T0901317

Name: T0901317
Brand: MedChemExpress
SKU: HY-10626
Rating: 5.0 (28 reviews)

Cat. No.: HY-10626 Purity: 99.93%: FAQs
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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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T0901317 Chemical Structure

CAS No. : 293754-55-9

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 28 publication(s) in Google Scholar

28 Publications Citing Use of MCE T0901317

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

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: 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	0.41 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	0.49 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]
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]
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	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]
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	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	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	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	0.066 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	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	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	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]
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]
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	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
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]
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	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	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
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: 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	0.14 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	0.17 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	0.17 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: 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	0.178 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]
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]
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	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]
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]
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	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	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]

In Vitro

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.

In Vivo

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.

Molecular Weight

481.33

Formula

C₁₇H₁₂F₉NO₃S

CAS No.

293754-55-9

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (253 KB) HNMR (272 KB) RP-HPLC (242 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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