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57

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T28276	OV-potentiator-28 OV potentiator 28
	OV-potentiator-28 is a potentiator of cancer virotherapy. OV-potentiator-28 significantly enhances virus replication-associated luciferase expression, specifically in tumors.
T25173	Bradykinin potentiator-5 BPP-5a\,BPP 5a\,BPP5a\
	Bradykinin potentiator-5 is a peptide inflammatory mediator, causes blood vessels to dilate (enlarge), and therefore causes blood pressure to fall.
T76505	Bradykinin potentiator B
	Bradykinin potentiator B 是 Agkistrodon halys blomhoffi 的毒液。Bradykinin potentiator B 是一种有效的 ACE 抑制剂。Bradykinin potentiator B 抑制缓激肽抑制肽酶的活性。
T76507	Bradykinin potentiator C
	Bradykinin potentiator C是一种有效的血管紧张素转化酶(ACE)抑制剂，对兔肺ACE的IC50值为7.1 μM，被认为是功能肽原型。
T63003	NMDA receptor potentiator-1
	NMDA receptor potentiator-1 (Compound 1368) 是一种亚基选择性的 NMDA receptor 增强剂。NMDA receptor potentiator-1 对 NR2C 和 NR2D 表达的 IC50 值分别为 4 μM 和 5 μM。
T23515	VU-29 VU 29	GluR	Neuroscience
	VU-29 是代谢型谷氨酸 5(mGlu5)受体的正变构调节剂，对 rmGluR5 的 EC50为 9 nM，Ki 为 244 nM。相对于其他亚型，它对 mGluR5 具有选择性，对 rmGluR1/rmGluR2和 hmGluR4的 EC50分别为557 nM/1.5 μM 和 154 nM。
T9499	Icenticaftor QBW251	CFTR	Membrane transporter/Ion channel
	Icenticaftor (QBW251) 是一种具有口服活性CFTR 通道增强剂，可用于慢性阻塞性肺疾病 (COPD) 和囊性纤维化研究，对F508del 和G551D CFTR 的EC50分别为 79 和 497 nM。
T15820	Mibampator LY451395	iGluR	Membrane transporter/Ion channel; Neuroscience
	Mibampator (LY451395) 是一种有效和选择性的 AMPA 受体增效剂。
T17238	VU0152100 VU152100	AChR	Neuroscience
	VU0152100 是一种选择性 M4 mAChR 变构增强剂，EC50为 380 ± 93 nM。
T7083	GLPG1837 ABBV-974	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	GLPG1837 (ABBV-974) 是一种有效的 CFTR 增强剂，对其 F508del 和 G551D 的 EC50 分别为 3 nM 和 339 nM。
TQ0289	LY450108	iGluR	Membrane transporter/Ion channel; Neuroscience
	LY450108 是有效的AMPA 受体增强剂，在抑郁和帕金森氏病中有研究的潜力。
T23513	VU10010 VU 10010	AChR	Neuroscience
	VU10010 (VU 10010) 是一种高度选择性的M4mAChR 变构增强剂，EC50为 400 nM。它与 M4mAChR 的变构位点结合，增强与 G 蛋白偶联，增加对乙酰胆碱的亲和力，还会增加卡巴胆碱引起的兴奋性传导抑制。
T14971	CIQ	NMDAR	Neuroscience
	CIQ 是亚基选择性NMDA 受体增强剂，可作用于NR2C 或NR2D 亚基。
T2588	Ivacaftor Ivacaftor (VX-770),VX-770,依伐卡托	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	Ivacaftor (VX-770) 是一种 CFTR 增强剂，靶向G551D-CFTR 和F508del-CFTR 的EC50分别为100 和 25 nM。
T29123	VU0152099 VU 0152099,VU-0152099	AChR	Neuroscience
	VU0152099 是选择性和可透过血脑屏障的 mAChR M4正变构调节剂，可增强 M4 对乙酰胆碱的反应，对大鼠 M4 受体的 EC50为 0.4 µM。
T61301	Chromenone 1	TGF-beta/Smad	Stem Cells
	Chromenone 1 是一种有效的成骨骨形态发生蛋白(BMP)增强剂，其通过诱导显著的非激酶依赖的负TGFβ反馈，独特地增强了核BMP-Smad信号输出。
T4573	Cyclothiazide	GluR	Neuroscience
	Cyclothiazide 是AMPA 受体的正变构调节剂，可快速抑制 AMPA 受体脱敏，并缓慢增强 AMPA 电流。它可以阻断天然和异源表达的AMPA 受体脱敏。
T8779	HBT1	GluR	Neuroscience
	HBT1 是一种 AMPA 受体增强剂，可诱导脑源性神经营养因子 (BDNF) 的产生，并且在原代神经元中几乎没有激动作用。 HBT1 以谷氨酸依赖的方式与 AMPA-R 的配体结合结构域结合。
T8890	653-47 hydrochloride	Epigenetic Reader Domain	Chromatin/Epigenetic
	653-47 hydrochloride 是一种增强剂，能显著增强 666-15 的 cAMP 反应元件结合蛋白 (CREB) 抑制活性。它也是 CREB 抑制剂，IC50为 26.3 μM。
T16516	PG01 Phenylglycine-01	CFTR	Membrane transporter/Ion channel
	PG01是一种有效的CFTR Cl-通道增效剂,PG01对 ΔF508（Ka 为 0.3 μM）有效。PG01 对 E193K，G970R 和 G551D (CFTR 突变体)也有效，Kd 值分别为 0.22 μM，0.45 μM 和 1.94 μM 。PG01在加入Forskolin 后可增加ΔF508-CFTR Cl-电流，纠正CFTR 突变体的门控缺陷。
T22720	3,3'-Difluorobenzaldazine DFB	Others	Others
	allosteric potentiator of mGlu5
T24916	UBP646 UBP-646,UBP 646
	UBP646 is a GluN1/GluN2 receptors potentiator.
T26263	TG3-95-1 TG3951,TG 3951,TG-3951
	TG3-95-1 is an EP2 allosteric potentiator agent.
T24010	DNAC-1 DNAC 1,DNAC1
	DNAC-1 is against Gram-positive and Gram-negative pathogens potentiator of β-lactam activity.
T23020	MRS 2219	Others	Others
	P2X1 receptor potentiator
T14615	Biphenylindanone A BINA	GluR	Neuroscience
	Biphenylindanone A is a selective potentiator of human mGluR2 (hmGluR2),and for the treatment of neurological disorders.
T13742L	Ivacaftor hydrate VX-770 hydrate	Others	Others
	Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.
T27935	LY2607540 LY-2607540,THIIC,LY 2607540
	LY2607540 is a metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties (EC(50) = 23 and 13 nM, respectively).
T24268	KP-544 KP 544
	KP-544 is an agent of neurotrophin potentiator.
T27953	LY-395153 LY 395153,LY395153
	LY-395153 is a novel potentiator of AMPA receptor.
T23130	PD 81723	Others	Others
	Allosteric potentiator at the adenosine A1 receptor
T70880	TAK-137
	TAK-137 is a novel AMPA receptor potentiator with little agonistic effect, producing antidepressant-like effect without causing psychotomimetic effects.
T0368L	Cinepazide Brendil,MD67350,Vasodistal,Cinepazide free base,MD-67350,MD 67350,NSC 291562
	Cinepazide is a vasodilator used for the treatment of cardiovascular, cerebrovascular, and peripheral vascular diseases. Cinepazide acts as a potentiator of adenosine A2 receptors.
T13742	Ivacaftor benzenesulfonate VX-770 benzenesulfonate	Others	Others
	Ivacaftor benzenesulfonate used for cystic fibrosis treatment. is an orally bioavailable CFTR potentiator.
T24767	SBI-0069332
	SBI-0069332 is a potentiator of metabotropic glutamate receptors. It was used against neurological and psychiatric disorders.
T39596	Dirocaftor PTI-808
	Dirocaftor (PTI-808) is a CFTR potentiator that augments CFTR protein function via the activation of chloride channels. Dirocaftor holds potential utility for research pertaining to cystic fibrosis (CF).
T13705	GLPG2451	Cysteine Protease	Proteases/Proteasome
	GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. It effectively potentiates low temperature rescued F508del CFTR (EC50: 11.1 nM).
TP1089	SPR741 TFA (1179330-52-9 free base) NAB741 TFA,SPR741 TFA
	SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule.
T22939	LY 2087101	Others	Others
	Allosteric potentiator of α7, α4β2 and α4β4 nAChRs
T24551	NSC339614 potassium NSC 339614 potassium,NSC-339614 potassium,NSC339614 potassium salt
	NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptors potentiator.
T27959	LY503430 LY-503430,LY 503430
	LY503430 is a AMPA receptor potentiator with oral activity. LY503430 has both nootropic and neuroprotective effects, reducing brain damage caused by 6-hydroxydopamine or MPTP.
T40386	CP-628006
	CP-628006 is a small molecule CFTR potentiator that effectively restores ATP-dependent channel gating to G551D-CFTR, the mutant form found in cystic fibrosis.
T24766	SBI-0061869 SBI0061869
	SBI-0061869 is a potentiator of metabotropic glutamate receptors. It was used against neurological and psychiatric disorders.
T25508	HUHS2002 HUHS 2002,HUHS-2002
	HUHS2002 is a free fatty acid derivative that works as a potentiator of GluA1 AMPA receptor responses and α7 ACh receptor responses.
T38936	KRAS G13D peptide, 25 mer KRAS G13D peptide, 25 mer
	KRAS G13D peptide, a 25-mer sequence, is derived from the KRAS activating oncogene mutation and serves as an immune potentiator. This peptide possesses immunogenic properties and can be utilized for the development of a KRAS vaccine.
T71975	5-MPEP
	5-MPEP is a neutral allosteric site ligand of the metabotropic glutamate receptor subtype 5 (mGlu5), blocking the effects of both the allosteric antagonist MPEP and potentiator CDPPB.
T13691	Etifoxine HOE 36-801	Others	Others
	Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. GABAA receptor Etifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration. Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons.
T37686	CFTR corrector 6
	CFTR corrector 6 is a highly effective CFTR potentiator utilized in research on cystic fibrosis (CF) and related CFTR-associated disorders[1]. This potent compound exhibits potentiation activity on the Cystic Fibrosis Transmembrane conductance Regulator (CFTR), rendering it beneficial for investigations in CF and other associated conditions.
T61655	AM-1488
	AM1488 是一种有效的、具有口服活性的甘氨酸受体 (GlyR) 增效剂 (hGlyRα3EC50=0.45 μM)。
T8889	653-47
	653-47 是一种增强剂，能显著增强 666-15 的 cAMP 反应元件结合蛋白(CREB)抑制活性。653-47 也是一种非常弱的CREB 抑制剂，IC50值为 26.3 μM。

化合物

OV-potentiator-28

Cat.No: T28276

Synonym: OV potentiator 28

Bradykinin potentiator-5

Cat.No: T25173

Synonym: BPP-5a\,BPP 5a\,BPP5a\

Bradykinin potentiator B

Cat.No: T76505

Bradykinin potentiator C

Cat.No: T76507

NMDA receptor potentiator-1

Cat.No: T63003

Cat.No: T23515

Synonym: VU 29

Target: GluR

Cat.No: T9499

Synonym: QBW251

Target: CFTR

Cat.No: T15820

Synonym: LY451395

Target: iGluR

Cat.No: T17238

Synonym: VU152100

Target: AChR

Cat.No: T7083

Synonym: ABBV-974

Target: CFTR, Autophagy

Cat.No: TQ0289

Target: iGluR

Cat.No: T23513

Synonym: VU 10010

Target: AChR

Cat.No: T14971

Target: NMDAR

Cat.No: T2588

Synonym: Ivacaftor (VX-770),VX-770,依伐卡托

Target: CFTR, Autophagy

Cat.No: T29123

Synonym: VU 0152099,VU-0152099

Target: AChR

Cat.No: T61301

Target: TGF-beta/Smad

Cat.No: T4573

Target: GluR

Cat.No: T8779

Target: GluR

653-47 hydrochloride

Cat.No: T8890

Target: Epigenetic Reader Domain

Cat.No: T16516

Synonym: Phenylglycine-01

Target: CFTR

3,3'-Difluorobenzaldazine

Cat.No: T22720

Synonym: DFB

Target: Others

Cat.No: T24916

Synonym: UBP-646,UBP 646

Cat.No: T26263

Synonym: TG3951,TG 3951,TG-3951

Cat.No: T24010

Synonym: DNAC 1,DNAC1

Cat.No: T23020

Target: Others

Biphenylindanone A

Cat.No: T14615

Synonym: BINA

Target: GluR

Ivacaftor hydrate

Cat.No: T13742L

Synonym: VX-770 hydrate

Target: Others

Cat.No: T27935

Synonym: LY-2607540,THIIC,LY 2607540

Cat.No: T24268

Synonym: KP 544

Cat.No: T27953

Synonym: LY 395153,LY395153

Cat.No: T23130

Target: Others

Cat.No: T70880

Cat.No: T0368L

Synonym: Brendil,MD67350,Vasodistal,Cinepazide free base,MD-67350,MD 67350,NSC 291562

Ivacaftor benzenesulfonate

Cat.No: T13742

Synonym: VX-770 benzenesulfonate

Target: Others

Cat.No: T24767

Cat.No: T39596

Synonym: PTI-808

Cat.No: T13705

Target: Cysteine Protease

SPR741 TFA (1179330-52-9 free base)

Cat.No: TP1089

Synonym: NAB741 TFA,SPR741 TFA

Cat.No: T22939

Target: Others

NSC339614 potassium

Cat.No: T24551

Synonym: NSC 339614 potassium,NSC-339614 potassium,NSC339614 potassium salt

Cat.No: T27959

Synonym: LY-503430,LY 503430

Cat.No: T40386

Cat.No: T24766

Synonym: SBI0061869

Cat.No: T25508

Synonym: HUHS 2002,HUHS-2002

KRAS G13D peptide, 25 mer

Cat.No: T38936

Synonym: KRAS G13D peptide, 25 mer

Cat.No: T71975

Cat.No: T13691

Synonym: HOE 36-801

Target: Others

CFTR corrector 6

Cat.No: T37686

Cat.No: T61655

Cat.No: T8889

Cat. No.	Product Name	Target	Signaling Pathways
T23172	Polygodial Tadeonal,水蓼二醛	Antifungal	Microbiology/Virology
	Polygodial (Tadeonal) 是一种抗真菌增效剂和抗生素。它是一种倍半萜，具有抗痛觉过敏的作用。
T0086	Galanthamine hydrobromide Galantamine hydrobromide,Galanthamine HBr,氢溴酸加兰他敏	AChR; AChE	Neuroscience
	Galanthamine hydrobromide (Galantamine hydrobromide) 是一种长效的中枢活性 AChE 抑制剂，IC50为 410 nM。它是神经元烟碱型 ACh 受体的变构增强剂，IC50值为 0.35 µM，可用于阿尔茨海默症的研究。
T81676	NG-012
	NG-012为一种神经生长因子(NGF)增强剂，来源于Penicillium verruculosum F-4542的培养液。该化合物能在大鼠嗜铬细胞瘤细胞系(PC12)中提升NGF引导的神经突生长效应。

天然产物

Cat.No: T23172

Synonym: Tadeonal,水蓼二醛

Target: Antifungal

Galanthamine hydrobromide

Cat.No: T0086

Synonym: Galantamine hydrobromide,Galanthamine HBr,氢溴酸加兰他敏

Target: AChR, AChE

Cat.No: T81676

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