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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T23283	2-Methoxyidazoxan monohydrochloride RX 821002 hydrochloride	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	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)。
T12617L	(R)-CR8 (R)-CR8,(R)-Isomer,(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,CR8	Apoptosis; CDK	Apoptosis; Cell Cycle/Checkpoint
	(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。
T70540	Pinokalant LOE-908	SARS-CoV; TRP/TRPV Channel	Membrane transporter/Ion channel; Microbiology/Virology
	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。
T28793	SKF-80723 HBr SKF80723 Hydrobromide,SKF 80723 HBr,SKF-80723 Hydrobromide,SKF 80723 Hydrobromide
	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.
T69456	Melagatran monohydrate
	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.
T70329	SH-11037
	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
T28251	ONO-8809 ONO8809
	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
T71811	Lobaric acid
	Lobaric acid is a depsidone metabolite that has been isolated from Stereocaulon lichen species with antioxidant, antiproliferative, antiviral, and enzyme inhibitory activites. It scavenges superoxide radicals in a cell-free assay (IC50 = 97.9 μmol) and inhibits proliferation in a panel of leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic, and lung cancer cell lines (EC50s = 15.2-63.9 μg/ml). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50 = 0.87 μM for the h...
T36357	Dimethyldioctadecylammonium (bromide)
	Dimethyldioctadecylammonium (DDA) is a cationic amphipathic lipid. DDA liposomes containing an Ag85B-ESAT-6 antigen induce antigen deposition at an intramuscular or subcutaneous injection site in mice, increasing immune cell exposure to the antigen. In a guinea pig model of M. tuberculosis infection, spleen bacterial load is reduced and lung and spleen lesion numbers are decreased when the mycobacterial lipid antigens Ac2SGL and PIM2 are administered in liposomes comprised of DDA and a synthetic...
T38274	Papyracillic Acid
	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 f...
T35985	CAY10487
	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....
T60854	ENMD-1068 hydrochloride
	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。
T37013	(+/-)-PPCC oxalate
	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 PMI...
T83669	PMX-53 TFA AcPhe-[Orn-Pro-D-Cyclohexylalanine-Trp-Arg],AcF-[OPdChaWR],3D53
	PMX-53是一种大环型补体5a (C5a) 类肽模拟物及C5a受体的拮抗剂（IC50 = 0.3 µM）。它能抑制C5a诱导的人类分离性多形核白细胞（PMNs）中的髓过氧化物酶（MPO）分泌。在大鼠腹膜亚瑟斯反应模型中，PMX-53（10 mg/kg, p.o.）能够抑制血管渗漏、多形核白细胞浸润以及腹膜TNF-α和IL-6的产生。在3-硝基丙酸（3-NP）诱导的亨廷顿病大鼠模型中，它能减少体重损失和厌食，抑制纹状体退化。PMX-53（3 mg/kg）还能在ApoE-/-小鼠中减小动脉粥样硬化斑块大小和脂质含量。
T83688	R 715 TFA [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
	R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩（pA2 = 8.49）。R 715（200、400及600 µg/kg）通过尾部闪烁测试减少了由链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白（MOG）（35-55）（MOG35-55）抗原肽诱导的实验性自体免疫性脑炎（EAE）小鼠模型中，通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率，改善对称步态，并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715（0.01 nmol/动物，脑室内）能在自发性高血压大鼠中降低平均动脉血压并增加心率。

化合物

2-Methoxyidazoxan monohydrochloride

Cat.No: T23283

Synonym: RX 821002 hydrochloride

Target: Adrenergic Receptor

Cat.No: T12617L

Synonym: (R)-CR8,(R)-Isomer,(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,CR8

Target: Apoptosis, CDK

Cat.No: T70540

Synonym: LOE-908

Target: SARS-CoV, TRP/TRPV Channel

Cat.No: T28793

Synonym: SKF80723 Hydrobromide,SKF 80723 HBr,SKF-80723 Hydrobromide,SKF 80723 Hydrobromide

Melagatran monohydrate

Cat.No: T69456

Cat.No: T70329

Cat.No: T28251

Synonym: ONO8809

Cat.No: T71811

Dimethyldioctadecylammonium (bromide)

Cat.No: T36357

Papyracillic Acid

Cat.No: T38274

Cat.No: T35985

ENMD-1068 hydrochloride

Cat.No: T60854

(+/-)-PPCC oxalate

Cat.No: T37013

Cat.No: T83669

Synonym: AcPhe-[Orn-Pro-D-Cyclohexylalanine-Trp-Arg],AcF-[OPdChaWR],3D53

Cat.No: T83688

Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

Cat. No.	Product Name	Target	Signaling Pathways
T36489	Malformin A
	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 proliferati...

天然产物

Cat.No: T36489

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