目录号 | 产品详情 | 靶点 | |
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T9042 | COX | ||
Teriflunomide impurity 3 (4-Amino-N-(4-trifluoromethylphenyl)benzamide) 是一种选择性COX-1抑制剂,IC50为 30 µM。 | |||
T0448 | BCL Thrombin Cysteine Protease COX PPAR | ||
(S)-(+)-Ibuprofen (Dexibuprofen) 是 Ibuprofen 的 S(+)-对映异构体,能够有效的抑制COX-1(IC50:2.1 μM)和COX-2(IC50:1.6 μM),。它具有抗癌、退热、止痛,抗炎的效果。 | |||
T19841 | Others | ||
Tribenoside (BG-356) 是血管保护剂,能够温和的镇痛、抗炎及伤口愈合,可用研究痔疮。 | |||
T6504 | Potassium Channel NMDAR iGluR | ||
Flupirtine maleate (Katadolon maleate) 是可透过血脑屏障的、具有口服活性的非阿片类化合物。它是间接 NMDAR 拮抗剂,可用于缓解疼痛的研究,具有神经保护特性。 | |||
T3S1416 | Apoptosis PKC | ||
Decursin (Decursinol angelate) 是一种细胞毒性剂,是一种来自朝鲜当归根的有效蛋白激酶 C 激活剂。它通过 Hippo/YAP 信号通路抑制 HepG2 细胞的生长。它通过下调 CXCR7 表达来抑制胃癌中的肿瘤生长,迁移和侵袭。 | |||
T6714 | Mitophagy FAAH Autophagy | ||
URB-597 (FAAH Inhibitor II) 是一种可口服的选择性FAAH 抑制剂。 它抑制大鼠脑膜、体外大鼠神经元和人肝微粒体中的 FAAH 活性,IC50分别为 5、0.5和 3 nM。它具有抗抑郁样作用,可研究缓解疼痛。 | |||
T6566 | Sodium Channel | ||
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是有效的钠通道阻滞剂。 | |||
T2S1464 | Others GABA Receptor | ||
Thiocolchicoside (Thiocolchicine 2-glucoside analog) 是秋水仙碱的半合成硫衍生物,是竞争性 GABAA 受体拮抗剂和甘氨酸受体拮抗剂。它是肌肉松弛剂,具有抗炎作用,可用于缓解疼痛的研究。 | |||
TP1559L | Calcium Channel | ||
Ziconotide Acetate (107452-89-1 free base) (Prialt) 是一种镇痛剂,已用于治疗神经性和非神经性疼痛。 Ziconotide 通过与位于伤害感受通路初级传入神经元末端部分的 N 型钙通道结合起作用,因此通过有效的镇痛作用减少突触传递。 | |||
T3280 | IL Receptor TNF | ||
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。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-00055 | Alpha-toxin Amm8 Protein, Androctonus mauritanicus, Recombinant (His & Myc) | Androctonus mauritanicus | Baculovirus | ||
Alpha toxins bind voltage-independently at site-3 of sodium channels (Nav) and inhibit the inactivation of the activated channels, thereby blocking neuronal transmission. The toxin principally slows the inactivation process of TTX-sensitive sodium channels. It discriminates neuronal versus muscular sodium channel, as it is more potent on rat brain Nav1.2/SCN2A (EC(50)=29 nM) than on rat skeletal muscle Nav1.4/SCN4A (EC(50)=416 nM). It also shows a weak activity on Nav1.7/SCN9A (EC(50)=1.76 uM). In vivo, the toxin produces pain hypersensibility to mechanical and thermal stimuli.(PubMed:23685008). It also exhibits potent analgesic activity (when injected intraperitoneally), increasing hot plate and tail flick withdrawal latencies in a dose-dependent fashion. This paradoxical analgesic action, is significantly suppressed by opioid receptor antagonists, suggesting a pain-induced analgesia mechanism that involves an endogenous opioid system. This led to hypothesis that pain relief induced by peripheral administration of Amm VIII may result from sensitization of primary afferent neurons and subsequent activation of an opioid-dependent noxious inhibitory control.
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