concentration ratio

4-Hydroxyantipyrine 是在氨基比林的氧化脱氨过程中形成的。

AGI-026（AGI-12026）是一种新型和有效的突变体异柠檬酸脱氢酶mIDH1 2双重抑制剂，具有口服和穿透血脑屏障的优点，脑组织中的药物浓度与血浆浓度的比值（脑 血浆比）达到 1.5，能够减少致癌代谢物 d-2-羟基戊二酸（2-HG） 的积累，用于研究mIDH胶质瘤。

MitoA is a ratiometric mass spectrometry probe that can be used for assessing changes in H2S within mitochondria in vivo. MitoA contains a triphenylphosphonium cation component that drives its accumulation in mitochondria where its aryl azide moiety selectively reacts with H2S to produce an amine product, MitoN. Quantifying the MitoN MitoA ratio by LC-MS MS reflects the mitochondrial matrix H2S concentration. In a mouse model of acute myocardial infarction with MitoA administered prior to ischemia, the MitoN MitoA ratio is increased only in the region of ischemia.

PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.)

20-Hydroxylucidenic acid E2 是一种在 Ganoderma ludicum 中发现的三萜类化合物，对 TPA 诱导的炎症具有显著的抑制作用。此外，20-Hydroxylucidenic acid E2 能抑制 TPA 诱导的 EBV 早期抗原表达，IC50 为 290 mol ratio 32 pmol TPA（即当此化合物的摩尔浓度为 TPA (32 pmol) 的 290 倍时，能抑制 50% 的 EBV 早期抗原表达）。20-Hydroxylucidenic acid E2 可用于抗炎和抗癌研究。

This novel compound is an orally bioavailable antagonist of P2X3 P2X2 3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2 3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2 3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1 2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smooth muscle cell) proliferation and migration in vitro and in neointimal formationin vivo[3]. CGP 53716 inhibited serum-induced cell growth in RASMC (rat aortic smooth muscle cells). And it completely blocked PDGF-BB tyrosine receptor autophosphorylation in RASMC and 3T3 cells, PDGF-BB-induced phosphorylation of mitogen-activated protein kinase at 1 μM in RASMC and inhibited PDGF-BB-induced c-Fos protein expression at 1 μM in RASMC; consistent with inhibition of PDGF-BB-induced DNA synthesis. Further, CGP 53716 inhibited PDGF-BB-, bFGF- and EGF-induced DNA synthesis in a concentration-dependent manner in each cell line. And it showed a 2- to 4-fold selectivity for PDGF-BB-stimulated DNA synthesis over bFGF or EGF in RASMC or 3T3 cells[1]. CGP 53716 inhibited dose dependently tyrosine phosphorylation of both the known PDGFRs: the PDGFR-α and PDGFR-β. After rat carotid artery ballooning injuryin vivo, the migration of alpha-actin-positive cells on the luminal side of internal elastic lamina was decreased with 50 mg kg day of CGP 53716 from 38 ± 10 (control group) to 4 ± 2. Intima media ratio was inhibited by 40% after 14 days in the CGP 53716-treated group (P=0.028) after rat aortic denudation[3].

Antimicrobial agent-34（compound 4h）是一种高效抗菌剂，其MIC值为1-4 μg mL，clogP为9.14。该化合物在血浆中展示出优异的稳定性，其HC50值为131.1 μg mL，并且具有出色的膜选择性（HC50 MIC比值为65.6），能够迅速杀灭细菌。Antimicrobial agent-34的抗菌机制涉及破坏细菌的细胞膜完整性，增加细胞内活性氧的生成，以及导致蛋白质和DNA的泄漏，最终引致细菌死亡。在金黄色葡萄球菌ATCC43300引起的小鼠败血症模型中，Antimicrobial agent-34表现出显著的体内抗菌效果。

Emetine hydrochloride (NSC 33669)，一种从ipecac根部提取的生物碱，用于临床上作为催吐及抗原生动物药物。它能够降低HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2)和BRD4，抑制细胞自噬，并展现抗疟疾、抗病毒、抗细菌及抗变形虫效果。

α-Synuclein inhibitor 4 (compound 3gh) is a highly effective and blood-brain barrier-permeable inhibitor of α-Synuclein aggregation. It displays potent activity, with an IC50 value of 0.98 μM, and exhibits a remarkable inhibition ratio of 91.2% at a concentration of 30 μM [1].

MitoP is a phenol product produced by the reaction of H2O2 with the ratiometric mass spectrometry probe MitoB . MitoB contains a triphenylphosphonium cation component that drives its accumulation in mitochondria where its arylboronic moiety selectively reacts with H2O2 to produce MitoP. Quantifying the MitoP/MitoB ratio by LC-MS/MS reflects the mitochondrial matrix H2O2 concentration.

Sterculic acid methyl ester, an ester derivative of sterculic acid known for inhibiting Δ9 desaturase, has been found to adversely affect and exhibit toxicity towards R. opacus bacteria at a concentration of 0.75 mM. It not only hampers bacterial growth but also modifies fatty acid composition by reducing stearate and oleate levels, increasing the palmitate ratio, and decreasing overall fatty acid content at 0.25 or 0.5 mM concentrations. Additionally, at 50 ppm, Sterculic acid methyl ester enhances the tumor growth-promoting effects of aflatoxin Q1 in rainbow trout, indicating a synergistic interaction between the two compounds. [Matreya, LLC. Catalog No. 1236]

Sphingosines are long-chain base precursors of cellular sphingolipids used directly in the synthesis of ceramide, which in combination with sialic acid forms ganglioside. Sphingosine can exist in four stereoisomers, however only sphingosine occurs naturally. Compared to other sphingolipids throughout the body, which are predominantly composed of C-18 sphingosine, only central nervous system (CNS) gangliosides contain significant amounts of sphingosine. The concentration of sphingosine within mammalian brain gangliosides apparently increases with developmental maturation. Furthermore, the ratio of C-18 to C-20 sphingosine in the brain is thought to be related to some nervous system degeneration processes.

Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50 IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 + - 0.08 micromol l after 24 h) than As(2)O(3) (IC50 = 1.60 + - 0.23 micromol l after 24 h) or melarsoprol (IC50 = 1.44 + - 0.08 micromol l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.

M4K2281是一种针对ALK2的高效选择性抑制剂，其半抑制浓度（IC50）为2纳摩尔。在生化及细胞分析中，M4K2281及M4K2308均展现出针对ALK2的高效作用。此外，M4K2281的大脑至血浆比率介于中等至高。