32
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3280 |
Clodronate disodium tetrahydrate
clodronic acid disodium tetrahydrate,Disodium clodronate tetrahydrate,Clastoban,氯屈膦酸二钠(四水合物),Clodronate disodium |
IL Receptor; TNF | Apoptosis; Immunology/Inflammation |
Clodronate disodium tetrahydrate (Clastoban) 是一种选择性、高效的,可逆、Cl-竞争性的囊泡核苷酸转运体阻滞剂(IC50:15.6 nM)。是一种双膦酸盐,具有抗骨质疏松、抗炎作用,可用于缓解疼痛的研究。它可抑制神经元释放囊泡 ATP,缓解慢性神经病理性疼痛和炎症性疼痛。 | |||
T7881 |
CTP disodium dihydrate
|
P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
CTP disodium dihydrate 是 P2X4 嘌呤受体的激动剂。 | |||
T23164 |
PIT
2,2'-Pyridylisatogen tosylate |
P2Y Receptor | GPCR/G Protein; Neuroscience |
PIT (2,2'-Pyridylisatogen tosylate) 是嘌呤能受体 P2Y1 的特异性非竞争性拮抗剂,对人 P2Y1 的 IC50 为 0.14 μM。 PIT 不影响核苷酸结合,可用于慢性支气管炎和哮喘的研究。 | |||
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。 | |||
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。 | |||
T20731 |
Brilliant blue G-250
酸性蓝 90,BBG,Acid blue 90, Coomassie Brilliant Blue G,Brilliant Blue G |
P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
Brilliant blue G-250 (Acid blue 90, Coomassie Brilliant Blue G) 是一种可视化的染料,常用于 SDS-PAGE 分离蛋白质,染色过程简单,定量高。在 Bradford 蛋白质分析中,它能够与蛋白质结合,通过595 nm 处的吸光度确定蛋白质浓度。它也是一种安全的 P2×7R 选择性拮抗剂,有望使 NLRP3炎症体失活。 | |||
T19049 |
Procion Blue HB
蓝色染料,Reactive Blue 2 |
Others | Others |
Procion Blue HB is an antagonist of purinergic. | |||
T23241 |
Ro 0437626
|
Others | Others |
P2X1 purinergic receptor antagonist | |||
T70450 |
BMS-870145
|
||
BMS-870145 is a potent and selective P2Y1 purinergic receptor antagonist.. | |||
T70667 |
KF 20274
|
||
KF 20274 is an adenosine A1 antagonist; purinergic receptor antagonist. | |||
T83823 |
Sp-Uridine-5'-O-(1-thiotriphosphate) sodium
Sp-UTP-α-S |
||
Sp-Uridine-5'-O-(1-thiotriphosphate) (Sp-UTP-α-S) 是 purinergic Y2 (P2Y2) 和 P2Y4 受体的核苷酸激动剂。它在表达 purinergic P2Y2 或 P2Y4 受体的 1321N1 星形胶质瘤细胞中诱导肌醇磷酸累积(EC50s 分别为 14 和 81 µM)。 | |||
T74409 | EVT-401 | ||
EVT-401 (P2X7 receptor antagonist-1),一种嘌呤能P2X7受体拮抗剂,具抗神经炎症作用。 | |||
T29730 |
AGR-540
AGR540 |
||
AGR-540 is a prodrug of AGR-529. AGR-540 has been shown to return plasma triglyceride concentrations to normal levels in mouse models. This effect may be attributed to an interaction of the molecule with A1 purinergic receptors of adipose tissue. | |||
T23581 |
2-Methylthioadenosine diphosphate trisodium
2 Methylthio ADP,2MeSADP,2-Methylthio-ADP,2 MeS ADP,2-MeS-ADP |
||
2-MeS-ADP is a purinergic agonist that acts by displaying selectivity for P2Y1, P2Y12, and P2Y13 receptors and inhibiting cAMP accumulation. | |||
T62488 | P2X7 receptor antagonist-1 | ||
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。 | |||
T39891 |
8-Bromo-ATP
8-Bromoadenosine 5'-triphosphate,8-Bromo-ATP,8-Br-ATP |
||
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. | |||
T83839 |
Uridine 5'-methylenediphosphate sodium
α,β-methylene UDP,UMP-CP |
||
Uridine 5’-methylenediphosphate (UMP-CP) 是 purinergic P2Y14 受体的激动剂,同时也是 UDP 的一种水解稳定衍生物。它在表达人类 P2Y14 的细胞中选择性地抑制 cAMP 产生,相较于表达人类 P2Y6 的细胞(EC50s 分别为 11 和 339 nM)。 | |||
T36222 |
2-oxo Clopidogrel
|
||
2-oxo Clopidogrel is an intermediary metabolite of clopidogrel . Clopidogrel is a prodrug that is converted to its active metabolite via two sequential oxidative steps. The first step leads to formation of 2-oxo clopidogrel, followed by conversion to the active metabolite, which binds specifically and irreversibly to the platelet P2Y12 purinergic receptor, inhibiting ADP-mediated platelet activation and aggregation. | |||
T83822 |
Rp-Uridine-5'-O-(1-thiotriphosphate) sodium
Rp-UTP-α-S |
||
Rp-Uridine-5'-O-(1-thiotriphosphate)(Rp-UTP-α-S)是一种核苷酸激动剂,针对嘌呤P2Y2和P2Y4受体。在表达P2Y2或P2Y4受体的1321N1星形胶质细胞中,它能够促进肌醇磷酸的积累(EC50s分别为5.4 和27 µM)。 | |||
T83833 |
Rp-2'-Deoxyuridine-5'-O-(1-thiotriphosphate) sodium
Rp-dUTP-α-S |
||
Rp-2'-Deoxyuridine-5'-O-(1-thiotriphosphate) (Rp-dUTP-α-S) 是含硫核苷酸 dUTP-α-S 的同分异构体,也是嘌呤P2Y2受体的激动剂。在表达P2Y2受体的1321N1星形胶质瘤细胞中,该化合物特异性诱导肌醇磷酸积累(EC50 = 12.5 µM),相较于表达P2Y4的1321N1细胞,在10 µM浓度下效果更显著。 | |||
T36112 |
Clopidogrel Carboxylic Acid (hydrochloride)
|
||
Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active thiol metabolite via CYP2C19 in the liver enables its anti-aggregating activity. An estimated 15% of administered clopidogrel is metabolized by CYP2C19 to the thiol metabolite. Clopidogrel carboxylic acid i... | |||
T83813 |
8-Azidoadenosine-5'-O-diphosphate sodium
8-azido-ADP,Click Tag™ 8-Azidoadenosine-5'-O-diphosphate |
||
8-Azidoadenosine-5'-O-diphosphate(8-azido-ADP)是ATP前体和嘌呤受体配体ADP的可点击形式。8-azido-ADP的放射性标记形式已被用作各种蛋白质的光亲和标签,包括从牛脑中分离的谷氨酸脱氢酶(GDH)同工酶,以及从兔网织红细胞中分离的真核翻译起始因子2(eIF2)和鸟苷核苷酸交换因子(GEF)。 | |||
T33631 |
Neocuproine
Neocuproin |
||
Neocuproine 是一种铜 (I) 螯合剂,可增强电场刺激引起的输精管收缩的嘌呤能成分,常被用作配位试剂和铜离子检测剂。Neocuproine 与铜离子形成稳定的络合物,并可在某些化学反应和分析方法中起到催化作用。Neocuproine 作为铁和钴上的氧化还原活性配体平台,对NSC34细胞氧化损伤的保护作用。 | |||
T37313 | ITH15004 | ||
ITH15004 is a non-nucleotide antagonist of the purinergic P2X7receptor (IC50= 9 μM in HEK293 cells expressing the human receptor).1It inhibits ATP-induced currents inX. laevisoocytes expressing the human P2X7receptor when used at a concentration of 100 μM. ITH15004 (1 μM) decreases IL-1β release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA). 1.Calzaferri, F., Narros-Fernández, P., de Pa... | |||
T35431 |
(±)-Clopidogrel (hydrochloride)
|
||
Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active metabolite via CYP2C19 in the liver enables its anti-aggregating activity. Marketed under the name Plavix , clopidogrel in combination with aspirin has been shown to be beneficial in the prevention of vascu... | |||
T83827 |
Adenosine-5'-O-(3-thiotriphosphate) sodium
ATPγS,Adenosine 5'-(γ-thio)-triphosphate |
||
Adenosine-5'-O-(3-thiotriphosphate)(ATPγS)是一种purinergic P2Y11受体的激动剂。在表达人类或犬类P2Y11受体的CHO-K1细胞中,能够诱导肌醇磷酸累积(EC50s分别为1.2和19.3 µM)。ATPγS(10 µM)能抑制Junin病毒导致的编码骨形态生成蛋白6(BMP6)的mRNA水平增加,并减少Junin病毒感染的初代大鼠成骨细胞中的粒子形成单位(PFUs)。使用25 µM浓度时,可以诱导MIN6胰岛β细胞分泌胰岛素。 | |||
T83803 |
UDP-β-S sodium
Uridine-5' O-(2-thiodiphosphate) |
||
UDP-β-S是一种针对嘌呤P2Y6受体的激动剂。它在表达P2Y6受体的1321N1细胞中,以选择性的方式诱导肌醇磷酸的累积(EC50 = 28 nM),相较于表达P2Y1、P2Y2或P2Y4受体的细胞,在10 µM时效果更显著。在1 µM浓度下,UDP-β-S诱导分离的大鼠主动脉平滑肌细胞的DNA合成。 | |||
T83840 |
Uridine-5'-O-(3-thiotriphosphate) sodium
UTP-γ-S |
||
Uridine-5'-O-(3-thiotriphosphate) (UTP-γ-S) 是UTP的一种抗水解衍生物,是嘌呤P2Y2受体的激动剂。在表达人类P2Y2受体的1321N1星形胶质瘤细胞中,其可诱导肌醇磷酸盐的形成(EC50 = 240 nM),并且在来自囊性纤维化患者的原代鼻上皮细胞中以浓度依赖的方式诱导氯离子分泌。UTP-γ-S在分离的人类冠状动脉中诱导血管收缩(EC50 = 25.1 µM)。 | |||
T83808 |
Sp-Adenosine-5'-O-(1-thiotriphosphate) sodium
Sp-ATP-α-S |
||
Sp-Adenosine-5'-O-(1-thiotriphosphate) (Sp-ATP-α-S) 是一种含硫核苷酸衍生物 ATP-α-S 的异构体,也是嘌呤P2Y1受体的激动剂。在表达P2Y1受体的HEK293细胞中增加钙离子的流动(对人类受体的EC50 = 9.4 nM)。Sp-ATP-α-S 抑制了ADP诱导的孤立人类血小板聚集(Ki = 4 μM)。它还能引起经卡巴胆碱预收缩的豚鼠十二指肠松弛(EC50 = 426 nM)。 | |||
T83807 |
Rp-Adenosine-5'-O-(1-thiotriphosphate) sodium
Rp-ATP-α-S |
||
Rp-Adenosine-5'-O-(1-thiotriphosphate)(Rp-ATP-α-S)是一种含硫核苷酸衍生物ATP-α-S的异构体,同时也是嘌呤P2Y1受体的激动剂。在表达人类P2Y1受体的HEK293细胞中,Rp-ATP-α-S能增加钙的动员(EC50 = 75 nM)。该化合物与洗涤的人类孤立血小板结合(Ki = 156 nM),抑制由ADP引发的人类富血小板血浆(PRP)的聚集(pA2 = 4.74),并且能够抑制前列腺素E1(PGE1)在人类孤立PRP中引发的cAMP产生(pA2 = 5.26)。同时,Rp-ATP-α-S还能引起用氨基甲酰胆碱预先缩紧的豚鼠结肠条带的松弛(EC50 = 56 nM)。此外,Rp-ATP-α-S已经被用于合成被细菌核糖开关识别的环状二核苷酸。 | |||
T83802 |
TNP-ATP sodium
|
||
TNP-ATP是ATP的衍生物,同时是嘌呤P2Y1、P2X3和P2X2/3受体的拮抗剂(IC50s分别为6、0.9和7 nM,在表达人类受体的HEK293细胞中)。该化合物相对于嘌呤P2X2、P2X4和P2X7受体显示出选择性(IC50s分别为2、15.2和>30 µM,在表达人类受体的HEK293细胞中)。TNP-ATP能降低表达P2X3和P2X2/3受体的1321N1细胞中乙酸诱导的钙流量(IC50s分别为100和62 nM)。它还可以减轻小鼠模型中由乙酸诱发的痛性绞曲(ED50 = 6.35 µmol/kg)。在403 nm激发下,其发射最大峰值为547 nm,当结合于胰岛素降解酶(IDE)时,其相对荧光强度增加四倍,并且发射峰移至538 nm。 | |||
T83820 |
TNP-GTP sodium
TNP-Guanosine 5'-triphosphate |
||
TNP-GTP是一种荧光衍生物,源自蛋白质合成与糖异生的能量底物鸟苷三磷酸(GTP)。其在水中激发波长为410 nm时,发射最大波长为552 nm,而在40%和80%的N,N-二甲基甲酰胺中,其荧光强度增加,发射波长分别向544 nm和532 nm移动,这是因为N,N-二甲基甲酰胺的极性比水小。TNP-GTP是谷氨酸脱氢酶的抑制剂(Ki = 2.7 μM)。当与谷氨酸脱氢酶结合时,TNP-GTP的荧光强度增加,且发射波长从552 nm变为545 nm,此效果可以通过加入GTP来阻断。TNP-GTP还是嘌呤P2X2和P2X2/3受体的拮抗剂(IC50s分别为0.4和1.2 nM)。它还选择性抑制大鼠可溶性鸟苷酸环化酶(sGC; Ki = 11 nM)高于牛肝谷氨酸脱氢酶(GDH; Ki = 2.7 µM)以及钙调素依赖的B. pertussis腺苷酸环化酶(AC)毒素(Kis在存在锰或镁时分别为20和320 µM)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T19397 |
L-Methionine sulfoxide
L-蛋氨酸亚砜,H-Met(O)-OH |
Endogenous Metabolite | Metabolism |
L-Methionine sulfoxide (H-Met(O)-OH) 是一种甲硫氨酸的代谢产物,能够诱导 M1/classical 巨噬细胞极化,并调节氧化应激和嘌呤能的信号传递参数。 | |||
T20089 |
ATP
Atipi,ATP disodium salt hydrate,Triphosphoric acid adenosine ester,Ara-ATP,Triphosphaden,Adenosine triphosphate;Ara-ATP,Adenosine triphosphate |
Endogenous Metabolite | Metabolism |
ATP (Adenosine triphosphate) 可为细胞提供能量,参与整体能量平衡,维持细胞内稳态。ATP 可以通过与特异性嘌呤能受体的相互作用充当细胞外信号分子,以介导神经传递、炎症、细胞凋亡和骨重塑等多种过程。 | |||
T2946 |
Tanshinone IIA sulfonate sodium
丹参酮IIA磺酸盐,丹参酮IIA-磺酸钠,Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium |
CaMK; P450; Calcium Channel | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) 是从丹参中提取的丹参酮IIA 的水溶性衍生物,是SOCE 抑制剂,用于心血管疾病的研究。 |