lesion

(R)​-​CR8 ((R)-Isomer) 是 Roscovitine 类似物，是CDK1/2/5/7/9抑制剂。它作为一种分子胶降解剂来消耗细胞周期蛋白 K。它诱导细胞凋亡并具有神经保护作用。

L-Albizziin (2-Methoxyidazoxan monohydrochloride) 是高效的 alpha 2r 肾上腺素受体选择性拮抗剂，对 imidazoline 拮抗作用很小或没有。它对 (豚鼠) alpha 2D 肾上腺素受体 (pKd9.7) 的亲和力明显高于 (兔子) alpha 2A 肾上腺素受体 (pKd8.2)。

Epinastine hydrochloride (WAL-801CL HCl) 是抗组胺剂和肥大细胞稳定剂，是一种可口服的选择性组胺 H1 受体拮抗剂，可抑制 IL-8 释放，具有抗过敏作用。

PKR-IN-C16 是一种特异性蛋白激酶抑制剂。它能够抑制 PKR 的自磷酸化，解除 PKR 在原代神经元细胞培养中诱导的翻译阻断。

PFI-4是一种可渗透细胞的选择性BRPF1溴结构域抑制剂，IC50为 80 nM，作用于BRPF1比作用于其他溴结构域选择性强 100 多倍。

TH1085是OGG1的增强剂。 TH1085 刺激 DNA 修复并保护细胞免受环境危害百草枯 (PQ) 的侵害。

Pinokalant (LOE-908) 是一种新型非选性阳离子通道抑制剂。Pinokalant 在体内实验中可显著减少皮质梗死体积，可改善缺血半影区的代谢和电生理状态，可减少大鼠大脑中动脉闭塞后急性期磁共振图像上的病变大小。Pinokalant是一种潜在的SARS-CoV-2蛋白酶抑制剂，可用于研究脑卒中。

Beauveriolide III 是一种存在于 Beauveria 属真菌中的环肽类化合物，可抑制脂滴形成（3-10 μM 时）及胆固醇合成（IC50=0.41 μM）。该化合物还能抑制酰基辅酶 A:胆固醇酰基转移酶（ACAT）活性（IC50=5.5 μM），并在 Ldlr-/- 和 ApoE-/- 小鼠模型中减少动脉粥样硬化斑块大小（25-50 mg/kg）。

C-lock-GGFG-DXd 是一种硫醇反应型药物连接剂，GGFG是一种可酶解的肽，进入病灶之后可以使有效载荷 DXd 释放发挥作用，C-lock-GGFG-DXd 常用于抗体-药物偶联物（ADC）的合成。

C-lock-GGFG-Exatecan 是一种硫醇反应型药物连接剂，GGFG是一种可酶解的肽，进入病灶之后可以使有效载荷 Exatecan 释放发挥作用，C-lock-GGFG-Exatecan 常用于抗体-药物偶联物（ADC）的合成。

GI-Y2是一种GSDMD抑制剂，能够抑制氧化低密度脂蛋白 (ox-LDL) 诱导的巨噬细胞焦亡 (Pyroptosis)。在体内，GI-Y2能够以剂量依赖的方式减少ApoE-/-小鼠的动脉粥样硬化斑块，降低主动脉根的病变大小和纤维化程度。GI-Y2 有望用于细胞焦亡和心血管疾病的研究，例如动脉粥样硬化。

A-86929 是一种强效且选择性的多巴胺D1受体激动剂，pKi值为7.3。在6-OHDA诱导的单侧黑质损伤的大鼠模型中，A-86929 可显著诱导旋转行为，并在MPTP诱导的帕金森病狨猴模型中改善运动功能。此外，它在减少可卡因诱导的大鼠渴求行为及改善Haloperidol导致的恒河猴认知缺陷上展现出潜力。A-86929 可用于神经疾病研究。

Dimephosphon 是一种抗炎剂，展现抗组胺 (antihistamine) 和抗血清素 (antiserotonin) 活性。它有助于维持脊髓传导功能，降低病变区域周围脊髓运动神经元的兴奋性。Dimephosphon 能直接激活淋巴管运动，改善淋巴循环，并可用于研究炎症性水肿、急性脊髓损伤和淋巴循环障碍。

Fenpyrazamine 是一种抗真菌剂，具有抗真菌活性、预防活性、内吸活性、抑制病斑发展活性以及持久的药效。其靶点为麦角甾醇生物合成途径中的 3-酮还原酶 (3-keto reductase)。Fenpyrazamine 对灰霉病、茎腐病和褐腐病具有预防作用。

ONO-8809 is a thromboxane A2 receptor antagonist. ONO-8809 inhibited the LTC4-induced airway hyperresponsiveness to histamine in a dose-dependent manner. Macrophage accumulation and matrix metalloproteinase-9 (MMP-9) activity in the stroke-negative area i

SKF-80723 HBr is a D1 receptor agonist. SKF-80723 HBr strongly potentiated the contralateral circling induced by quinpirole in rats with a unilateral 6-hydroxydopamine (6-OHDA) lesion of the medial forebrain bundle.

The early stage of atherosclerosis is characterized by the aggregation of foam cells, so called a fatty streak, in the inner arterial wall. CAY10487 inhibits formation of fatty streak lesions of the thoracic aorta in high cholesterol-fed rabbits without affecting plasma lipid profiles or significantly inhibiting ACAT-1 or ACAT-2 activity. The percent area occupied by the atherosclerotic lesion in rabbits supplemented with 0.05% CAY10487 in the diet was 16.1% compared to 53.5% in control rabbits. CAY10487 also exhibits antioxidant activity, inhibiting copper-mediated oxidation of low-density lipoprotein by about 75% at a concentration of 2 μM.

Dimethyldioctadecylammonium bromide是一种合成的双链阳离子脂质，由带正电的季铵头基和两条长链疏水烷基构成，能够自组装形成脂质体及纳米颗粒体系，常用于基因递送和疫苗佐剂开发，通过与核酸形成复合物促进细胞摄取；此外亦具有表面活性剂和乳化剂应用。

Malformin A is a cyclopentapeptide fungal metabolite that has been found in A. niger and has diverse biological activities. It is a plant growth regulator that induces malformations in plant structure. Malformin A inhibits replication of tobacco mosaic virus (TMV) in local lesion and leaf-disc assays (IC50s = 19.7 and 45.4 μg/ml, respectively). It is cytotoxic to NCI-H460, MIA PaCa-2, MCF-7, SF-268, and WI-38 cancer cells (IC50s = 70, 50, 100, 70, and 100 nM, respectively), inhibits proliferation of PC3 and LNCaP cells (IC50s = 130 and 90 nM, respectively), and induces apoptosis and necrosis in PC3 and LNCaP cells. Malformin A also increases the accumulation of reactive oxygen species, decreases the mitochondrial membrane potential, and induces autophagy in PC3 and LNCaP cells. It is toxic to mice when administered intraperitoneally (LD50 = 3.1 mg/kg) but not orally up to doses of 50 mg/kg.

Selective sigma (σ) receptor ligand. Displays high affinity for σ1; also binds at σ2 sites (Ki = 1.5 nM and 50.8 nM respectively). Selective over a range of receptor types including dopaminergic and muscarinic receptors, DAT and SERT. Prezzavento et al (2007) Novel sigma receptor ligands: synthesis and biological profile. J.Med.Chem. 50 951 PMID:17328523 |Prezzavento et al (2008) A new sigma ligand, (±)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect. Life Sci. 82 549 PMID:18261749 |Antonini et al (2009) Anti-amnesic properties of (±)-PPCC, a novel sigma receptor ligand, on cognitive dysfunction induced by selective cholinergic lesion in rats. J.Neurochem. 109 744 PMID:19245662

Papyracillic acid is a fungal metabolite and a derivative of penicillic acid originally isolated fromL. papyraceumand has antibiotic, antifungal, and phytotoxic activities.1,2It is active against the bacteriaX. campestrisandB. subtilisand the fungusC. tropicalisin a disc assay when used at a concentration of 5 μg/disc.2Papyracillic acid (1 mg/ml) induces necrotic lesion formation in a panel of 10 plants. 1.Shan, R., Anke, H., Stadler, M., et al.Papyracillic acid, a new penicillic acid analogue from the Ascomycete Lachnum papyraceumTetrahedron52(30)10249-10254(1996) 2.Evidente, A., Berestetskiy, A., Cimmino, A., et al.Papyracillic acid, a phytotoxic 1,6-dioxaspiro[4,4]nonene produced by Ascochyta agropyrina Var. nana, a potential mycoherbicide for Elytrigia repens biocontrolJ. Agric. Food Chem.57(23)11168-11173(2009)

ENMD-1068 hydrochloride 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride 可通过抑制TGF-β1/Smad 信号转导而减少肝星状细胞的活化和胶原蛋白的表达。ENMD-1068 hydrochloride 还能抑制子宫内膜细胞的增殖，并诱导病灶中上皮细胞的凋亡。ENMD-1068 hydrochloride 可用于子宫内膜异位症、肝纤维化的研究。

Melagatran monohydrate is a thrombin inhibitor. Melagatran prevents tissue factor expression in human platelet-monocyte heterotypic complexes. Melagatran reduces advanced atherosclerotic lesion size and may promote plaque stability in apolipoprotein E-deficient mice.

SH-11037 is a novel potent seh inhibitor, effectively blocking key angiogenic properties of human retinal endothelial cells (hrecs), inhibiting choroidal sprouting and significantly suppressing cnv lesion volume