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| 货号 | 产品名 | 中文名称 | 产品描述 |
|---|---|---|---|
| SJ-MX0777 | KN-62 |
KN-62是有效的、高择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂，它直接与酶的钙调蛋白结合位点结合，对大鼠脑 CaMK-II 的Ki 值为 0.9 μM。KN-62 是一种非竞争性purinergic receptor P2X7 (P2RX7)的拮抗剂，IC50是15 nM。 |
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| SJ-MX3275 | AF-353 | AF-353 (Ro-4) is a potent P2X3/P2X2/3 receptor antagonist; inhibits human and rat P2X3 (pIC50 = 8.0). | |
| SJ-MX3597 | A-317491 | A-317491 is a selective non-nucleotide antagonist of P2X3 and P2X2/3 receptor activation. A-317491 potently blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and is highly selective (IC50 >10 uM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 also blocks native P2X3 and P2X2/3 receptors in rat dorsal root ganglion neurons. | |
| SJ-MX1584 | Gefapixant | 吉法匹生 | Gefapixant (MK-7264)是一个口服的、P2X3受体活性拮抗剂，其对人同源重组 hP2X3和hP2X2/3的IC50值分别是~30 nM和100-250 nM. |
| SJ-MX3633 | A 438079 hydrochloride | A-438079 hydrochloride (A438079; A 438079), the hydrochloride salt of -438079, is a novel, potent, and selective P2X7 receptor antagonist with anti-Parkinson's disease effects. It inhibits P2X7 receptor with a pIC50 of 6.9. A438079 protects against acetaminophen-induced liver injury by inhibiting p450 isoenzymes, not by inflammasome activation. A-438079 reduced electrographic and clinical seizure severity during status epilepticus and reduced seizure-induced neuronal death in the neocortex. Blockade of P2X(7) receptors may represent a novel protective strategy for striatal DA terminals in Parkinson's disease. | |
| SJ-MN1171 | Lappaconitine | 高乌甲素 | 高乌甲素 (Lappaconitine) 是从高乌头中分离到的一种天然产物，可用于缓解疼痛的研究。 |
| SJ-MX0159 | A-740003 | A-740003 是一种有效的，选择性的，竞争性的 P2X7 receptor 拮抗剂，抑制大鼠和人的 P2X7 受体，IC50 值分别为 18 和 40 nM。 | |
| SJ-MX1139 | Indophagolin | Indophagolin 是一种有效的含 indoline 的自噬 (autophagy) 抑制剂 (IC50=140 nM)。Indophagolin 拮抗嘌呤能受体P2X4、P2X1 和 P2X3，IC50 分别为 2.71、2.40 和 3.49 μM。Indophagolin 还拮抗 Gq 蛋白偶联的 P2Y4、P2Y6 和 P2Y11 受体(IC50s =3.4~15.4 μM)。Indophagolin 五羟色胺受体5-HT6 有较强的拮抗作用 (IC50=1.0 μM)，对 5-HT1B、5-HT2B、5-HT4e 和 5-HT7 有中度拮抗作用。 | |
| SJ-MX1407 | A-804598 | 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 nM， 10 nM 和 11 nM。 | |
| SJ-MX4295 | BX430 |
BX430是人P2X4受体通道的非竞争性变构拮抗剂 (通过膜片钳电生理学测定的IC50值为0.54 μM)，BX430对P2X4的选择性是P2X1-P2X3, P2X5和P2X7的10-100倍。BX430 具有物种特异性。BX430 用于慢性疼痛和心血管疾病。 |
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| SJ-MX5473 | JNJ-47965567 | ||
| SJ-MX5381 | Minodronic acid | ||
| SJ-MX5028 | BAY-1797 | ||
| SJ-MX4914 | AZ10606120 dihydrochloride | ||
| SJ-BP0296 | 10Panx | ||
| SJ-MX5735 | Piromelatine |
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