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102

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T4584 BMS-813160

BMS 813160

CCR Immunology/Inflammation; Microbiology/Virology
BMS-813160 是CCR2/CCR5双重拮抗剂。有用于心血管的研究潜力。
T36716 RO0270608

RO0270608

RO0270608, the active metabolite of R411, is a dual α4β1/α4β7 integrin antagonist with anti-inflammatory activity[1][2].
TQ0029 ASTX660

IAP Apoptosis
ASTX660 是一种口服生物可利用的 cIAP 和 XIAP 双重拮抗剂。
T61807 5-HT6/7 antagonist 1

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
5-HT6/7 antagonist 1是一种 5-HT6/7/2A 和 D2 受体双重拮抗剂,可用于研究痴呆和阿尔兹海默症。
T10914 Cyclodrine hydrochloride

AChR Neuroscience
Cyclodrine hydrochloride 是一种胆毒蕈碱受体(mAChR)和烟碱受体(nAChR)双重拮抗剂,可以用于研究神经系统相关疾病。
T2710 TCS 1102

OX Receptor GPCR/G Protein; Neuroscience
TCS 1102 是双食欲素受体拮抗剂,对 OX1和OX2受体的Ki 分别为3和 0.2 nM。
T67782 Daridorexant hydrochloride

Nemorexant hydrochloride,Quviviq

OX Receptor GPCR/G Protein; Neuroscience
Daridorexant hydrochloride (Nemorexant hydrochloride) 是一种新型的双Orexin 受体拮抗剂。Daridorexant hydrochloride 可用于失眠研究。
T5500 DORA-22

OX Receptor GPCR/G Protein; Neuroscience
DORA-22 是一种双食欲素受体拮抗剂,可改善轻度压力引起的失眠,对记忆的影响很小。
T62420 P2Y2R/GPR17 antagonist 1

GPR Endocrinology/Hormones; GPCR/G Protein
P2Y2R/GPR17 antagonist 1 (Compound 14m) 是一种双重的 P2Y2R (IC50: 3.17 μM) 和 GPR17 (IC50: 1.67 μM) 拮抗剂。P2Y2R/GPR17 antagonist 1 在人肝微粒体中表现出极好的代谢稳定性。
T38144 Elinzanetant

Neurokinin receptor GPCR/G Protein; Neuroscience
Elizanetant 是有效的神经激肽受体拮抗剂,在精神分裂症研究中有价值。
T6242 Rupatadine Fumarate

富马酸卢帕他定,Rinialer,Rupafin,Alergoliber

PAFR; Autophagy; Histamine Receptor Autophagy; GPCR/G Protein; Immunology/Inflammation; Neuroscience
Rupatadine Fumarate (Rinialer) 是一种可口服的长效PAF/H1受体的双抑制剂,Ki 值分别为 0.55 μM 和 0.1 μM。它可研究过敏性鼻炎和荨麻疹。
T14078 AB928

Adenosine Receptor GPCR/G Protein; Neuroscience
AB928 是可口服的选择性腺苷受体(A2aR/A2bR)双拮抗剂,可减轻腺苷介导的免疫抑制,具有免疫调节和抗肿瘤活性。
T17232 Vidupiprant

AMG 853

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
Vidupiprant (AMG 853) 是一种有效的 CRTH2 和前列腺素 D 受体双重拮抗剂,在人源血浆中的 IC50 分别为 8 nM 和 35 nM。 Vidupiprant 可用于治疗哮喘的研究。
T5355 Sparsentan

RE-021,DARA-a

RAAS; Endothelin Receptor Endocrinology/Hormones; GPCR/G Protein
Sparsentan (DARA-a) 是一种具有高度选择的血管紧张素 II (Ki:0.8 nM)和内皮素 A 受体(Ki:9.3 nM)的双重拮抗剂。
T6265 Bosentan (hydrate)

波生坦水合物,Bosentan Hydrate,Benzenesulfonamide,Actelion,Ro 47-0203

Endothelin Receptor GPCR/G Protein
Bosentan hydrate (Ro 47-0203) 是endothelin-1 (ET)竞争性拮抗剂,在人SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。
T16854 SB-674042

SB674042

OX Receptor GPCR/G Protein; Neuroscience
SB-674042 是一种具有高效性和选择性的非肽类食欲肽 OX1和 OX2 受体双重拮抗剂, IC50 分别为 3.76 nM 和 531 nM。SB-674042 可用于治疗抑郁症 。
T24827 SR 16832

SR-16832,SR16832

PPAR DNA Damage/DNA Repair; Metabolism
SR 16832 是一种化学合成中的砌块
T12596 (4E)-SUN9221

5-HT Receptor; Adrenergic Receptor GPCR/G Protein; Neuroscience
(4E)-SUN9221 是一种有效的 α1-adrenergic 受体和 5-HT2 受体双重拮抗剂,在高血压大鼠中显示出抗高血压和抗血小板聚集活性。
T5310 TR-14035

MDK-1191

Integrin Cytoskeletal Signaling
TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7/α4β1整合素双重抑制剂,对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM,可用于炎症和自体免疫疾病的研究。
T30751 Carotegrast methyl

AJM300

Integrin Cytoskeletal Signaling
Carotegrast methyl (AJM300) 是一种口服有效和选择性 α4 整联蛋白拮抗剂,可预防小鼠结肠炎。HCA2969 是 Carotegrast methyl 的活性代谢产物,是一种特异的双重 α4β1/α4β7 整联蛋白拮抗剂。
TQ0297 Cenicriviroc

TAK-652,TBR-652

HIV Protease; CCR Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
Cenicriviroc (TAK-652) 是一种可口服的CCR2/CCR5拮抗剂,可抑制 HIV-1 和 HIV-2,具有抗炎、抗感染作用。
T60325 Viloxazine

Emovit,Viloxazin

5-HT Receptor; Norepinephrine GPCR/G Protein; Neuroscience
Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].
T2613 Almorexant

阿莫伦特,ACT 078573

OX Receptor GPCR/G Protein; Neuroscience
Almorexant (ACT 078573) 是一种有效的竞争性食欲素 1 受体 (OX1)/食欲素 2 受体 (OX2) 双重拮抗剂,OX1 和 OX2 的 Ki 值分别为 1.3 和 0.17 nM。
T23382 Spiroxatrine

R 5188

Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor GPCR/G Protein; Neuroscience
Spiroxatrine (R 5188) 是一种选择性和有效性的 5-HT1α 和 α2-adrenergic 双重拮抗剂,具有镇静活性,对5-HT1α、5-HT1 β、5-HT2和多巴胺受体具有抑制作用。Spiroxatrine 可用于研究心血管系统相关疾病。
T77593 KSK67

Sigma receptor GPCR/G Protein
KSK67 是一种具有选择性的 sigma-2 和 组胺 H3 受体双重拮抗剂,对 H3 受体、sigma-1、sigma-2 受体有抑制作用, Ki 值分别为 3.2, 1531, 101 nM。KSK67 可用于研究伤害性疼痛和神经性疼痛。
T79499 KSK68

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
KSK68 是一种高效的 sigma-1 和 组胺 H3 受体双重拮抗剂,具有潜在的镇痛活性,对 H3 受体、sigma-1、sigma-2 受体有很高的亲和力。KSK68 可用于研究与疼痛相关的疾病。
T9833 Opiranserin hydrochloride

P2X Receptor; GlyT; 5-HT Receptor GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
Opiranserin hydrochloride 是甘氨酸转运蛋白 2 型 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂,IC50 分别为 0.86 和 1.3 μM。它显示对 rP2X3 的拮抗活性 (IC50=0.87 μM)。它正在开发为用于治疗术后疼痛的注射剂。
T19839 Oxatomide

Oxatomida

P2X Receptor; Calcium Channel; 5-HT Receptor; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
Oxatomide (Oxatomida) 是一种有效且具有口服活性的双重 H1 组胺受体 和 P2X7 受体双重拮抗剂,具有抗组胺和抗过敏活性。Oxatomide 可用于阻断人 P2X7 受体中 ATP 诱导的电流 ,IC50 为 0.95 μM。Oxatomide 对 ATP 诱导的 Ca2+ 内流具有抑制作用,IC50 值为 0.43 μM。Oxatomide 对 5-羟色胺具有抑制作用。Oxatomide可用于治疗免疫系统疾病和研究超敏反应。
T19686 SCH-37370

乙酰地氯雷他定

Platelet aggregation Others
SCH-37370 是一种有效且具有口服活性的血小板活化因子和组胺双重拮抗剂。 Sch 37370 阻断 [3H]pyrilamine 与大鼠脑膜中组胺-H1 受体的结合。 Sch 37370 选择性地抑制 PAF 诱导的人血小板聚集(IC50:0.6 mM),并且还与 PAF 竞争与人肺膜制剂中特定位点的结合(IC50:1.2 mM)。
T22582 Arachidonyl serotonin

Others Others
Dual FAAH inhibitor/TRPV1 antagonist
T23760 AT-IAP

AT-IAP is an effective dual antagonist of XIAP and cIAP1.
T24013 DORA 42

DORA42,DORA-42

DORA 42 is a dual antagonist of the orexin receptor OX1R and OX2R.
T22953 LY 393558

Others Others
Dual 5-HT1B/1D receptor antagonist
T71045 FK-1052 HCl

FK-1052 HCl is a serotonin 3 & 4 dual receptor antagonist.
T71046 FK-1052

FK-1052 is a serotonin 3 & 4 dual receptor antagonist.
T69295 DNK 333

DNK 333 is a dual neurokinin NK1/NK2 receptor antagonist.
T35112 WAY 126299A

WAY126299A,WAY-126299A

Way 126299a is a dual-acting 5-lipoxygenase inhibitor and leukotriene D4 antagonist.
T30515 BMS-346567

BMS346567,BMS 346567

BMS-346567 is a potent and selective dual angiotensin II and endothelin receptor antagonist.
T23245 Ro-51

Ro 51

Others Others
dual P2X3 and P2X2/3 antagonist
T69505 BM573

BM573 is a dual thromboxane synthase inhibitor and thromboxane receptor antagonist.
T68392 ONO-4310321

ONO-4310321 is a potent, orally available dual CysLT1 and CysLT2 receptor antagonist.
T11293 (±)-Fabesetron hydrochloride

FK1052 hydrochloride

5-HT Receptor GPCR/G Protein; Neuroscience
FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
T10844 CMI-392

Others Others
CMI-392 is a dual 5-lipoxygenase inhibitor and platelet-activating factor (PAF) receptor antagonist (IC50s: 100 and 10 nM).
T27877 LY 163443

LY163443,LY-163443

LY 163443 is an dual receptor antagonist of LTD4 and LTE4.
T69715 ORN-0829 hydrate

ORN-0829 hydrate is a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia.
T69583 AMD-3451 trihydrochloride

AMD-3451 trihydrochloride is a CCR5/CXCR4 dual antagonist that may be useful in the treatment of HIV.
T28325 PD 127443

PD127443,PD-127443

PD 127443 is a Leukotriene B4 antagonist, it is also a dual inhibitor of cyclooxygenase and 5-lipoxygenase.
T70764 SIPI-6360

SIPI-6360 is a D2/5-HT2A receptor dual antagonist.
T11764 KP496

Others Others
KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor.
T71103 AZD3676

AZD3676 is a novel dual antagonist of serotonin 5-HT1A and 5-HT1B receptor.

化合物

BMS-813160
Cat.No: T4584
Synonym: BMS 813160
Target: CCR
RO0270608
Cat.No: T36716
Synonym: RO0270608
Target:
ASTX660
Cat.No: TQ0029
Synonym:
Target: IAP
5-HT6/7 antagonist 1
Cat.No: T61807
Synonym:
Target: Dopamine Receptor, 5-HT Receptor
Cyclodrine hydrochloride
Cat.No: T10914
Synonym:
Target: AChR
TCS 1102
Cat.No: T2710
Synonym:
Target: OX Receptor
Daridorexant hydrochloride
Cat.No: T67782
Synonym: Nemorexant hydrochloride,Quviviq
Target: OX Receptor
DORA-22
Cat.No: T5500
Synonym:
Target: OX Receptor
P2Y2R/GPR17 antagonist 1
Cat.No: T62420
Synonym:
Target: GPR
Elinzanetant
Cat.No: T38144
Synonym:
Target: Neurokinin receptor
Rupatadine Fumarate
Cat.No: T6242
Synonym: 富马酸卢帕他定,Rinialer,Rupafin,Alergoliber
Target: PAFR, Autophagy, Histamine Receptor
AB928
Cat.No: T14078
Synonym:
Target: Adenosine Receptor
Vidupiprant
Cat.No: T17232
Synonym: AMG 853
Target: Prostaglandin Receptor
Sparsentan
Cat.No: T5355
Synonym: RE-021,DARA-a
Target: RAAS, Endothelin Receptor
Bosentan (hydrate)
Cat.No: T6265
Synonym: 波生坦水合物,Bosentan Hydrate,Benzenesulfonamide,Actelion,Ro 47-0203
Target: Endothelin Receptor
SB-674042
Cat.No: T16854
Synonym: SB674042
Target: OX Receptor
SR 16832
Cat.No: T24827
Synonym: SR-16832,SR16832
Target: PPAR
(4E)-SUN9221
Cat.No: T12596
Synonym:
Target: 5-HT Receptor, Adrenergic Receptor
TR-14035
Cat.No: T5310
Synonym: MDK-1191
Target: Integrin
Carotegrast methyl
Cat.No: T30751
Synonym: AJM300
Target: Integrin
Cenicriviroc
Cat.No: TQ0297
Synonym: TAK-652,TBR-652
Target: HIV Protease, CCR
Viloxazine
Cat.No: T60325
Synonym: Emovit,Viloxazin
Target: 5-HT Receptor, Norepinephrine
Almorexant
Cat.No: T2613
Synonym: 阿莫伦特,ACT 078573
Target: OX Receptor
Spiroxatrine
Cat.No: T23382
Synonym: R 5188
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor
KSK67
Cat.No: T77593
Synonym:
Target: Sigma receptor
KSK68
Cat.No: T79499
Synonym:
Target: Histamine Receptor
Opiranserin hydrochloride
Cat.No: T9833
Synonym:
Target: P2X Receptor, GlyT, 5-HT Receptor
Oxatomide
Cat.No: T19839
Synonym: Oxatomida
Target: P2X Receptor, Calcium Channel, 5-HT Receptor, Histamine Receptor
SCH-37370
Cat.No: T19686
Synonym: 乙酰地氯雷他定
Target: Platelet aggregation
Arachidonyl serotonin
Cat.No: T22582
Synonym:
Target: Others
AT-IAP
Cat.No: T23760
Synonym:
Target:
DORA 42
Cat.No: T24013
Synonym: DORA42,DORA-42
Target:
LY 393558
Cat.No: T22953
Synonym:
Target: Others
FK-1052 HCl
Cat.No: T71045
Synonym:
Target:
FK-1052
Cat.No: T71046
Synonym:
Target:
DNK 333
Cat.No: T69295
Synonym:
Target:
WAY 126299A
Cat.No: T35112
Synonym: WAY126299A,WAY-126299A
Target:
BMS-346567
Cat.No: T30515
Synonym: BMS346567,BMS 346567
Target:
Ro-51
Cat.No: T23245
Synonym: Ro 51
Target: Others
BM573
Cat.No: T69505
Synonym:
Target:
ONO-4310321
Cat.No: T68392
Synonym:
Target:
(±)-Fabesetron hydrochloride
Cat.No: T11293
Synonym: FK1052 hydrochloride
Target: 5-HT Receptor
CMI-392
Cat.No: T10844
Synonym:
Target: Others
LY 163443
Cat.No: T27877
Synonym: LY163443,LY-163443
Target:
ORN-0829 hydrate
Cat.No: T69715
Synonym:
Target:
AMD-3451 trihydrochloride
Cat.No: T69583
Synonym:
Target:
PD 127443
Cat.No: T28325
Synonym: PD127443,PD-127443
Target:
SIPI-6360
Cat.No: T70764
Synonym:
Target:
KP496
Cat.No: T11764
Synonym:
Target: Others
AZD3676
Cat.No: T71103
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3417 Amentoflavone

Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物,有抗炎、抗氧化和神经保护等作用。
T3S1612 kuwanon G

桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G

Phosphatase; Antibacterial; Bombesin Receptor; AChR; AChE; Glucosidase GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
Kuwanon G (Moracenin B) 是一种从桑树中得到的黄酮类蛙皮素受体拮抗剂,具有杀菌作用。

天然产物

Amentoflavone
Cat.No: T3417
Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin
Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal
kuwanon G
Cat.No: T3S1612
Synonym: 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G
Target: Phosphatase, Antibacterial, Bombesin Receptor, AChR, AChE, Glucosidase
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