liver x receptor

GW3965 hydrochloride (GW3965 HCl) 是一种肝 X 受体 (LXR) 激动剂，主要作用于 hLXRα (EC50:190 nM) 和 hLXRβ (EC50:30 nM)

SR9243 是一种 liver-X-receptor 的反向激动剂，可诱导 LXR-辅阻遏物相互作用。

GSK2033 是LXR 的有效拮抗剂，抑制LXRα和LXRβ的pIC50分别为 7 和 7.4。

T0901317 是一种口服有效且高度选择性的LXR 激动剂，对 LXRα 的EC50为 20 nM。它激活FXR，EC50为 5 μM。它是RORα和RORγ双重反向激动剂，Ki 值分别为 132 nM 和 51 nM。它诱导细胞凋亡，并抑制低密度脂蛋白受体缺失小鼠动脉粥样硬化的发展。

GSK3987 是广谱LXRα β激动剂，EC50分别为 50 nM 和 40 nM。GSK3987增加 ABCA1 和 SREBP-1c 蛋白的表达，诱导细胞甘油三酯的积累和胆固醇流出。

RGX-104 (RGX-104 free Acid) 是一种口服具有活力的肝X 核激素受体激动剂，通过 ApoE 基因的转录激活调节先天免疫。

LXR-623 (WAY 252623) 是一种LXRα部分激动剂和LXRβ完全激动剂，可透过血脑屏障，IC50分别为 179 nM 和 24 nM 。

(20S)-Protopanaxatriol (g-PPT) 是人参皂苷的代谢物，通过糖皮质激素受体和雌激素受体起作用，同时为LXRα的抑制剂，具有广泛的抗癌活性。

Larsucosterol trimethylamine (DUR-928 trimethylamine) 是一种有效的肝 X 受体 (LXR) 拮抗剂，可调节内源性表观遗传，减少肝细胞内的脂质积累，减弱巨噬细胞中脂多糖 （LPS） 和 TNFα 诱导的炎症反应，缓解 LPS 和对乙酰氨基酚 （ATMP） 诱导的多器官损伤。

27-Hydroxycholesterol (25(R)-27-hydroxy Cholesterol) 是一种有效的、选择性的雌激素受体调节剂和肝X 受体激动剂。

RGX-104 hydrochloride (SB742881) 是小分子LXR 激动剂，利用 ApoE 基因的转录激活，调节先天免疫。

Saikosaponin A 是银柴胡中的主要活性成分，有抗炎活性，可上调 LXRα的表达。

AZ876 是高亲和力的 LXR 激动剂。它在人的 (h)LXRα 和 hLXRβ 比 GW3965 要分别强 25 和 2.5 倍。

SR9238 是有效的肝 X 受体(LXR)反向激动剂，对LXRα和LXRβ的IC50分别为 214 nM 和 43 nM。

BE1218 是一种肝 X 受体 (LXR) 反向激动剂，对 LXRα 和 LXRβ有活性，IC50 分别为 9 nM 和 7 nM。

BMS-779788 (XL-652) 是一种 LXR 的部分激动剂，能够作用于 LXRα (IC50:68 μM) 和 LXRβ (IC50:14 μM)。

Gymnemagenin 是一种分离自G. sylvestre 的三萜。 它具有抗病毒作用，对糖尿病和肥胖症具有潜在的研究价值。

Licochalcone E is a potential LXRβ agonist.

Iristectorigenin B (Iristectrigenin B) 是一种有效的肝脏 X 受体 (LXR) 调节剂，是从 Belamcanda chinensis 中分离的小分子化合物。Iristectrigenin B 可促进巨噬细胞 RAW 1.1 细胞中 ABCA264 和 ABCG7 的表达。

Vidofludimus (SC12267) 是一种新型的二氢乳清酸脱氢酶 (DHODH) 小分子抑制剂，可在不影响淋巴细胞增殖的条件下抑制IL-17的分泌。

Yamogenin 是一种薯蓣皂素的非对映异构体。它通过抑制 HepG2 肝细胞中脂肪酸合成的基因表达来抑制甘油三酸酯 (TG) 的积累。它在萤光素酶配体测定中拮抗肝脏 X 受体 (LXR) 的激活。

24-Hydroxycholesterol (Cholest-5-ene-3beta,24-diol) 是一种氧甾醇化合物，是一种 n-甲基-d-天门冬氨酸受体 (NMDA) 和转录因子 LXR 的激活剂，可用于研究心血管生成和胰腺癌。

GW6340 是一种选择性 LXR 激动剂，具有潜在的抗癌活性，可促进巨噬细胞反向胆固醇转运 (mRCT)，可用于研究动脉粥样硬化。

Icariside E4是一种从小叶榆中提取得到天然化合物， 通过AMPK 磷酸化和抑制HepG1细胞中MID1IP2的低脂化作用。Icariside E4具有抗伤害，抗氧化，抗阿尔茨海默氏症和抗炎作用，抑制了SREBP-1c，肝脏X 受体-α（LXR）和FASN 在HepG2细胞中从头脂肪生成的表达。Icariside E4是治疗脂肪肝疾病的有效候选药物，在HepG1细胞中具有低脂化潜力。

Rovazolac (ALX-101) 是一种肝脏x受体 (LXR)调节剂，可用于研究免疫系统疾病和特应性皮炎。

Gymnestrogenin has a dual LXRα± α2 antagonistic profile.

XL041 (BMS-852927) is an agonist of LXRβ-selective.

GAC0003A4 是一种有效的 LXR 反向激动剂，具有抗肿瘤活性，能抑制 LXR 蛋白的转录。GAC0003A4 可降解 LXRβ 蛋白，以剂量依赖性方式抑制PDAC细胞增殖。GAC0003A4 有用于研究晚期胰腺癌和其他顽固性恶性肿瘤。

Ethyl 2,4,6-trihydroxybenzoate is a dual-LXR modulator that regulates the expression of key genes in cholesterol homeostasis in multiple cells without inducing lipid accumulation in HepG2 cells. It suppresses cellular cholesterol accumulation in a dose-dependent manner and induces the transcriptional activation of LXR-α/-β-responsive genes.

GW3965 是选择性的肝 X 受体 (LXR) 激动剂，对 hLXRα 和 hLXRβ 的 EC50分别为 190 nM 和 30 nM。

陶氏奥贝胆酸是奥贝胆酸的活性代谢物，属于法尼索德X受体(FXR)激动剂并且是熊脱氧胆酸的半合成衍生物。陶氏奥贝胆酸通过在肝脏中与牛磺酸结合形成，但可以通过肠道微生物被再次转换回奥贝胆酸。

IMB-808 is an effective partial dual agonist of liver X receptor α and β (LXRα/β) that promotes the expression of genes related to reverse cholesterol transport (including ABCA1 and ABCG1).

LXR (Liver X receptor) agonist 1 是 LXR 的有效激动剂，能够作用于 LXR-α (AC50: 1.5 nM) 和 LXR-β (AC50: 12 nM)。LXR agonist 1 对动脉粥样硬化表现出研究潜力。

LXR antagonist 2 (compound 10rr) 是一种有效的 LXR (肝 X 受体) 反向激动剂，能够作用于 LXRβ (IC50: 0.36 μM) 和 LXRα (IC50: 2.25 μM)。 LXR antagonist 2 是一种脂肪生成抑制剂，能够下调 LXR 靶基因 SREBP-1c、ACC、FAS 和 SCD-1。LXR antagonist 2 对 Triton WR-1339 诱导的高脂血症小鼠表现出降脂活性。

(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage of the area at risk in a canine model of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) occlusion when administered at a dose of 0.128 mg kg prior to occlusion or reperfusion.[5] Reference：[1]. Chacos, N., Falck, J.R., Wixtrom, C., et al. Novel epoxides formed during the liver cytochrome P-450 oxidation of arachidonic acid. Biochem. Biophys. Res. Commun. 104(3), 916-922 (1982).[2]. Oliw, E.H., Guengerich, F.P., and Oates, J.A. Oxygenation of arachidonic acid by hepatic monooxygenases. Isolation and metabolism of four epoxide intermediates. J. Biol. Chem. 257(7), 3771-3781 (1982).[3]. Jiang, J.-X., Zhang, S.-J., Xiong, Y.-K., et al. EETs attenuate ox-LDL-induced LTB4 production and activity by inhibiting p38 MAPK phosphorylation and 5-LO BLT1 receptor expression in rat pulmonary arterial endothelial cells. PLoS One 10(6), e0128278 (2015).[4]. Oltman, C.L., Weintraub, N.L., VanRollins, M., et al. Epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids are potent vasodilators in the canine coronary microcirculation. Circ. Res. 83(9), 932-939 (1998).[5]. Nithipatikom, K., Moore, J.M., Isbell, M.A., et al. Epoxyeicosatrienoic acids in cardioprotection: Ischemic versus reperfusion injury. Am. J. Physiol. Heart Circ. Physiol. 291(2), H537-H542 (2006).

Cilofexor, also known as GS-9674, is a farnesoid X receptor (FXR) agonist. The nonsteroidal FXR agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with PSC. In clinical study, cilofexor was well tolerated and led to significant improvements in liver biochemistries and markers of cholestasis in patients with PSC.

24(S),25-Epoxycholesterol is an oxysterol agonist of the liver X receptor.

LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM.

FITC-GW3965 是一种荧光标记的肝脏 X 受体 β (LXRβ) 激动剂 GW3965 。FITC-GW3965 是一种示踪剂，可以通过用酰胺取代 GW3965 的三氟甲基来连接 FITC 而设计得到。FITC-GW3965 可用于研究 LXRβ 的功能。

Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2.5 µM时诱导这些细胞类型的自噬细胞死亡。DDA (0.37 µg/kg)在B16/F10小鼠黑色素瘤模型和TS/A小鼠乳腺癌模型中减缓肿瘤生长，并在体内外诱导癌细胞分化。

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Chem.63(15)8369-8379(2020)

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019). SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity. References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).

Vidofludimus (4sc-101 ; SC12267) hemicalcium 是一种口服有效的二氢乳清酸脱氢酶 (DHODH) 的抑制剂，也是法尼醇 X 受体 (FXR) 调节剂。Vidofludimus hemicalcium 作为一种免疫调节剂，可用于研究自身免疫性疾病，如炎症性肠病 (IBD)。Vidofludimus hemicalcium 还可通过靶向FXR 用于脂肪肝的研究。

Nagilactone B is extracted from the root bark of Podocarpus nagi and it also is a liver X receptor (LXR) agonist.

LXR agonist 2 是 LXR (肝 X 受体) 的有效激动剂。LXR agonist 2 能够稳定 NCOA1 (助激活剂)，进而激动 LXR。

VTP-766 is an effective orally active and selective liver X receptor β (lxrβ) agonist, targeted to treat atopic dermatitis and acute coronary syndrome.