102
2
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. |
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。 |