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15

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13865	Resorcinolnaphthalein	RAAS	Endocrinology/Hormones
	Resorcinolnaphthalein 是一种特异性的血管紧张素转换酶 2 激活剂，EC50=19.5 μM。Resorcinolnaphthalein 能够用于高血压和肾纤维化的研究
T5326	Sugammadex sodium Org25969,Sugammadex (sodium),舒更葡糖钠	Others	Others
	Sugammadex sodium (Org25969) 是合成的 γ 环糊精衍生物，是一种新型的神经肌肉阻断逆转剂。
T10820L1	Ciraparantag acetate Ciraparantag acetate(1438492-26-2 Free base)	Others	Others
	Ciraparantag acetate 是一种抗凝逆转剂，是一种小分子，专门设计用于通过电荷-电荷相互作用与普通肝素和低分子量肝素非共价结合。它显示出与直接口服抗凝剂 (DOAC) 相似的结合特性。
T34645	Simetride
	Simetride is used in the Reversal of resistance to vincristine in P388 leukemia.
T10820	Ciraparantag PER977	Others	Others
	Ciraparantag is an inhibitor of thrombin and factor Xa. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including unfractionated heparin, low-molecular-weight heparin, and certain direct oral anticoagulants.
T74826	AcrB-IN-1
	AcrB-IN-1 (Compound H6) 是一种有效的 AcrB 抑制剂。AcrB-IN-1 可用于逆转细菌多药耐药。
T82083	Idarucizumab BI 655075
	Idarucizumab 是一种专门中和口服直接凝血酶抑制剂（DOAC）效用的人源化单克隆抗体片段，是首个用于逆转DOAC抗凝作用的逆转剂（reversal agent），适用于恢复正常止血功能。
T10820L	Ciraparantag TFA PER977 TFA	Others	Others
	Ciraparantag TFA is an inhibitor of thrombin and factor Xa. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including unfractionated heparin, low-molecular-weight heparin, and certain direct oral anticoagulants.
T82898	Bentracimab PB 2452,MEDI 2452
	Bentracimab (PB 2452) 是高度亲和性的中和单克隆抗体，专门结合于Ticagrelor及其主要活性代谢产物。该抗体能迅速逆转Ticagrelor的抗血小板功能。
T72665	P-gp inhibitor 3
	P-gp inhibitor 3 是一种高效 P 糖蛋白（P-gp）抑制剂，通过激活 P-gp ATP酶抑制其外排功能，具有显著的多重耐药性（MDR）逆转能力，并能增强紫杉醇的抗肿瘤活性。
T5326L	Sugammadex Org-25969,Org25969,Org 25969,361LPM2T56
	Sugammadex is an agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). Sugammadex is a modified γ-cyclodextrin, with a lipophilic core and a hydrophilic periph
T80245	LL-37(17-32)
	LL-37(17-32)为具有生物活性的肽段，为LL-37抗菌肽C末端结构域源自的活性片段。报道显示，LL-37(17-32)能逆转癌细胞系中ABCG2介导的多药耐药性。
T67948	OY-101
	OY-101为口服生效的特异性P-glycoprotein(P-gp)抑制剂。该化合物可增强耐药性肿瘤的敏感性，并有效逆转多药耐药现象。相较于Tetrandrine，OY-101在水溶性、细胞毒性以及逆转活性方面均表现出改进。
T36847	Coelenterazine hcp
	Coelenterazine hcp is a synthetic bioluminescent luciferin that displays an emission maximum of 445 nm.1It has been used as a calcium indicator and substrate to quantifyRenillaluciferase activity.1,2,3 1.Sabnis, R.W.Handbook of biological dyes and stains: Synthesis and industrial applications(2010) 2.Shimomura, O., Kishi, Y., and Inouye, S.The relative rate of aequorin regeneration from apoaequorin and coelenterazine analoguesBiochemistry Journal296(Pt 3)549-551(1993) 3.Pichler, A., Prior, J.L.,...
T36720	Deacetylforskolin
	Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor...

化合物

Resorcinolnaphthalein

Cat.No: T13865

Target: RAAS

Sugammadex sodium

Cat.No: T5326

Synonym: Org25969,Sugammadex (sodium),舒更葡糖钠

Target: Others

Ciraparantag acetate

Cat.No: T10820L1

Synonym: Ciraparantag acetate(1438492-26-2 Free base)

Target: Others

Cat.No: T34645

Cat.No: T10820

Synonym: PER977

Target: Others

Cat.No: T74826

Cat.No: T82083

Synonym: BI 655075

Ciraparantag TFA

Cat.No: T10820L

Synonym: PER977 TFA

Target: Others

Cat.No: T82898

Synonym: PB 2452,MEDI 2452

P-gp inhibitor 3

Cat.No: T72665

Cat.No: T5326L

Synonym: Org-25969,Org25969,Org 25969,361LPM2T56

Cat.No: T80245

Cat.No: T67948

Coelenterazine hcp

Cat.No: T36847

Deacetylforskolin

Cat.No: T36720

Cat. No.	Product Name	Target	Signaling Pathways
T3924	Astragaloside II 黄芪皂苷 II,Astrasieversianin VIII	TGF-beta/Smad	Stem Cells
	Astragaloside II (Astrasieversianin VIII) 是一种分离自黄芪中的天然化合物。
T3330	trans-Trimethoxyresveratrol trans-trismethoxy Resveratrol,E-Resveratrol Trimethyl Ether,MR-3,Tri-O-methylresveratrol,白藜芦醇三甲醚,3,4',5-Trimethoxy-trans-stilbene,Trimethoxystilbene	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	trans-Trimethoxyresveratrol (MR-3) 是一种 Resveratrol(RSV) 的衍生物，与Resveratrol(RSV)相比，它可能是一个更有效的抗炎、抗血管新生的化合物。
T3S1775	Tectochrysin NSC 80687,Techtochrysine,Techtochrysin,柚木柯因	NF-κB; STAT	JAK/STAT signaling; NF-κB; Stem Cells
	Tectochrysin (Techtochrysine) 是Alpinia oxyphylla 的主要黄酮类化合物之一，能够抑制NF-κB 活性。
T4S1050	Pristimerin 扁塑藤素,Celastrol methyl ester	NF-κB; Antibacterial	Microbiology/Virology; NF-κB
	Pristimerin (Celastrol methyl ester) 是一种可逆的单酰基甘油脂肪酶高效抑制剂，IC50值为93 nM。
T4A2399	Cinobufotalin 华蟾毒它灵,华蟾素	IL Receptor; Akt; MRP; P-gp	Cytoskeletal Signaling; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; PI3K/Akt/mTOR signaling
	Cinobufotalin 是一种从蟾蜍的皮肤分泌物中提取的强心类固醇或丁二烯内酯。它已被用作强心药，利尿药和止血药，也是潜在的抗肺癌药物。
TJS1779	Protosappanin A 原苏木素A,PTA	NADPH-oxidase; IL Receptor; IκB/IKK; TNF; NF-κB; TLR; ROS; COX; HIV Protease; JAK; NO Synthase; STAT	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Microbiology/Virology; Neuroscience; NF-κB; Proteases/Proteasome; Stem Cells
	Protosappanin A (PTA) 是从苏木中分离得到的免疫抑制成分和主要联苯化合物，通过下调 JAK2和 STAT3的磷酸化，抑制 JAK2/STAT3依赖的炎症通路。
T5S0053	Coptisine 黄连碱,Coptisin	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Coptisine (Coptisin) 是一种从黄连中分离到的生物碱，是非竞争性的IDO 抑制剂，Ki=为 5.8 μM，IC50=6.3 μM。
T10018	1-Methyladenine	Others	Others
	1-Methyladenine is a DNA alkylation product that undergoes damage reversal through oxidative demethylation for repair purposes.
TN3911	Ecdysterone 2,3:20,22-diacetonide	Others	Others
	Due to the multi-drug resistance reversal activity of the less polar ecdysteroids, several new products( including 20-hydroxyecdysone,20-hydroxyecdysone 2,3;20,22-diacetonide) are promising for being tested against various cancer cell lines.
T23610	Acerinol
	Acerinol is an active ingredient from traditional Chinese medicinal herbs. It could be used as a cancer multidrug resistance reversal agent. Acerinol can significantly stimulate the activity of ABCB1 ATPase without affecting the expression of ABCB1 on nei
TN5414	Wallichinine
	Wallichinine shows inhibitory activity on platelet aggregation caused by platelet activating factor (PAF). Wallichinine with ABCB1 presents valuable clues for the development of novel MDR reversal reagents from natural products, wallichinine can significa
T83055	Anti-inflammatory agent 57
	Anti-inflammatory agent 57（Compound 13），一种天然产自Peucedanum praeruptorum根部的吡喃香豆素，既能逆转多药耐药性（MDR）又具备抗炎效果。

天然产物

Astragaloside II

Cat.No: T3924

Synonym: 黄芪皂苷 II,Astrasieversianin VIII

Target: TGF-beta/Smad

trans-Trimethoxyresveratrol

Cat.No: T3330

Synonym: trans-trismethoxy Resveratrol,E-Resveratrol Trimethyl Ether,MR-3,Tri-O-methylresveratrol,白藜芦醇三甲醚,3,4',5-Trimethoxy-trans-stilbene,Trimethoxystilbene

Target: Reactive Oxygen Species

Cat.No: T3S1775

Synonym: NSC 80687,Techtochrysine,Techtochrysin,柚木柯因

Target: NF-κB, STAT

Cat.No: T4S1050

Synonym: 扁塑藤素,Celastrol methyl ester

Target: NF-κB, Antibacterial

Cat.No: T4A2399

Synonym: 华蟾毒它灵,华蟾素

Target: IL Receptor, Akt, MRP, P-gp

Protosappanin A

Cat.No: TJS1779

Synonym: 原苏木素A,PTA

Target: NADPH-oxidase, IL Receptor, IκB/IKK, TNF, NF-κB, TLR, ROS, COX, HIV Protease, JAK, NO Synthase, STAT

Cat.No: T5S0053

Synonym: 黄连碱,Coptisin

Target: Indoleamine 2,3-Dioxygenase (IDO)

1-Methyladenine

Cat.No: T10018

Target: Others

Ecdysterone 2,3:20,22-diacetonide

Cat.No: TN3911

Target: Others

Cat.No: T23610

Cat.No: TN5414

Anti-inflammatory agent 57

Cat.No: T83055

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