nos in 1 

NOS-IN-1 (2-Imino-4-methylpiperidine acetate) 是有效的、具有口服活性的一氧化氮合酶 (NOS) 的抑制剂。NOS-IN-1抑制人 iNOS (hiNOS)，hnNOS 和 heNOS 的 IC50 分别为 0.1 μM，0.2 μM 和1.1 μM。

NOS1-IN-1（nNOS Inhibitor I） 是一种强效、选择性和细胞渗透性 nNOS 抑制剂（Ki：120 nM）。NOS1-IN-1 对 eNOS 的 Ki 值为 39 μM，对 iNOS 的 Ki 值为 325 μM。

iNOs-IN-1 (YPW) 是一种诱导型一氧化氮合酶 (inducible nitric oxide synthase,iNOS) 的有效抑制剂，具有抗炎作用。iNOs-IN-1 在小鼠巨噬细胞中，能够以剂量依赖性的方式明显抑制 IL-6 和 iNOS 的表达，对 LPS 诱导的 NO 生成也具有抑制作用。

Ebselen (CCG-39161) 是一种谷胱甘肽过氧化物酶模拟物，是电压依赖性钙通道阻断剂。它抑制Mpro 和COVID-19病毒，是HIV-1衣壳 CTD 二聚化的抑制剂，具有抗炎、抗癌和抗氧化活性。

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators.[1],[2]Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EET which are prime candidates for the actual active mediator.[3] However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic acid have been little studied relative to arachidonate epoxygenase metabolites. (±)16(17)-EpDPA is the DHA homolog of (±)14(15)-EpETrE, derived via epoxidation of the 16,17-double bond of DHA. The EDHF activity of (±)16(17)-EpDPA has not yet been determined. The epoxygenase metabolites of DHA have also been detected in a mouse inflammation model.[4]

9(E),11(E)-12-nitro Conjugated linoleic acid (9(E),11(E)-12-nitro CLA) is a nitrated fatty acid. It is formed from 9(Z),11(E)-CLA upon exposure to acidified nitrite, peroxynitrite, gaseous nitrogen dioxide, or a combination of myeloperoxidase, hydrogen peroxide, and nitrite.1It is also formed in LPS-stimulated RAW 264.7 macrophages, an effect that can be reduced by the nitric oxide synthase (NOS) inhibitor L-NAME .29(E),11(E)-12-nitro CLA has been found in human plasma. 1.Woodcock, S.R., Salvatore, S.R., Bonacci, G., et al.Biomimetic nitration of conjugated linoleic acid: Formation and characterization of naturally occurring conjugated nitrodienesJ. Org. Chem.79(1)25-33(2014) 2.Bonacci, G., Baker, P.R.S., Salvatore, S.R., et al.Conjugated linoleic acid is a preferential substrate for fatty acid nitrationJ. Biol. Chem.287(53)44071-44082(2012)

NOS-IN-2 (Compound 4i) 是一个强效的、选择性的由 imidamide 衍生的NOS 抑制剂，对iNOS 的IC50值为20 μM。NOS-IN-2 不抑制 eNOS，几乎没有毒性，可用于研究炎症性疾病。

NOS-IN-3 是一个强效的、选择性的由 imidamide 衍生的NOS 抑制剂，对iNOS 的IC50值为20 µM。 NOS-IN-3 不抑制eNOS，几乎没有毒性，可用于研究治疗可诱导亚型涉及的疾病，如感染性休克。

亚甲蓝（Basic Blue 9）水合物，作为鸟苷酸环化酶（sGC）、单胺氧化酶A（MAO-A）及NO合酶（NOS）的抑制剂，常用于医疗作为血管加压剂及染料。该化合物通过影响一氧化氮合成酶 鸟苷酸环化酶信号通路，能够减少脉冲前抑制，同时作为一种氧化还原循环化合物，具有穿透血脑屏障的能力，并作为Tau蛋白聚集的抑制剂，有助于缓解脑水肿、减轻小胶质细胞活化和神经炎症。

Aminoguanidine hemisulfate 作为NOS及ROS的抑制剂，能够在体外有效清除ANE诱导的ROS生成，因此它被广泛应用于癌症研究领域。

GW274150 (dihydrochloride) 是高效、选择性的 NADPH 依赖型人诱导型一氧化氮合成酶 (iNOS) (Kd=40 nM) 抑制剂，具有口服活性，同时对大鼠 (iNOS) 也有效。相较于人和大鼠的内皮一氧化氮合酶 (eNOS) 及神经元一氧化氮合酶 (nNOS)，其效力显著较低。GW274150 (dihydrochloride) 在急性肺损伤炎症模型中具有保护作用。