x 25

SRX 251, a vasopressin V1a receptor antagonist, is used potentially for the treatment of primary dysmenorrhea.

Durlobactam sodium salt (ETX2514) 是一种 β-内酰胺酶抑制剂，针对 A 类 KPC-2、C 类 AmpC 和 D 类 OXA-24，IC50 值分别为 4 nM、14 nM 和 190 nM。

NRX-252262 是 β-Catenin 与同源 E3 ligaseSCFβ-TrCP 的相互作用增强剂，能够诱导 β-catenin 的降解，其 EC50=3.8 nM。

NRX-252114 (NRX252114) 能够诱导突变体 β-catenin 的降解。NRX-252114 是一种 β-catenin 与 同源 E3 ligase SCFβ-TrCP 的相互作用的高效增强剂，能够加强 pSer33 S37A β-catenin 与 β-TrCP 的结合，EC50 为 6.5 nM，Kd 为 0.4 nM。

Durlobactam Triethylamine (ETX2514 Triethylamine) 是一种二氮杂双环辛烷β-内酰胺酶抑制剂，可抑制 A、C 和 D 类β-内酰胺。Durlobactam Triethylamine 具有抗真菌感染活性。

GRA Ex-25 (GRA-Ex-25) 是glucagon 受体抑制剂，其对大鼠和人的 glucagon 受体的IC50值分别为 56 和 55 nM。

GATA4-NKX2-5-IN-1 剂量依赖性地抑制 GATA4–NKX2-5转录协同作用(IC50:3 μM)，但不影响参与调节 GATA4 磷酸化的蛋白激酶的活性。它能够调节肥大激动剂诱导的心脏基因表达。

TX-2552为口服型TDP1 (酪氨酰DNA磷酸二酯酶1) 抑制剂,具备IC50为0.62 μM的活性.该化合物能够提升拓扑替康在小鼠骨髓细胞中的断裂活性,并增强其在Krebs-2腹水瘤模型中的抗肿瘤效果.

MBX2546 is an Influenza A Virus Fusion Inhibitor. MBX2546 binds to HA and inhibits HA-mediated membrane fusion. Both binding and stabilization of HA by MBX2546 are required for the inhibition of viral infection. Mutations in MBX2546-resistant influenza A

COX-2 5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent and dual inhibitor of COX-2 5-LOX. It exhibits superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. COX-2 5-LOX-IN-1 displays strong inhibitory activity against COX-1, COX-2, and 5-LOX, with IC50 values of 12.13 μM, 0.4 μM, and 4.96 μM, respectively [1].

COX-2 5-LOX-IN-2 是苯并噻吩-2-基吡唑羧酸衍生物。COX-2 5-LOX-IN-2 (5b) 对COX-2和5-LOX 均有抑制作用。COX-2 5-LOX-IN-2 抑制 COX-1、COX-2 和 5-LOX 的IC50s 分别为 5.40、0.01 和 1.78 μM。COX-2 5-LOX-IN-2 显示出超过塞来昔布和吲哚美辛的镇痛和抗炎活性。

Bexarotene (LGD1069) 是一种高亲和力的选择性类视黄醇 X 受体 (RXR) 激动剂，对 RXRα、RXRβ和 RXRγ的 EC50分别为 33、24和25 nM。它是一种类视黄醇类似物，用于治疗皮肤 T 细胞淋巴瘤的皮肤表现。

Fexaramine 是小分子法尼醇 X 受体 (FXR) 激动剂，EC50为 25 nM，与天然化合物相比，亲和力提高了 100 倍。

Cathepsin X-IN-1 (compound 25) 降低人前列腺癌细胞 PC-3 的迁移且具有较低的细胞毒性，它是组织蛋白酶 X 的有效抑制剂 (IC50 = 7.13 μM)。

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

CX-6258 hydrochloride (Pim-Kinase Inhibitor X) 是一种强效选择性的泛 Pim 激酶抑制剂，对Pim-1、Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。

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。

Apogossypolone (ApoG2) 是一种具有口服活性的Bcl-2 家族蛋白抑制剂，对 Bcl-2, Mcl-1 和 Bcl-XL 的Ki 值分别为 35, 25 和 660 nM。Apogossypolone 具有抗肿瘤活性，可诱导细胞凋亡 (apoptosis) 和 自噬 (autophagy)。Apogossypolone 具有抗真菌活性。

25-Hydroxytachysterol3 是 Vitamin D3 的一种代谢产物。它能够抑制表皮角质细胞和真皮成纤维细胞的增殖，并促进角质形成细胞的分化及抗氧化相关基因的表达。25-Hydroxytachysterol3 能够激活维生素 D 受体 (VDR)、芳烃受体 (AhR)、肝 X 受体 α β (LXRα β) 和过氧化物酶体增殖激活受体 γ (PPARγ)，并刺激 CYP24A1 的表达。

Mn(III)TMPyP is a manganese-porphyrin which acts as a superoxide dismutase (SOD) mimetic and peroxynitrite decomposition catalyst. SOD mimetics described to date are unstable and are capable of catalyzing undesired side-reactions in addition to the dismutation of the superoxide radical (O2-). Mn(III)TMPyP is an SOD mimetic with increased stability to pH and hydrogen peroxide. The rate constant for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M-1s-1 and ~2 x 106 M-1s-1, respectively. Mn(III)TMPyP protected and enhanced the growth of SOD E. coli with a doubling time of 60 minutes (as compared to 240 minutes of the control) at 25 µM.

Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan .1Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay. 1.van Giersbergen, P.L.M., Gnerre, C., Treiber, A., et al.Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptorBr. J. Clin. Pharmacol.54(5)561-562(2002)

Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellular proteins, promotes protein-vesicle interactions, and regulates various G protein-coupled receptor functions.1Red blood cell palmitic acid levels are increased in patients with metabolic syndrome compared to patients without metabolic syndrome and are also increased in the plasma of patients with type 2 diabetes compared to individuals without diabetes.3,4 1.Fatima, S., Hu, X., Gong, R.-H., et al.Palmitic acid is an intracellular signaling molecule involved in disease developmentCell. Mol. Life Sci.76(13)2547-2557(2019) 2.Santos, M.J., López-Jurado, M., Llopis, J., et al.Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patientsAnn. Nutr. Metab.39(1)52-62(1995) 3.Yi, L.-Z., He, J., Liang, Y.-Z., et al.Plasma fatty acid metabolic profiling and biomarkers of type 2 diabetes mellitus based on GC/MS and PLS-LDAFEBS Lett.580(30)6837-6845(2006) 4.Kabagambe, E.K., Tsai, M.Y., Hopkins, P.N., et al.Erythrocyte fatty acid composition and the metabolic syndrome: A National Heart, Lung, and Blood Institute GOLDN studyClin. Chem.54(1)154-162(2008)