stearoyl-coa desaturase

GSK1940029 (SCD inhibitor 1) 是酰基-辅酶A 去饱和酶 (SCD) 抑制剂。

A939572 是口服具有活性的硬脂酰 CoA 去饱和酶 1SCD1抑制剂，对mSCD1和hSCD1的IC50分别为 <4 nM 和 37 nM。

SLC13A5-IN-1 是柠檬酸钠协同转运蛋白 (SLC13A5)选择性抑制剂，在 HepG2 细胞中阻断 14C-柠檬酸盐摄取的 IC50 : 0.022 μM。

SSI-4为SCD1 (硬脂酰辅酶A去饱和酶1) 抑制剂，能够通过11C标记，用于SCD1体内小动物PET CT成像的配体。

CAY10566 是选择性的、口服具有活性的硬脂酰辅酶 A 去饱和酶 1 抑制剂，在小鼠和人酶测定中IC50分别为 4.5 和 26 nM。它具有显著的细胞活性，可阻断 HepG2 细胞中饱和长链脂肪酸-CoAs (LCFA-CoAs) 向单不饱和 LCFA-CoAs 的转化 。

PluriSIn 1 (NSC 14613) 是一种酰基-辅酶 A 去饱和酶抑制剂，是一种多能细胞特异性的抑制剂。

XEN723 是新型的硬脂酰辅酶 A 去饱和酶的噻唑基咪唑烷酮抑制剂，能够抑制小鼠和 HepG2 细胞的活性，它们的 IC50值分别为 45 和 524 nM。

MK8245 是肝靶向的硬脂酰 -CoA 去饱和酶(SCD)抑制剂，对人 SCD1 和鼠 SCD1 的IC50值分别为 1 nM 和 3 nM，具有抗糖尿病和抗血脂异常的作用。

SCD1 inhibitor-4 是一种具有口服活性的 stearoylCoA desaturase-1 抑制剂，可用于研究糖尿病。

CVT-12012 是口服具有活性的硬脂酰-CoA 去饱和酶抑制剂，能够抑制大鼠微粒体和人 HEPG2 的活性，它们的IC50值分别为 38 nM，6.1 nM。

MF-438 是一种口服具有活力的 stearoyl-CoA desaturase 1 抑制剂，其对 rSCD1 的 EC50值为 2.3 nM。

Elemicin (Elemicine) 是广泛分布于许多草药和香料中的一种烯基苯。它是芳香族食品中的主要成分之一，具有抗微生物，抗氧化剂和抗病毒活性，有遗传毒性和致癌性。它通过代谢激活抑制硬脂酰辅酶 A 去饱和酶 1。

YTX-465 是有效的硬脂酰辅酶 A 去饱和酶 (Ole1 SCD) 抑制剂，抑制 Ole1 和 SCD1的IC50=分别为 0.039 μM 和 30.4 μM。YTX-465在帕金森病和其他突触核蛋白病领域有研究的价值。

PFM046 是一种肝 X 受体 (LXR) 的拮抗剂，能够抑制 LXRα 和 LXRβ 的活化，其 IC50 分别为 2.04 μM 和 1.58 μM。此外，PFM046 可下调 SCD1 和 FASN 的表达，上调 ABCA1 的表达，并在小鼠模型中显示出抗肿瘤活性。

SW209049 是一种硬脂酰辅酶A 9-去饱和酶抑制剂。 SW209049 对H2122细胞表现出有效的活性，IC50为0.13uM。

Sterculic acid 是一种硬脂酰辅酶 A 去饱和酶 1 (SCD1) 抑制剂。Sterculic acid 剂量依赖性抑制 delta-9 去饱和酶 (Δ9D) 活性，IC50值为 0.9 μM。

MK-8245 analog 是 MK-8245 的类似物，MK-8245 是一种肝脏靶向的硬脂酰辅酶 A 去饱和酶 (SCD) 抑制剂。它可用于治疗血脂异常和糖尿病。

CVT-11127 是 SCD 抑制剂。它将细胞周期阻滞在 G1 S 期，诱导细胞凋亡。它可用于肺癌的研究。

Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants. Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid . Jacaric acid induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 μM). It increases the production of reactive oxygen species, and cytotoxicity is abolished by the antioxidant α-tocopherol, suggesting that apoptosis results from oxidative stress. Jacaric acid is metabolized in vivo to conjugated linoleic acid , which is also cytotoxic to cancer cells. Jacaric acid inhibits cyclooxygenase-1 in vitro (Ki = 1.7 μM) and, with long term feeding, decreases stearoyl-CoA desaturase expression and activity in mice.

MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. IC50 value: 1 nM (hSCD1) Target: SCD1 in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay. in vivo: Administration of MK-8245 at 10 mg kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg kg.

XEN103 is a potent and selective Stearoyl-CoA Desaturase-1 inhibitor.

SW208108 is a tumor-specific irreversible inhibitor of stearoyl CoA desaturase (SCD).

SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production in the H2122 wild-type and nonobese diabetic severe combined immunodeficiency (NOD-SCID) mouse xenograft models when administered at doses of 20 and 6 mg kg, respectively.

8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland microsomes (IC50= 31 μM).4 1.Crombie, L., and Holloway, S.J.The biosynthesis of calendic acid, octadeca-(8E,10E, 12Z)-trienoic, acid, by developing marigold seeds: origins of (E,E,Z) and (Z,E,Z) conjugated triene acids in higher plantsJ. Chem. Soc. Perk. T. 12425-2434(1985) 2.Yasui, Y., Hosokawa, M., Kohno, H., et al.Growth inhibition and apoptosis induction by all-trans-conjugated linolenic acids on human colon cancer cellsAnticancer Res.26(3A)1855-1860(2006) 3.Shinohara, N., Ito, J., Tsuduki, T., et al.Jacaric acid, a linolenic acid isomer with a conjugated triene system, reduces stearoyl-CoA desaturase expression in liver of miceJ. Oleo Sci.61(8)433-441(2012) 4.Nugteren, D.H., and Christ-Hazelhof, E.Naturally occurring conjugated octadecatrienoic acids are strong inhibitors of prostaglandin biosynthesisProstaglandins33(3)403-417(1987)