T8372
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Potassium Channel
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VU 0134992 是一个亚型偏好的,口服有效的和选择性的内向整流钾通道 Kir4.1阻滞剂,IC50为 0.97 μM。在 -120 mV 时,VU0134992对同分 Kir4.1 比 Kir4.1/5.1 共分通道 (IC50=9 μM) 高出 9 倍的选择性。 |
T13316
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Potassium Channel
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VU0134992 hydrochloride 是一个亚型偏好的,具有口服活性和选择性的内向整流钾通道Kir4.1阻滞剂,IC50为 0.97 μM。在 -120 mV 时,VU0134992 hydrochloride 对同分 Kir4.1 比 Kir4.1/5.1 共分通道 (IC50=9 μM) 高出 9 倍的选择性。 |
T0030
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Sodium Channel
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Bupivacaine hydrochloride (Vivacaine) 是NMDA 受体抑制剂,可用于慢性疼痛的研究。它可阻断钠、L-钙和钾通道,还阻断SCN5A 通道,IC50为 69.5 μM。 |
T26862
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BMS-902483 is a potent α7 partial agonist. BMS-902483 improved cognition in preclinical rodent models. BMS-902483 showed FLIR α7 EC50=9.3nM; α7 Electrophysiology, rat; Area EC50 = 140 nM; Peak, Area (Ymax %) = 40, 54. 5-HT3A IC50 = 480 nm. |
T4316
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Potassium Channel
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ML365 是有效的,选择性的双孔结构域钾通道TASK1/KCNK3抑制剂,IC50为 4 nM。它可用于检查 TASK1 通道的特定作用。 |
T26865
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BMS-933043 is a Selective α7 nAChR partial agonist. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM). BMS-933043 shows agonist activity in a calcium fluoresc |
T37702
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Pancuronium is an aminosteroid antagonist of muscle-type nicotinic acetylcholine receptors (nAChRs) with an IC50value of 14.8 nM using patch clamp electrophysiology in BOSC23 cells expressing mouse nAChRs.1It acts as a non-depolarizing neuromuscular blocking agent.2Pancuronium enhances anesthesia induced by isoflurane , reducing immobilization with an ED50value of 1.62 μg/kg.3
1.Liu, M., and Dilger, J.P.Site selectivity of competitive antagonists for the mouse adult muscle nicotinic acetylcholine receptorMol. Pharmacol.75(1)166-173(2009) 2.Buckett, W.R., Marjoribanks, C.E., Marwick, F.A., et al.The pharmacology of pancuronium bromide (Org.NA97), a new potent steroidal neuromuscular blocking agentBr. J. Pharmacol. Chemother.32(3)671-682(1968) 3.Miyazaki, Y., Sunaga, H., Hobo, S., et al.Pancuronium enhances isoflurane anesthesia in rats via inhibition of cerebral nicotinic acetylcholine receptorsJ. Anesth.30(4)671-676(2016) |
T11377
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Others
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GDC-0276, a potent, selective, reversible, and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM, offers potential for pain treatment while overcoming limitations associated with current pain medications, including addiction and off-target side effects. It is well tolerated and demonstrates a favorable pharmacokinetic profile. |