T0901317

製品コードS7076 バッチS707603

印刷

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	T0901317は、LXRとFXRの両方に強力で選択的なアゴニストであり、それぞれEC50が約50 nMと5 μMです。T0901317は、RORαとRORγのデュアルインバースアゴニストであり、それぞれKiが132 nMと51 nMです。T0901317は、細胞増殖を著しく抑制し、アポトーシスを誘発します。
in vitro	T0901317 acts through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This compound upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism. It 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. This chemical is also a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). It binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. This compound induces expression not only of LXR target genes, but also of PXR target genes in cells and animals, including the scavenger receptor CD36. It decreases amyloid-β production in primary neurons in vitro. This chemical 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. It 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).
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, this compound causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice.

製品説明

T0901317は、LXRとFXRの両方に強力で選択的なアゴニストであり、それぞれEC50が約50 nMと5 μMです。T0901317は、RORαとRORγのデュアルインバースアゴニストであり、それぞれKiが132 nMと51 nMです。T0901317は、細胞増殖を著しく抑制し、アポトーシスを誘発します。

in vitro

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

It 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.

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

It decreases amyloid-β production in primary neurons in vitro.

This chemical 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. It 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).

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, this compound causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice.

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 this compound 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

https://pubmed.ncbi.nlm.nih.gov/10968783/
https://pubmed.ncbi.nlm.nih.gov/15464433/
https://pubmed.ncbi.nlm.nih.gov/17418145/

https://pubmed.ncbi.nlm.nih.gov/15557325/
https://pubmed.ncbi.nlm.nih.gov/19887649/
https://pubmed.ncbi.nlm.nih.gov/35169231/

+ 展开

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]

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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

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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