID: 17587573]
THP-1	EC₅₀	0.044 μM Compound: 1 (TO901317)	Effect on ABCA1 gene expression in human differentiated THP1 cells Effect on ABCA1 gene expression in human differentiated THP1 cells	[PMID: 19962892]
THP-1	EC₅₀	0.044 μM Compound: 1, T0901317	Induction of ABCA1 mRNA upregulation in human THP1 cells Induction of ABCA1 mRNA upregulation in human THP1 cells	[PMID: 20005711]
THP-1	EC₅₀	0.044 μM Compound: 1a	Induction of ABCA1 expression in human THP1 cells Induction of ABCA1 expression in human THP1 cells	[PMID: 20350005]
THP-1	EC₅₀	3 nM Compound: 1 (TO901317)	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL	[PMID: 19962892]
THP-1	EC₅₀	3 nM Compound: 1 (TO901317)	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO901317 Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO901317	[PMID: 19962892]
THP-1	EC₅₀	3 nM Compound: 1, T0901317	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL	[PMID: 18973288]
THP-1	EC₅₀	35 nM Compound: 1, T0901317	Induction of ABCA1 mRNA upregulation in human THP1 cells Induction of ABCA1 mRNA upregulation in human THP1 cells	[PMID: 20006495]
THP-1	EC₅₀	44 nM Compound: 1, T0901317	Effect on ABCA1 gene expression in human differentiated THP1 cells Effect on ABCA1 gene expression in human differentiated THP1 cells	[PMID: 18973288]
THP-1	EC₅₀	44 nM Compound: 3, TO901317	Effect on ABCA1 gene expression in human THP1 cells Effect on ABCA1 gene expression in human THP1 cells	[PMID: 18023179]
THP-1	IC₅₀	>10 μM Compound: 3, T1317	Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA	[PMID: 22873709]
THP-1	IC₅₀	100 nM Compound: 3, T1317	Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA	[PMID: 18800767]
THP-1	IC₅₀	26 μM Compound: 3, T0901317	Transrepression activity of LXR in human THP1 cells assessed as inhibition of LPS-induced IL-6 level after 18 hrs by ELISA Transrepression activity of LXR in human THP1 cells assessed as inhibition of LPS-induced IL-6 level after 18 hrs by ELISA	[PMID: 26288691]

体外実験

rateand the T0901317 (5-50 μM; 72 hours) significantly inhibits cellular proliferation in CaOV3, SKOV3, A2780 (human ovarian carcinoma cell lines) in a dose-dependent and time-dependent manner^[5].
T0901317 (10 μM; 24-72 hours) decreases the percentage of cells in S phase and increases the percentage of cells in the G0/G1 phase, indicating a cell cycle arrest at the G1-S checkpoint. The percentage of cells in G0/G1 phase increases in a time-dependent manner^[5].
T0901317 (10-40 μM; 24 hours ) results in a significant increase of cells in early apoptosis^[5].
T0901317 (5-40 μM; 48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[5]

Cell Line:

A2780, CaOV3 and SKOV3 ovarian cancer cell lines
Concentration:

5, 10, 20, 40 or 50 μM
Incubation Time:

72 hours
Result:

Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner.

Cell Cycle Analysis^[5]

Cell Line:

A2780, CaOV3 and SKOV3 cells
Concentration:

10 μM
Incubation Time:

24, 48 or 72 hours
Result:

Decreased the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase.

Apoptosis Analysis^[5]

Cell Line:

CaOV3 cells
Concentration:

10 to 40 μM
Incubation Time:

24 hours
Result:

Resulted in a significant increase of cells in early apoptosis.

Western Blot Analysis^[5]

Cell Line:

CaOV3 cells
Concentration:

5 to 40 μM
Incubation Time:

48 hours
Result:

Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner.

体内実験

T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis^[5].
T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) can protect male C57BL/6 mice from high fat diet-induced obesity and insulin resistance^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

8- to 10-week-old LDL receptor null mice^[5]
Dosage:

10 mg/kg
Administration:

Orally; daily; for 12 weeks
Result:

Inhibited the progression of atherosclerosis.

化学情報

CAS 番号 293754-55-9
性状 Solid
分子量 481.33
分子式 C₁₇H₁₂F₉NO₃S
Color White to off-white
SMILES

OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(N(CC(F)(F)F)S(C2=CC=CC=C2)(=O)=O)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (45)

All 2D/3D Cell Culture and DifferentiationCell Imaging/StainingRT-PCR

Sort by:

Journal Impact Factor

Immunity

Membrane integrity changes upon viral infection activate sphingomyelinase SMPDL3B to restrict cGAS-STING signaling via cGAMP degradation. [Abstract]

2025 Nov 11;58(11):2670-2684.e10. PMID: 41175872
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

PROTAC repurposing uncovers a noncanonical binding surface that mediates chemical degradation of nuclear receptors. [Abstract]

2025 Nov 6;16(1):9805. PMID: 41198675
Nat Commun

Nuclear receptor-SINE B1 network modulates expanded pluripotency in blastoids and blastocysts. [Abstract]

2024 Nov 19;15(1):10011. PMID: 39562549

T0901317 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 19;15(1):10011. [Abstract]

Representative images of blastoids harvested at Day 5 of differentiation with or without T09 treatment, and quantification of the type I and II blastoid formation efficiency with or without T09 (10 µM) treatment. Scale bar, 150 µm.

T0901317 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 19;15(1):10011. [Abstract]

Quantification of the developmental rate of mouse blastocysts after supplementing T09 (10 µM) in culture media from one-cell stage.

T0901317 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 19;15(1):10011. [Abstract]

Representative images of porcine SCNT morula and blastocyst in T09(10 µM)-treated and control group post-SCNT. Scale bar, 50 µm.

T0901317 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 19;15(1):10011. [Abstract]

Sequential ChIP-qPCR indicating the increased co-binding of Kdm1a and Nr1h2-FLAG under T09 (10 µM) treatment at Abca1, Hdac2, Grn and Scd1, normalized to EGFP-FLAG control. Regions not bound by Kdm1a and Nr1h2-FLAG were used as negative control.

T0901317 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 19;15(1):10011. [Abstract]

Quantification of blastoid formation efficiency from NrESC treated with T09 (10 µM) and/ or Scd1 inhibitor.
Nat Commun

Glutathione synthesis in the mouse liver supports lipid abundance through NRF2 repression. [Abstract]

2024 Jul 21;15(1):6152. PMID: 39034312
Cardiovasc Res

Protective functions of liver X receptor α on calcified aortic valve: involvement of regulating endoplasmic reticulum-mediated osteogenic differentiation. [Abstract]

2025 Jun 12;121(6):957-970. PMID: 40088465
J Exp Clin Cancer Res

Ficolin 3 promotes ferroptosis in HCC by downregulating IR/SREBP axis-mediated MUFA synthesis. [Abstract]

2024 May 3;43(1):133. PMID: 38698462
Cell Death Dis

Latexin deficiency limits foam cell formation and ameliorates atherosclerosis by promoting macrophage phenotype differentiation. [Abstract]

2024 Oct 18;15(10):754. PMID: 39424784
Phytomedicine

2025 Dec 28.
Cell Chem Biol

Identification of aryl hydrocarbon receptor as a functional target that enhances astrocytic ApoE secretion. [Abstract]

2026 Jan 15;33(1):91-101.e12. PMID: 41483807
J Med Chem

Design, Synthesis, and Biological Evaluation of Arylimidazole Derivatives as Potent PPARδ Agonists for the Treatment of Renal Fibrosis. [Abstract]

2026 Feb 26;69(4):4469-4492. PMID: 41667192
J Med Chem

First-in-Class Small Molecule Degrader of Pregnane X Receptor Enhances Chemotherapy Efficacy. [Abstract]

2024 Oct 24;67(20):18549-18575. PMID: 39405362
J Med Chem

Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis. [Abstract]

2022 Feb 10;65(3):2571-2592. PMID: 35060744
Neural Regen Res

Thrombin increases the expression of cholesterol 25-hydroxylase in rat astrocytes after spinal cord injury. [Abstract]

2023 Jun;18(6):1339-1346. PMID: 36453421
Anal Chem

Codetermination of Sphingomyelin and Cholesterol in Cellular Plasma Membrane in Sphingomyelin-Depletion-Induced Cholesterol Efflux. [Abstract]

2019 Jan 15;91(2):1501-1506. PMID: 30548066
Ecotoxicol Environ Saf

Activation of LXRα attenuates 2-Ethylhexyl diphenyl phosphate (EHDPP) induced placental dysfunction. [Abstract]

2023 Nov 1:266:115605. PMID: 37864966
Food Biosci

2025 Nov 1;74:107860.
Eur J Med Chem

Design, synthesis, and biological evaluation of imidazolidinone derivatives as potent PPARα/δ agonists for the treatment of cholestatic liver diseases. [Abstract]

2025 Jan 15:286:117284. PMID: 39827490
Eur J Med Chem

Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis. [Abstract]

2024 Apr 5:269:116344. PMID: 38522113
Chin Med

Combination of mangiferin and T0901317 targeting autophagy promotes cholesterol efflux from macrophage foam cell in atherosclerosis. [Abstract]

2024 Jan 5;19(1):5. PMID: 38183139
Atherosclerosis

TIGAR mitigates atherosclerosis by promoting cholesterol efflux from macrophages. [Abstract]

2021 Jun:327:76-86. PMID: 33994201
Chem Biol Interact

Vitamin D inhibits tamoxifen-induced non-alcoholic fatty liver disease through a nonclassical estrogen receptor/liver X receptor pathway. [Abstract]

2024 Feb 1:389:110865. PMID: 38191086
Int Immunopharmacol

LXRs agonists alleviate fat transplantation-induced cognitive dysfunction by inhibiting STING-dependent type I interferon response. [Abstract]

2026 Mar 1:172:116229. PMID: 41558290
Int Immunopharmacol

Sirtuin 6 activator UBCS039 ameliorates hepatic lipogenesis through liver X receptor deacetylation. [Abstract]

2026 Jan 1;168(Pt 2):115878. PMID: 41265217
Int Immunopharmacol

Chalcone derivative 1m mitigates hepatic fibrosis and inflammation, enhances cholesterol efflux and reduces atherosclerosis. [Abstract]

2025 Sep 23:162:115189. PMID: 40644861
Int Immunopharmacol

Effects of allyl isothiocyanate on the expression, function, and its mechanism of ABCA1 and ABCG1 in pulmonary of COPD rats. [Abstract]

2021 Dec;101(Pt B):108373. PMID: 34802946
Biol Res

RASAL1 induces to downregulate the SCD1, leading to suppression of cell proliferation in colon cancer via LXRα/SREBP1c pathway. [Abstract]

2019 Dec 17;52(1):60. PMID: 31847887
Cancers (Basel)

Menin Maintains Cholesterol Content in Colorectal Cancer via Repression of LXR-Mediated Transcription. [Abstract]

2023 Aug 16;15(16):4126. PMID: 37627154
Structure

Subtle changes in ligand-receptor interactions dramatically alter transcriptional outcomes of pregnane X receptor modulators. [Abstract]

2025 Oct 24:S0969-2126(25)00386-7. PMID: 41138720
FASEB J

SREBP-1-mediated lipogenesis confers resistance to ferroptosis and improves endothelial injury. [Abstract]

2024 Jul 15;38(13):e23806. PMID: 38970404
J Cell Mol Med

Photobiomodulation therapy promotes the ATP-binding cassette transporter A1-dependent cholesterol efflux in macrophage to ameliorate atherosclerosis. [Abstract]

2021 Jun;25(11):5238-5249. PMID: 33951300
Nutr Metab

A novel small compound TOIDC suppresses lipogenesis via SREBP1-dependent signaling to curb MAFLD. [Abstract]

2022 Dec 6;19(1):80. PMID: 36474251
J Funct Foods

January 2022, 104901.
Food Chem Toxicol

Toosendanin induces hepatotoxicity via disrupting LXRα/Lipin1/SREBP1 mediated lipid metabolism. [Abstract]

2024 May:187:114631. PMID: 38570025
Viruses

Pseudorabies Virus Inhibits Expression of Liver X Receptors to Assist Viral Infection. [Abstract]

2022 Mar 3;14(3):514. PMID: 35336921
Curr Issues Mol Biol

Dimethyloxalylglycine Suppresses SREBP1c and Lipogenic Gene Expressions in Hepatocytes Independently of HIF1A. [Abstract]

2024 Mar 13;46(3):2386-2397. PMID: 38534767
Br J Nutr

Oleic and palmitic acids induce hepatic angiopoietin-like 4 expression predominantly via PPAR-γ in Larimichthys crocea. [Abstract]

2023 May 28;129(10):1657-1666. PMID: 34556193
J Atheroscler Thromb

MicroRNA-320b Modulates Cholesterol Efflux and Atherosclerosis. [Abstract]

2022 Feb 1;29(2):200-220. PMID: 33536383
Gastroenterol Res Pract

Role of Baicalin and Liver X Receptor Alpha in the Formation of Cholesterol Gallstones in Mice. [Abstract]

2020 Apr 21;2020:1343969. PMID: 32382260
Cell Press Blue

2026 Apr 22.
SSRN

2025 Jul 25.
bioRxiv

Cholesterol-mediated Lysosomal Dysfunction in APOE4 Astrocytes Promotes α-Synuclein Pathology in Human Brain Tissue. [Abstract]

2025 Feb 14:2025.02.09.637107. PMID: 39975381
Research Square Preprint

2023 May 25.
bioRxiv

2023 Mar 10.
Universitetet i Oslo

2021 Jul.

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (207.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (207.76 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0776 mL

10.3879 mL

20.7758 mL

5 mM

0.4155 mL

2.0776 mL

4.1552 mL

10 mM

0.2078 mL

1.0388 mL

2.0776 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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分子量分子量

希釈計算機

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濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.5 mg/mL (5.19 mM); Suspended solution; Need ultrasonic

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

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純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[1]. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8. [Content Brief]

[2]. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7. [Content Brief]

[3]. Naresh Kumar, et al. The Benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-Alpha/Gamma Inverse Agonist. Mol Pharmacol. 2010 Feb;77(2):228-36. [Content Brief]

[4]. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13. [Content Brief]

[5]. Todd G Kirchgessner, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33. [Content Brief]

[6]. Mingming Gao, et al. The Liver X Receptor Agonist T0901317 Protects Mice From High Fat Diet-Induced Obesity and Insulin Resistance. AAPS J. 2013 Jan;15(1):258-66. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	2.0776 mL	10.3879 mL	20.7758 mL	51.9394 mL
	5 mM	0.4155 mL	2.0776 mL	4.1552 mL	10.3879 mL
	10 mM	0.2078 mL	1.0388 mL	2.0776 mL	5.1939 mL
	15 mM	0.1385 mL	0.6925 mL	1.3851 mL	3.4626 mL
	20 mM	0.1039 mL	0.5194 mL	1.0388 mL	2.5970 mL
	25 mM	0.0831 mL	0.4155 mL	0.8310 mL	2.0776 mL
	30 mM	0.0693 mL	0.3463 mL	0.6925 mL	1.7313 mL
	40 mM	0.0519 mL	0.2597 mL	0.5194 mL	1.2985 mL
	50 mM	0.0416 mL	0.2078 mL	0.4155 mL	1.0388 mL
	60 mM	0.0346 mL	0.1731 mL	0.3463 mL	0.8657 mL
	80 mM	0.0260 mL	0.1298 mL	0.2597 mL	0.6492 mL
	100 mM	0.0208 mL	0.1039 mL	0.2078 mL	0.5194 mL

T0901317

45 Cited Publications

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T0901317

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Chemical Probe Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 T0901317

ROR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (45)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

T0901317

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Chemical Probe Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 T0901317

ROR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (45)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

T0901317 関連分類

製品番号: HY-10626