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Targets Recommended: P2X Receptor Others

50

抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
T61490 P2X receptor-1

Others Others
P2X receptor-1 是一种潜在的 P2X 受体抑制剂,用于治疗疼痛和炎症。
T10466 BAY-1797

P2X Receptor Membrane transporter/Ion channel; Neuroscience
BAY-1797 是具有口服活性的选择性P2X4高效拮抗剂,对人 P2X4 的IC50为 211 nM,具有抗伤害和抗炎作用。
T10207 A 438079

P2X Receptor Membrane transporter/Ion channel; Neuroscience
A 438079 是选择性P2X7受体拮抗剂,pIC50值为 6.9。
T3690 A-740003

A 740003

P2X Receptor Membrane transporter/Ion channel; Neuroscience
A-740003 (A 740003) 是一种选择性和竞争性的P2X7 受体拮抗剂,抑制大鼠和人的 P2X7 受体,IC50值分别为 18 和 40 nM。
T22518 5-BDBD

P2X Receptor Membrane transporter/Ion channel; Neuroscience
5-BDBD 是选择性P2X4受体拮抗剂,抑制 rP2X4R 介导的电流,IC50为0.75μM。它可完全阻断硝酸甘油诱导的基础性和急性痛觉过敏。
T3639 A-804598

A 804598

P2X Receptor Membrane transporter/Ion channel; Neuroscience
A-804598 是一个 CNS 渗透,竞争性和选择性的 P2X7受体拮抗剂,作用于小鼠、大鼠和人的 P2X7 受体,IC50s 分别是 9、10 和 11 nM。
T8946 Indophagolin

P2X Receptor; 5-HT Receptor; Autophagy Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
Indophagolin 是一种有效的含有二氢吲哚的自噬抑制剂,IC50 为 140 nM。它拮抗 Gq 蛋白偶联的 P2Y4、P2Y6和 P2Y11受体。它还拮抗嘌呤能受体 P2X4 以及 P2X1 和 P2X3,IC50 分别为 2.71、2.40 和 3.49 μM。
T9519 Eliapixant

BAY 1817080

P2X Receptor Membrane transporter/Ion channel; Neuroscience
Eliapixant (BAY 1817080) 是一种选择性的P2X3受体拮抗剂,IC50值为 8 nM,可用于难治性慢性咳嗽的研究。
T40045 Sivopixant

S-600918,Sivopixant

P2X Receptor Membrane transporter/Ion channel; Neuroscience
Sivopixant (S-600918) 是P2X3受体选择性拮抗剂 (P2X3IC50=4.2 nM; P2X2/3IC50=1100 nM)。Sivopixant 可用于缓解疼痛的研究。
T8333 Aurintricarboxylic acid

ATA,NSC-4056,NSC4056,金精三羧酸,NSC 4056

Apoptosis; P2X Receptor; Influenza Virus; Topoisomerase Apoptosis; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Aurintricarboxylic acid (NSC-4056) 是高效的αβ-亚甲基-ATP 敏感选择性P2X1Rs 和P2X3Rs 变构拮抗剂。 它是核糖核酸酶和拓扑异构酶 II 的有效抑制剂,可阻止核酸与酶结合。
T2087 AF-353

Ro-4

P2X Receptor Membrane transporter/Ion channel; Neuroscience
AF-353 (Ro-4) 是一种选择性、可口服的 P2X3/P2X2/3 受体拮抗剂,抑制人和大鼠 P2X3 的 pIC50值为 8.0,抑制人 P2X2/3 的 pIC50值为 7.3。
T14385 AZD9056 hydrochloride

P2X Receptor Membrane transporter/Ion channel; Neuroscience
AZD9056 hydrochloride 是一种 P2X7 抑制剂,在炎症和引起疼痛的疾病中起重要作用。
T5513 RO-3

P2X Receptor Membrane transporter/Ion channel; Neuroscience
RO3 是一种能透过大脑的P2X3和P2X2/3拮抗剂,口服有活性。它对人同型多聚体 P2X3和异型多聚体 P2X2/3受体的 pIC50分别为 5.9 和 7.0。
T4298 JNJ-47965567

JNJ-479655

P2X Receptor Membrane transporter/Ion channel; Neuroscience
JNJ-47965567 (JNJ-479655) 是中枢通透性、高亲和力、选择性的P2X7拮抗剂,可用于探讨中枢 P2X7 在中枢神经系统病理生理模型中的作用。它对人和大鼠 P2X7 作用的pKi 值分别为 7.9 和 8.7。
T12568 PSB-12062

N-(p-Methylphenylsulfonyl)phenoxazine

P2X Receptor Membrane transporter/Ion channel; Neuroscience
PSB-12062 (N-(p-Methylphenylsulfonyl)phenoxazine)是选择性 P2X4拮抗剂,对人类 P2X4 的 IC50值为1.38 μM。
T14920 CE-224535

PF-04905428

P2X Receptor Membrane transporter/Ion channel; Neuroscience
CE-224535 (PF-04905428) 是 P2X7 受体的特异性拮抗剂。 CE-224535 可用于改善疾病的抗风湿研究。
T14366 AZ10606120 dihydrochloride

P2X Receptor Membrane transporter/Ion channel; Neuroscience
AZ10606120 dihydrochloride 是一种可选择的、有效的、高亲和力的受体拮抗剂,在人和大鼠 P2X 7 受体上的 K D 值分别为 1.4 和 19 nM。AZ10606120 dihydrochloride 抑制肿瘤生长,具有抗血管生成活性 。AZ 10606120在与 ATP 结合位点偶联的位点结合时充当负变构调节剂。
T2694 KN-62

CaMK; P2X Receptor; Autophagy Autophagy; Membrane transporter/Ion channel; Neuroscience
KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂,直接与 CaMK-II 酶的钙调蛋白结合位点结合,对大鼠脑 CaMK-II 的IC50值为 0.9 μM。它是非竞争性的P2X7受体拮抗剂,IC50约为 15 nM。
T9786 Lu AF27139

P2X Receptor Membrane transporter/Ion channel; Neuroscience
Lu AF27139 是一种有效的选择性 P2X7 受体拮抗剂(人和大鼠的 IC50 分别为 12 和 2.4 nM,小鼠、人和大鼠的 Ki 分别为 22、54 和 13 nM)。 Lu AF27139 可用于中枢神经系统疾病研究。
T14844 BX430

P2X Receptor; Calcium Channel Membrane transporter/Ion channel; Metabolism; Neuroscience
BX430 是一种有效的选择性非竞争性变构人 P2X4 受体通道拮抗剂,IC50 为 0.54 μM。它具有物种特异性,可用于治疗慢性疼痛和心血管疾病。
TQ0002 A-317491

ABT 202

P2X Receptor Membrane transporter/Ion channel; Neuroscience
A-317491 (ABT 202) 是选择性和非核苷酸的 P2X3和 P2X2/3受体的拮抗剂,通过阻断 P2X3和 P2X2/3受体介导的钙通量减轻炎性和神经性疼痛。它对其他 P2 受体和神经递质受体,离子通道以及酶具有高度选择性,IC50大于10 μM。
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。
T7805 GW791343 dihydrochloride

GW791343 (HCl)

P2X Receptor Membrane transporter/Ion channel; Neuroscience
GW791343 dihydrochloride (GW791343 (HCl)) 是有种属特异性的 P2X7变构调节剂,对人 P2X7的 pIC50为6.9-7.2。
T5099 Gefapixant

RO 4926219,AF219,MK-7264

P2X Receptor Membrane transporter/Ion channel; Neuroscience
Gefapixant (AF219) 是一个 P2X3 受体拮抗剂,其对人同源重组 hP2X3 和 hP2X2/3 的 IC50值分别是约 30 和 100-250 nM。
T2673 A 438079 hydrochloride

A 438079 (hydrochloride),A-438079 hydrochloride,A-438079 HCl

P2X Receptor Membrane transporter/Ion channel; Neuroscience
A 438079 hydrochloride (A-438079 HCl) 是一种选择性的P2X7受体拮抗剂,pIC50值为 6.9。
T16399 Opiranserin

P2X Receptor; GlyT; 5-HT Receptor GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
Opiranserin 是一种非阿片类和非 NSAID 镇痛候选药物,是 2 型甘氨酸转运蛋白 (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。它可用于术后疼痛的研究,对 rP2X3 有拮抗作用,IC50为0.87 μM。
T6526 GW791343 trihydrochloride

GW791343 3HCl

P2X Receptor Membrane transporter/Ion channel; Neuroscience
GW791343 trihydrochloride (GW791343 3HCl) 是 P2X7变构调节剂,有种属特异性,对人 P2X7的pIC50为6.9-7.2。
T75254 P2X7-IN-2 TFA

Others Others
P2X7-IN-2 TFA(化合物58)为P2X7受体抑制剂,以IC50为0.01 nM抑制IL-Iβ释放,适用于自身免疫病、炎症及心血管疾病研究。
T81579 P2X7 receptor antagonist-4

Others Others
P2X7 receptor antagonist-4(Compound 14a)是一种选择性P2X7R拮抗剂,其对人类和小鼠P2X7R的IC50值分别为64.7 nM和10.1 nM。该化合物能有效抑制NLRP3炎性体的激活,并在脓毒症模型小鼠中减少肾损伤,降低caspase-1、gasdermin D、IL-1β和IL-18的表达。
T63197 P2X3 antagonist 36

Others Others
P2X3 antagonist 36 是 P2X3拮抗剂。
T62488 P2X7 receptor antagonist-1

Others Others
P2X7 receptor antagonist-1 是一种嘌呤能 P2X7 受体拮抗剂,具有抗神经炎症效果。
T75162 P2X2/3 modulator-1

Others Others
P2X2/3 modulator-1 (化合物 46) 作为一种P2X2/3调节剂,主要应用于疼痛、中枢神经系统紊乱及炎症的研究。
T10560 P2X3 antagonist 34

BLU-5937

P2X3 antagonist 34 是一种对P2X3同型三聚体受体具有高效性、选择性和口服活性的拮抗剂,其IC50值针对人类P2X3、大鼠P2X3及豚鼠P2X3分别为25 nM、92 nM和126 nM。相比之下,该化合物对人类、大鼠和豚鼠的P2X2/3异三聚体受体展现低活性。P2X3 antagonist 34 显著具有抗咳功效,同时不会影响味觉。
T72198 P2X7 receptor antagonist-3

Others Others
P2X7 receptorantagonist-3 是一种有效的 P2X7受体拮抗剂,作用于人和大鼠的 P2X7RIC50值分别是 4.2 nM 和 6.8 nM。
T61566 P2X7 receptor antagonist-2

Others Others
P2X7 receptor antagonist-2 is a highly potent antagonist of the P2X7 receptor, exhibiting a pIC50 value range of 6.5-7.5. Its efficacy in combating neuroinflammation has been demonstrated [1].
T73335 P2X7-IN-2

Others Others
P2X7-IN-2 是P2X7受体抑制剂。P2X7-IN-2 抑制 IL-Iβ 的释放,IC50值为 0.01 nM。P2X7-IN-2 可用于自身免疫病,炎症以及心血管疾病的研究。
T79115 P2X3 antagonist 38

P2X Receptor Membrane transporter/Ion channel; Neuroscience
P2X3 Antagonist 38 (compound 4)为高效的口服P2X3拮抗剂,其IC50值对hP2X3为0.132 µM、对rP2X3为0.165 µM、对gpP2X3为0.421 µM。
T78606 P2X3-IN-1

P2X Receptor Membrane transporter/Ion channel; Neuroscience
P2X3-IN-1(示例7)为P2X3受体抑制剂,适用于神经源性疾病的研究。
T16564 PPADS tetrasodium

P2X Receptor; Na+/Ca2+ Exchanger Membrane transporter/Ion channel; Neuroscience
PPADS tetrasodiuma 是一种有效的 P2X 受体拮抗剂,也是是豚鼠气道平滑肌 Na/Ca²⁺ 交换逆模式的抑制剂,对谷氨酸/NMDA毒性有神经保护作用。PPADS tetrasodiuma 抑制 P2X1、P2X-2、P2X-3 和 P2X-5。
T8635 CI 75300

P2X Receptor Membrane transporter/Ion channel; Neuroscience
CI 75300 靶向 P2X 嘌呤受体 7(人)。
T13541 α,β-Methylene ATP trisodium

P2X Receptor Membrane transporter/Ion channel; Neuroscience
α,β-Methylene ATP trisodium 是 ATP 的膦酸酯类似物,是选择性 P2X 激动剂,诱导UBSM 收缩增强。α,β-Methylene ATP trisodium 抑制 P2X1 和 P2X3 但对 P2X2, 4 和 7 没有活性。
TP2226 BzATP triethylammonium salt

P2X Receptor Membrane transporter/Ion channel; Neuroscience
BzATP triethylammonium salt 是一种 P2X 受体激动剂,对 P2X1、P2X2、P2X3、P2X2/3、P2X4 和 P2X7 均有效 (pEC50=8.74/5.26/7.10/7.50/6.19/6.31/5.33)。BzATP triethylammonium salt 可以诱导细胞死亡并减少突触传递。
TP2297 TNP-ATP triethylammonium salt

Others Others
P2X receptor antagonist
T69053 ANAPP3

Others Others
ANAPP3 is a P2x-purinoceptor antagonist. It affects contractions in various muscle groups and tissues.
T69255 MRS-2339

Others Others
MRS-2339 is a P2X receptor activator.
T33506 MRS2220

MRS 2220,MRS-2220

Others Others
MRS2220 is a selective enhancer of the ATP effects at fast desensitizing P2X (P2X1 and P2X3) receptors.
T71950 PSB-12054

Others Others
PSB-12054 is a potent P2X4 receptor inhibitor. PSB-12054 has IC(50) of 0.189 μM and good selectivity versus the other human P2X receptor subtypes.
T39891 8-Bromo-ATP

8-Bromoadenosine 5'-triphosphate,8-Bromo-ATP,8-Br-ATP

Others Others
8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate) is a purinergic P2X receptor agonist and an ATP analogue. It exhibits cytotoxicity towards multiple myeloma cells, with an IC50 of 23.1 μM.
T71651 GSK1370319A

Others Others
GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM). GSK1370319A inhibits ATP-induced increase in IL-1β release and caspase 1 activation in lipopolysaccharide (LPS)-primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-relate...
T84928 2-Chloroadenosine 5-triphosphate sodium

2-chloro ATP

Others Others
2-Chloroadenosine 5-triphosphate (2-chloro ATP), an analog of ATP and adenine nucleotide, functions as an antagonist of the purinergic P2Y1 receptor, inhibiting ADP-induced intracellular calcium mobilization in Jurkat cells with a Ki value of 2.3 µM. Additionally, 2-chloro ATP acts as an agonist of purinergic P2X receptors, demonstrated by inducing inward currents in HEK293 cells expressing either human bladder smooth muscle or rat PC12 receptor forms, with EC50 values of 0.5 and 2.5 µM, respect...

化合物

P2X receptor-1
Cat.No: T61490
Synonym:
Target: Others
BAY-1797
Cat.No: T10466
Synonym:
Target: P2X Receptor
A 438079
Cat.No: T10207
Synonym:
Target: P2X Receptor
A-740003
Cat.No: T3690
Synonym: A 740003
Target: P2X Receptor
5-BDBD
Cat.No: T22518
Synonym:
Target: P2X Receptor
A-804598
Cat.No: T3639
Synonym: A 804598
Target: P2X Receptor
Indophagolin
Cat.No: T8946
Synonym:
Target: P2X Receptor, 5-HT Receptor, Autophagy
Eliapixant
Cat.No: T9519
Synonym: BAY 1817080
Target: P2X Receptor
Sivopixant
Cat.No: T40045
Synonym: S-600918,Sivopixant
Target: P2X Receptor
Aurintricarboxylic acid
Cat.No: T8333
Synonym: ATA,NSC-4056,NSC4056,金精三羧酸,NSC 4056
Target: Apoptosis, P2X Receptor, Influenza Virus, Topoisomerase
AF-353
Cat.No: T2087
Synonym: Ro-4
Target: P2X Receptor
AZD9056 hydrochloride
Cat.No: T14385
Synonym:
Target: P2X Receptor
RO-3
Cat.No: T5513
Synonym:
Target: P2X Receptor
JNJ-47965567
Cat.No: T4298
Synonym: JNJ-479655
Target: P2X Receptor
PSB-12062
Cat.No: T12568
Synonym: N-(p-Methylphenylsulfonyl)phenoxazine
Target: P2X Receptor
CE-224535
Cat.No: T14920
Synonym: PF-04905428
Target: P2X Receptor
AZ10606120 dihydrochloride
Cat.No: T14366
Synonym:
Target: P2X Receptor
KN-62
Cat.No: T2694
Synonym:
Target: CaMK, P2X Receptor, Autophagy
Lu AF27139
Cat.No: T9786
Synonym:
Target: P2X Receptor
BX430
Cat.No: T14844
Synonym:
Target: P2X Receptor, Calcium Channel
A-317491
Cat.No: TQ0002
Synonym: ABT 202
Target: P2X Receptor
Opiranserin hydrochloride
Cat.No: T9833
Synonym:
Target: P2X Receptor, GlyT, 5-HT Receptor
GW791343 dihydrochloride
Cat.No: T7805
Synonym: GW791343 (HCl)
Target: P2X Receptor
Gefapixant
Cat.No: T5099
Synonym: RO 4926219,AF219,MK-7264
Target: P2X Receptor
A 438079 hydrochloride
Cat.No: T2673
Synonym: A 438079 (hydrochloride),A-438079 hydrochloride,A-438079 HCl
Target: P2X Receptor
Opiranserin
Cat.No: T16399
Synonym:
Target: P2X Receptor, GlyT, 5-HT Receptor
GW791343 trihydrochloride
Cat.No: T6526
Synonym: GW791343 3HCl
Target: P2X Receptor
P2X7-IN-2 TFA
Cat.No: T75254
Synonym:
Target: Others
P2X7 receptor antagonist-4
Cat.No: T81579
Synonym:
Target: Others
P2X3 antagonist 36
Cat.No: T63197
Synonym:
Target: Others
P2X7 receptor antagonist-1
Cat.No: T62488
Synonym:
Target: Others
P2X2/3 modulator-1
Cat.No: T75162
Synonym:
Target: Others
P2X3 antagonist 34
Cat.No: T10560
Synonym: BLU-5937
Target:
P2X7 receptor antagonist-3
Cat.No: T72198
Synonym:
Target: Others
P2X7 receptor antagonist-2
Cat.No: T61566
Synonym:
Target: Others
P2X7-IN-2
Cat.No: T73335
Synonym:
Target: Others
P2X3 antagonist 38
Cat.No: T79115
Synonym:
Target: P2X Receptor
P2X3-IN-1
Cat.No: T78606
Synonym:
Target: P2X Receptor
PPADS tetrasodium
Cat.No: T16564
Synonym:
Target: P2X Receptor, Na+/Ca2+ Exchanger
CI 75300
Cat.No: T8635
Synonym:
Target: P2X Receptor
α,β-Methylene ATP trisodium
Cat.No: T13541
Synonym:
Target: P2X Receptor
BzATP triethylammonium salt
Cat.No: TP2226
Synonym:
Target: P2X Receptor
TNP-ATP triethylammonium salt
Cat.No: TP2297
Synonym:
Target: Others
ANAPP3
Cat.No: T69053
Synonym:
Target: Others
MRS-2339
Cat.No: T69255
Synonym:
Target: Others
MRS2220
Cat.No: T33506
Synonym: MRS 2220,MRS-2220
Target: Others
PSB-12054
Cat.No: T71950
Synonym:
Target: Others
8-Bromo-ATP
Cat.No: T39891
Synonym: 8-Bromoadenosine 5'-triphosphate,8-Bromo-ATP,8-Br-ATP
Target: Others
GSK1370319A
Cat.No: T71651
Synonym:
Target: Others
2-Chloroadenosine 5-triphosphate sodium
Cat.No: T84928
Synonym: 2-chloro ATP
Target: Others
Cat. No. Product Name Target Signaling Pathways
T4S0536 Bullatine A

Apoptosis; P2X Receptor Apoptosis; Membrane transporter/Ion channel; Neuroscience
Bullatine A 是一种有效的 P2X7拮抗剂,可抑制 ATP 诱导的细胞凋亡和 P2X 受体介导的炎症反应。它是乌头属的二萜生物碱,能缓解过敏反应,具有抗风湿、抗炎和抗伤害作用,可用于治疗关节炎等神经退行性疾病。

天然产物

Bullatine A
Cat.No: T4S0536
Synonym:
Target: Apoptosis, P2X Receptor
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