A939572
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A939572是一种有效的和可口服的硬脂酰辅酶A去饱和酶1(SCD1)抑制剂,IC50值为37 nM[1]。
SCD是一种微粒体酶,催化单不饱和脂肪酸的生物合成。SCD1是SCD家族的成员,由饮食和激素因素所调节,在脂质代谢和体重控制中发挥重要作用。因此,SCD1是治疗肥胖和糖尿病的靶标。A939572是合成的SCD1抑制剂,比其母体化合物具有更好的抑制活性和亲油性。A939572抑制小鼠和人的SCD1,IC50值分别为 < 4 nM和37 nM。此外,A939572对SCD1的辅酶细胞色素b5和细胞色素b5还原酶没有抑制活性。A939572直接和特异性地与SCD1相互作用。而且,A939572在小鼠中具有很高的口服生物利用度[1]。
参考文献:
[1] Xin Z, Zhao H, Serby M D, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorganic & medicinal chemistry letters, 2008, 18(15): 4298-4302.
- 1. Yuki Katoh, Tomonori Yaguchi, et al. "Inhibition of stearoyl-CoA desaturase 1 (SCD1) enhances the antitumor T cell response through regulating β-catenin signaling in cancer cells and ER stress in T cells and synergizes with anti-PD-1 antibody." J Immunother Cancer. 2022 Jul;10(7):e004616. PMID: 35793868
- 2. Ling Tao, Mahmoud A. Mohammad, et al. "MYCN-driven fatty acid uptake is a metabolic vulnerability in neuroblastoma." Nat Commun. 2022 Jun 28;13(1):3728. PMID: 35764645
- 3. Magtanong L, Ko PJ, et al. "Exogenous Monounsaturated Fatty Acids Promote a Ferroptosis-Resistant Cell State." Cell Chem Biol. 2018 Dec 11. pii:S2451-9456(18)30438-0. PMID: 30686757
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 387.86 |
Cas No. | 1032229-33-6 |
Formula | C20H22ClN3O3 |
Solubility | insoluble in H2O; ≥17.15 mg/mL in DMSO; ≥2.5 mg/mL in EtOH with ultrasonic |
Chemical Name | 4-(2-chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide |
SDF | Download SDF |
Canonical SMILES | CNC(C1=CC(NC(N2CCC(OC3=CC=CC=C3Cl)CC2)=O)=CC=C1)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
动物实验 [1]: | |
动物模型 |
ob/ob小鼠 |
给药剂量 |
10 mg/kg;每天2次 |
实验结果 |
在ob/ob小鼠中,A939572降低去饱和指数 (18:0/18:1n9)。此外,A939572呈剂量依赖性地降低甘油三酯的去饱和指数。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Xin Z, Zhao H, Serby M D, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorganic & medicinal chemistry letters, 2008, 18(15): 4298-4302. |
质量控制和MSDS
- 批次: