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33

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T10979	DCPIB	Potassium Channel; Chloride channel	Membrane transporter/Ion channel
	DCPIB 是选择性可逆体积调节性阴离子通道抑制剂，抑制肿胀激活氯电流，在 CPAE 细胞中，IC50值为 4.1 μM。它能够电压依赖性激活钾离子通道 TREK1 和 TRAAK，抑制 TRESK、TASK1 和 TASK3的 IC50值分别为 0.14、0.95 和 50.72 μM。
T9216	MLT-943 MLT943	MALT	Immunology/Inflammation
	ML-943 是选择性的、口服活性的MALT1 protease 抑制剂。它可抑制 PBMC 或全血中 IL-2 的分泌，PBMC 中抑制的IC50值为 0.07~0.09 μM，全血中抑制的IC50值为 0.6~0.8 μM)。它具有抗炎作用，可用于研究 FcgR 介导的炎症。
T1230	Pamabrom 巴马溴,帕马溴	Others	Others
	Pamabrom 是一种利尿剂，有效成分为8-bromotheophylline，能够缓解月经相关症状。
T24859	TC-AQP1-1	Aquaporin	Membrane transporter/Ion channel
	TC-AQP1-1 是一种通过虚拟筛选鉴定的水通道蛋白 1 通道的阻断剂，并在低微摩尔浓度下抑制非洲爪蟾卵母细胞肿胀试验中通过 hAQP1 的水通量。
T21996	Zoniporide hydrochloride CP-597396 hydrochloride	Sodium Channel	Membrane transporter/Ion channel
	Zoniporide hydrochloride 是一种特异性的 NHE-1 抑制剂，IC50 为 14 nM，是其他 NHE 同工型的 >150 倍特异性。 Zoniporide hydrochloride 对人血小板的 NHE-1 依赖性肿胀的 IC50 为 59 nM。
T5000	Diflucortolone valerate Afusona,戊酸双氟可龙,Diflucortolone 21-valerate	Others; Antibacterial; Antifungal	Microbiology/Virology; Others
	Diflucortolone valerate (Diflucortolone 21-valerate) 是一种强效皮质类固醇，可研究各种皮肤疾病。
T36851L	Peptide5 acetate	Others	Others
	Peptide5 acetate 可减少脊髓损伤后的动物肿胀、星形胶质细胞增生和神经元细胞死亡。 Peptide5 acetate 显着降低啮齿动物离体模型中的脊髓损伤 (SCI) 程度。
T21445	Naphazoline AK-Con,Naphcon-a,Clear Eyes,All Clear,萘甲唑林	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Naphazoline (Naphcon-a) 是一种具有显着 α 肾上腺素能活性的拟交感神经化合物。萘甲唑啉可用作血管收缩剂，当应用于粘膜时可快速减少肿胀。
T0839L	S-(+)-Ketoprofen RP-19583,Dexketoprofen,(S)-(+)-Ketoprofen,(S)-Ketoprofen,(S)-(+)-酮洛芬,右旋酮洛芬	COX	Immunology/Inflammation; Neuroscience
	S-(+)-Ketoprofen ((S)-(+)-Ketoprofen) 抑制 COX-1和 COX-2的IC50值分别为 1.9 和 27 nM。
T35689	MTP 131 acetate	Others	Others
	MTP 131 acetate 是一种小的线粒体靶向四肽。
T69267	Naproxen glucuronide
	Naproxen glucuronide is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid class (the same class as ibuprofen) that relieves pain, fever, swelling, and stiffness. It is a nonselective COX inhibitor.
T21074	Dexamethasone acetate Dexamethasone 21-acetate monohydrate,Decadron-LA,Decadron
	Dexamethasone acetate is an adrenocortical steroid. It is used in the treatment of many conditions, including rheumatic problems, a number of skin diseases, asthma, severe allergies, chronic obstructive lung disease, brain swelling, croup, and antibiotics
T70161	Berotralstat HCl
	Berotralstat HCl is a novel selective inhibitor of plasma kallikrein, blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
T68682	Piriprost
	Piriprost is a leukotriene inhibitor attenuates the smoke-induced increase in alveolar-capillary barrier permeability and decrease in plasminogen activator activity and causes a swelling of type I alveolar epithelium.
T69474	Naproxen ethyl ester
	Naproxen ethyl ester is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid class (the same class as ibuprofen) that relieves pain, fever, swelling, and stiffness. It is a non-selective COX inhibitor.
T36851	Peptide5
	Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 \|Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats....
T78967	Anti-inflammatory agent 40	Parasite	Microbiology/Virology
	Anti-inflammatory agent 40 是潜在的口服抗疟疾(anti-malarial)与抗炎(Anti-inflammatory)化合物，能抑制卡拉胶诱导的足跖肿胀。
T68211	Piroxicam betadex
	Piroxicam betadex is a nonsteroidal anti-inflammatory drug. The mechanism of action of piroxicam is as a cyclooxygenase Inhibitor. It is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. It is used to reduce pain, swelling, and joint stiffness from arthritis. Reducing these symptoms helps you do more of your normal daily activities.
T64264	ISIS 104838
	ISIS 104838 是一种反义寡核苷酸药物，能够抑制肿瘤坏死因子 (TNF-alpha) 的产生，造成类风湿关节炎关节疼痛和肿胀。
T79473	Anti-inflammatory agent 46	NO Synthase	Immunology/Inflammation
	Anti-inflammatory agent 46（compound 7h）是一种能够抑制一氧化氮（NO）生成的化合物，通过与iNOS低能量结合，在体内有效减缓小鼠肿胀（剂量为10 mg/kg）。
T78977	Antitrypanosomal agent 12	Parasite	Microbiology/Virology
	Antitrypanosomal agent 12 是 C20-苯基硫脲化合物，显示出杀锥虫和细胞毒性。该化合物在实现 50% 生长抑制(GI50)时所需浓度为0.22 μM，能在血流形式的锥虫中引起细胞肿胀。
T78061	Peptide5 TFA	Gap Junction Protein	Cytoskeletal Signaling
	Peptide5 TFA，一种connexin 43模拟肽，能够降低动物脊髓损伤后的肿胀、抑制星形胶质细胞增生和神经元死亡。该化合物还可抑制NLRP3炎症小体，具有抗炎作用。
T35869	Berotralstat
	Berotralstat (BCX7353) is a second-generation, synthetic, and orally active plasma kallikrein inhibitor with low toxicity. It is highly specific and effectively used in the research of hereditary angioedema (HAE) attacks. Berotralstat functions by inhibiting the enzymatic activity of plasma kallikrein, which is responsible for the release of bradykinin. This blocking mechanism targets the major biologic peptide involved in the promotion of swelling and pain associated with HAE attacks[1][2].
T68266	BMS-751324
	BMS-751324 是一种p38αMAPK 抑制剂。BMS-751324 含有氨基甲酰基亚甲基连接的前体，含有羟基苯基乙酸 (HPA) 衍生的酯和磷酸盐官能团。BMS-751324 在关节炎大鼠模型中有效抑制足部肿胀，并抑制 LPS 诱导的 TNFα 的生成。
T82017	JAK-IN-34	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	JAK-IN-34 对JAKs具有有效抑制作用，其IC50值分别针对JAK1、JAK2、JAK3、TYK2为0.40、0.83、2.10、1.95 nM 。此外，JAK-IN-34 能够降低关节肿胀，并展现出良好的安全性。
T73544	MPM-1
	MPM-1 是海洋生物 Eusynstyelamides 模拟物，是一种有效的抗癌剂。MPM-1 可通过诱导坏死样死亡，在体外快速杀死癌细胞。MPM-1具有诱导免疫原性细胞死亡的能力。MPM-1在癌细胞中干扰细胞自噬 (autophagy) 和溶酶体膨胀。
T68393	SNX-7081
	NX-7081 is a novel small molecule inhibitor of Hsp90, which blocks components of inflammation, including cytokine production, protein kinase activity, and angiogenic signaling. SNX-7081 showed strong binding affinity to Hsp90 and expected induction of Hsp70. NF-kappaB nuclear translocation was blocked by SNX-7081 at nanomolar concentrations, and cytokine production was potently inhibited. Growth factor activation of ERK and JNK signaling was significantly reduced by SNX-7081. NO production was a...
T60292	Ibuprofen sodium
	Ibuprofen ((±)-Ibuprofen) sodium 是一种口服活性的选择性COX-1抑制剂，IC50值为 13 μM。Ibuprofen sodium 抑制细胞增殖、血管生成，并诱导细胞凋亡 (apoptosis)。Ibuprofen sodium 是一种非甾体抗炎剂和一氧化氮 (NO) 供体。Ibuprofen sodium 可用于疼痛、肿胀、炎症、感染、免疫学、癌症的研究。
T69451	R-130823
	R-130823 is a ighly selective inhibition against mitogen-activated protein kinase p38alpha (IC50=22 nM). The release of tumor necrosis factor-alpha, interleukin-1beta, -6 and -8 was inhibited in lipopolysaccharide-stimulated human blood pretreated by R-130823 , with IC50 values of 0.089, 0.066, 0.95 and 0.16 microM, respectively. R-130823 reduced the established hind paw swelling in rat adjuvant-induced arthritis, while methotrexate showed no suppression. In the same model, R-130823 ameliorated ...
T36713	Streptochlorin
	Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the productio...
T83681	IRBP (1-20) (human, rat) TFA IRBP1-20,Interphotoreceptor Retinoid-Binding Protein (1-20)
	IRBP1-20（1-20）是IRBP的一个十二肽片段，亦称视黄醇结合蛋白3，负责运输视锥细胞中的视黄醇和视黄醛至视网膜色素上皮，参与色素再生。在携带H-2b等位基因型的C57BL/6小鼠中，IRBP1-20用于诱导自身免疫性葡萄膜视网膜炎。IRBP1-20（3 µM）能增加初级小鼠脾淋巴细胞分泌IL-4、IL-5和IL-6的水平。用IRBP1-20免疫并再次挑战，可增加IFN-γ缺乏小鼠的耳部肿胀、眼部血管炎症、免疫细胞浸润和视锥细胞层损伤，以及视网膜脱落。
T61585	Sulindac sodium
	Sulindac (sodium) (MK-231) 是一种非甾体抗炎剂，具有口服活性。Sulindac (sodium) 用于减轻疼痛，肿胀和关节僵硬的关节炎。Sulindac 还用于脊柱关节炎、痛风性关节炎的研究。Sulindac (sodium) 作为一种免疫调节剂，可通过阻断 NF-κB 信号通路下调 PD-L1，调节 pMMR CRC 对抗 PD-L1 免疫治疗的应答，抑制结直肠癌 CRC 的发生发展。 Sulindac 还可通过下调 SIRT1 抑制 TGF-β1-诱导的 EMT，抑制肺癌细胞的迁移和侵袭。
T23800	BI-9627 hydrochloride BIX Hydrochloride,BIX HCl
	BIX HCl is a sodium-hydrogen exchange type 1 inhibitor.

化合物

Cat.No: T10979

Target: Potassium Channel, Chloride channel

Cat.No: T9216

Synonym: MLT943

Target: MALT

Cat.No: T1230

Synonym: 巴马溴,帕马溴

Target: Others

Cat.No: T24859

Target: Aquaporin

Zoniporide hydrochloride

Cat.No: T21996

Synonym: CP-597396 hydrochloride

Target: Sodium Channel

Diflucortolone valerate

Cat.No: T5000

Synonym: Afusona,戊酸双氟可龙,Diflucortolone 21-valerate

Target: Others, Antibacterial, Antifungal

Peptide5 acetate

Cat.No: T36851L

Target: Others

Cat.No: T21445

Synonym: AK-Con,Naphcon-a,Clear Eyes,All Clear,萘甲唑林

Target: Adrenergic Receptor

S-(+)-Ketoprofen

Cat.No: T0839L

Synonym: RP-19583,Dexketoprofen,(S)-(+)-Ketoprofen,(S)-Ketoprofen,(S)-(+)-酮洛芬,右旋酮洛芬

Target: COX

MTP 131 acetate

Cat.No: T35689

Target: Others

Naproxen glucuronide

Cat.No: T69267

Dexamethasone acetate

Cat.No: T21074

Synonym: Dexamethasone 21-acetate monohydrate,Decadron-LA,Decadron

Berotralstat HCl

Cat.No: T70161

Cat.No: T68682

Naproxen ethyl ester

Cat.No: T69474

Cat.No: T36851

Anti-inflammatory agent 40

Cat.No: T78967

Target: Parasite

Piroxicam betadex

Cat.No: T68211

Cat.No: T64264

Anti-inflammatory agent 46

Cat.No: T79473

Target: NO Synthase

Antitrypanosomal agent 12

Cat.No: T78977

Target: Parasite

Cat.No: T78061

Target: Gap Junction Protein

Cat.No: T35869

Cat.No: T68266

Cat.No: T82017

Target: JAK

Cat.No: T73544

Cat.No: T68393

Ibuprofen sodium

Cat.No: T60292

Cat.No: T69451

Cat.No: T36713

IRBP (1-20) (human, rat) TFA

Cat.No: T83681

Synonym: IRBP1-20,Interphotoreceptor Retinoid-Binding Protein (1-20)

Sulindac sodium

Cat.No: T61585

BI-9627 hydrochloride

Cat.No: T23800

Synonym: BIX Hydrochloride,BIX HCl

Cat. No.	Product Name	Target	Signaling Pathways
T6S2238	Eupalinolide B	Others	Others
	Eupalinolide B 是一种胚芽倍半萜，分离自Eupatorium lindleyanum 中。它对BGC-823、A-549 和 HL-60 等肿瘤细胞具有细胞毒性。
T14140	Agaric acid 落叶松蕈酸,Agaricinic Acid	Mitochondrial Metabolism; AChR	Metabolism; Neuroscience
	Agaric acid (Agaricinic Acid) 来一种自真菌部落的Polyporus officinalis 和Polyporus igniarius。它可促进积累的 Ca2+流出，跨膜电位的破坏和线粒体肿胀。它通过其与腺嘌呤核苷酸转位酶的相互作用诱导线粒体通透性转变。它用于调节脂类代谢。
TN5238	Viscidulin II	IL Receptor; TNF	Apoptosis; Immunology/Inflammation
	Viscidulin II can be potential therapeutic agents against P. acnes-induced skin inflammation, it can significantly suppress P. acnes-induced IL-8 and IL-1β production in THP-1 cells, concomitant intradermal injection of viscidulin II with P. acnes can effectively attenuate P. acnes-induced ear swelling, and decrease the production of IL-6 and tumor necrosis factor-α in ear homogenates.

天然产物

Cat.No: T6S2238

Target: Others

Cat.No: T14140

Synonym: 落叶松蕈酸,Agaricinic Acid

Target: Mitochondrial Metabolism, AChR

Cat.No: TN5238

Target: IL Receptor, TNF

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