T0901317

製品コードS7076 バッチS707601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₁₂F₉NO₃S
	分子量	481.33	CAS No.	293754-55-9
Solubility (25°C)*	体外	DMSO	96 mg/mL (199.44 mM)
		Ethanol	96 mg/mL (199.44 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. T0901317 significantly suppresses cell proliferation and induces apoptosis.
in vitro	T0901317 acts through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. T0901317 upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism.^[1] T0901317 displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs), 10-fold more potent than natural FXR ligand chenodeoxycholic acid. ^[2] T0901317, is also a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 induces expression not only of LXR target genes, but also of PXR target genes in cells and animals, including the scavenger receptor CD36. ^[3] T0901317 decreases amyloid-β production in primary neurons in vitro. ^[4] T0901317 is found to directly bind to RORα and RORγ with high affinity (Ki = 132 and 51 nM, respectively), resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 represses RORα/γ-dependent transactivation of ROR-responsive reporter genes and in HepG2 cells reduces recruitment of steroid receptor coactivator-2 by RORα at an endogenous ROR target gene (G6Pase). ^[5]
in vivo	T0901317 treatment of 11-week-old APP23 mice for 6 days shows a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)β- to sAPPα-cleavage products. Most importantly, the treatment causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice. ^[4]

製品説明

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. T0901317 significantly suppresses cell proliferation and induces apoptosis.

in vitro

T0901317 acts through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. T0901317 upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism.^[1]

T0901317 displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs), 10-fold more potent than natural FXR ligand chenodeoxycholic acid. ^[2]

T0901317, is also a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 induces expression not only of LXR target genes, but also of PXR target genes in cells and animals, including the scavenger receptor CD36. ^[3]

T0901317 decreases amyloid-β production in primary neurons in vitro. ^[4]

T0901317 is found to directly bind to RORα and RORγ with high affinity (Ki = 132 and 51 nM, respectively), resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 represses RORα/γ-dependent transactivation of ROR-responsive reporter genes and in HepG2 cells reduces recruitment of steroid receptor coactivator-2 by RORα at an endogenous ROR target gene (G6Pase). ^[5]

in vivo

T0901317 treatment of 11-week-old APP23 mice for 6 days shows a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)β- to sAPPα-cleavage products. Most importantly, the treatment causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	BMDMs
	濃度	5 µM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentration of drug for 24 h.
動物実験	動物モデル	APP23 mice
	投薬量	50 mg/kg/day
	投与方法	gastric gavage

参考

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カスタマーフィードバック

: , , FEBS Lett, 2015, 589(1):52-8.

: Data from [Data independently produced by , , Life Sci, 2018, doi:10.1016/j.lfs.2018.10.060]

: Data from [Data independently produced by , , Nanoscale Res Lett, 2017, 12(1):322]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Integrated Analysis Highlights the Immunosuppressive Role of TREM2+ Macrophages in Hepatocellular Carcinoma [ Front Immunol, 2022, 13:848367]	PubMed: 35359989
The LXRB-SREBP1 network regulates lipogenic homeostasis by controlling the synthesis of polyunsaturated fatty acids in goat mammary epithelial cells [ J Anim Sci Biotechnol, 2022, 13(1):120]	PubMed: 36336695
Macrophage Jak2 deficiency accelerates atherosclerosis through defects in cholesterol efflux [ Commun Biol, 2022, 5(1):132]	PubMed: 35169231
Role of PCSK9 in Homocysteine-Accelerated Lipid Accumulation in Macrophages and Atherosclerosis in ApoE-/- Mice [ Front Cardiovasc Med, 2021, 8:746989]	PubMed: 34660746
Liver X receptor β is required for the survival of single-positive thymocytes by regulating IL-7Rα expression [ Cell Mol Immunol, 2020, 10.1038/s41423-020-00546-y]	PubMed: 32963358
Deficiency of histone methyltransferase SETD2 in liver leads to abnormal lipid metabolism and hepatocarcinoma [ Hepatology, 2020, 10.1002/hep.31594]	PubMed: 33058300
Setosphapyrone C and D accelerate macrophages cholesterol efflux by promoting LXRα/ABCA1 pathway [ Arch Pharm Res, 2020, 10.1007/s12272-020-01255-w]	PubMed: 32779151
Hydrogen Sulfide Accumulates LDL Receptor Precursor via Downregulating PCSK9 in HepG2 Cells [ Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00244.2019]	PubMed: 32938225
The marine-derived furanone reduces intracellular lipid accumulation in vitro by targeting LXRα and PPARα [ J Cell Mol Med, 2020, 24(6):3384-3398]	PubMed: 31981312
The marine-derived furanone reduces intracellular lipid accumulation in vitro by targeting LXRα and PPARα. [ J Cell Mol Med, 2020, 24(6):3384-3398]	PubMed: 31981312

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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