Sodium Channel

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1614	Riluzole	<1 mg/mL	46 mg/mL	46 mg/mL
S2454	Bupivacaine HCl	23 mg/mL	65 mg/mL	65 mg/mL
S1811	Amiloride HCl	6 mg/mL	53 mg/mL	5 mg/mL
S1256	Rufinamide	<1 mg/mL	18 mg/mL	<1 mg/mL
S1603	Furosemide	<1 mg/mL	66 mg/mL	<1 mg/mL
S5814	cariporide	<1 mg/mL	87 mg/mL	3 mg/mL
S5710	Ambroxol	-1 mg/mL	76 mg/mL	-1 mg/mL
S5490	Disopyramide	-1 mg/mL	67 mg/mL	-1 mg/mL
S5274	GS967	<1 mg/mL	45 mg/mL	46 mg/mL
S1445	Zonisamide	<1 mg/mL	42 mg/mL	5 mg/mL
S2524	Phenytoin Sodium	3 mg/mL	32 mg/mL	11 mg/mL
S1693	Carbamazepine	<1 mg/mL	47 mg/mL	18 mg/mL
S2785	A-803467	<1 mg/mL	72 mg/mL	11 mg/mL
S2560	Amiloride HCl dihydrate	17 mg/mL	0 mg/mL	0 mg/mL
S2525	Phenytoin	<1 mg/mL	50 mg/mL	13 mg/mL
S2874	Camostat Mesilate	10 mg/mL	99 mg/mL	<1 mg/mL
S2114	Dronedarone HCl	<1 mg/mL	80 mg/mL	40 mg/mL
S3024	Lamotrigine	<1 mg/mL	10 mg/mL	3 mg/mL
S4016	Ouabain	<1 mg/mL	100 mg/mL	100 mg/mL
S1965	Primidone	<1 mg/mL	44 mg/mL	3 mg/mL
S3064	Ambroxol HCl	<1 mg/mL	4 mg/mL	<1 mg/mL
S2041	Dyclonine HCl	6 mg/mL	15 mg/mL	36 mg/mL
S4229	Oxybuprocaine HCl	69 mg/mL	69 mg/mL	69 mg/mL
S3155	Mepivacaine HCl	57 mg/mL	3 mg/mL	8 mg/mL
S2500	Propafenone HCl	<1 mg/mL	69 mg/mL	<1 mg/mL
S4023	Procaine HCl	55 mg/mL	55 mg/mL	<1 mg/mL
S1619	Prilocaine	<1 mg/mL	44 mg/mL	44 mg/mL
S4038	Dibucaine HCl	76 mg/mL	76 mg/mL	76 mg/mL
S1391	Oxcarbazepine	<1 mg/mL	7 mg/mL	<1 mg/mL
S4058	Ropivacaine HCl	46 mg/mL	62 mg/mL	<1 mg/mL
S4180	Nefopam HCl	21 mg/mL	1 mg/mL	<1 mg/mL
S4061	Levobupivacaine HCl	64 mg/mL	64 mg/mL	57 mg/mL
S4080	Triamterene	<1 mg/mL	20 mg/mL	<1 mg/mL
S4200	Tolperisone HCl	56 mg/mL	56 mg/mL	56 mg/mL
S4210	Benzocaine	<1 mg/mL	33 mg/mL	33 mg/mL
S4669	Benzocaine hydrochloride	<1 mg/mL	40 mg/mL	40 mg/mL
S4668	Procaine	<1 mg/mL	47 mg/mL	47 mg/mL
S4225	Mexiletine HCl	43 mg/mL	43 mg/mL	43 mg/mL
S4235	Phenazopyridine HCl	<1 mg/mL	50 mg/mL	<1 mg/mL
S3751	Quinidine sulfate	9 mg/mL	100 mg/mL	100 mg/mL
S3907	Bulleyaconi cine A	-1 mg/mL	7 mg/mL	-1 mg/mL
S4284	Chloroprocaine HCl	61 mg/mL	61 mg/mL	<1 mg/mL
S2110	Vinpocetine	<1 mg/mL	3 mg/mL
S4290	Digoxin	<1 mg/mL	100 mg/mL	<1 mg/mL
S2118	Ibutilide Fumarate	89 mg/mL	89 mg/mL	89 mg/mL
S4294	Procainamide HCl	54 mg/mL	54 mg/mL	54 mg/mL
S3911	Veratramine	-1 mg/mL	63 mg/mL	-1 mg/mL
S1828	Proparacaine HCl	66 mg/mL	12 mg/mL	<1 mg/mL

Sodium Channel抑制剂（51）
新Sodium Channel产品

产品目录	产品描述	文献引用	实验数据
S1614	Riluzole Riluzole是谷氨酸盐释放抑制剂，具有神经保护、抗癫痫、抗焦虑以及麻醉作用。	Int J Mol Sci, 2016, 17(3):357 J Neuroimmune Pharmacol, 2013, 8(5):1098-105	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
S2454	Bupivacaine HCl Bupivacaine HCl 可以与钠离子通道的胞内部分结合从而阻断进入神经细胞的钠离子流，用于治疗心律不齐。	J Steroid Biochem Mol Biol, 2017, 172:89-97
S1811	Amiloride HCl Amiloride是一种选择性的T-type calcium channel阻滞剂，epithelial sodium channel（ENaC）阻滞剂，urokinase plasminogen activator (uPA)抑制剂，Ki=7 μM。	Environ Sci Technol, 2013, 47(18):10601-10 Atherosclerosis, 2015, 239(1):252-9
S1256	Rufinamide Rufinamide是一种电压门控式的sodium channel阻断剂，用作抗惊厥的药物。
S1603	Furosemide Furosemide 是一种有效的NKCC2抑制剂，用于治疗充血性心脏衰竭和水肿。	Sci Rep, 2018, 8(1):9302 Vascul Pharmacol, 2017, 99:74-82 Biomed Pharmacother, 2018, 101:145-154
S5814^New	cariporide Cariporide是有效的选择性NHE1抑制剂，在CHO-K1细胞中对hNHE1的IC50值为30 nM。
S5710^New	Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
S9142^New	Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
S5556^New	(-)-Sparteine Sulfate Sparteine Sulfate, a quinolizidine alkaloid, is the sulfate form of sparteini, which is a sodium channel blocker used as an oxytocic and an anti-arrhythmia agent.
S5490^New	Disopyramide Disopyramide is a class IA antiarrhythmic drug which acts via blockade of sodium channels depressing phase 0 of the action potential. Disopyramide possesses significant negative inotropic, anticholinergic effects and enhances AV nodal conduction.
S5274^New	GS967 GS967 is a potent and selective inhibitor of late I_Na with anti-arrhythmic actions.
S1445	Zonisamide Zonisamide是FDA批准的抗癫痫药物，阻断电压依赖性钠（+）通道和T型钙离子通道。
S2524	Phenytoin Sodium Phenytoin Sodium是一种失活的电压门控钠离子通道稳定剂。
S1693	Carbamazepine Carbamazepine 是一种钠离子通道抑制剂，作用于大鼠脑突触体时， IC50为131 μM。	DNA Cell Biol, 2019, 10.1089/dna.2018.4553
S2785	A-803467 A-803467是一种选择性Na_V1.8 channel抑制剂，IC50为8 nM，抑制抗河豚毒的电流，比作用于人类Na_V1.2， Na_V1.3， Na_V1.5和Na_V1.7选择性高100倍以上。
S2560	Amiloride HCl dihydrate Amiloride HCl dihydrate是一种有效的上皮细胞钠离子通道抑制剂。	Environ Sci Technol, 2013, 47(18):10601-10 Sci Rep, 2017, 7(1):5586
S2525	Phenytoin Phenytoin是一种失活的电压门控钠离子通道稳定剂。
S2874	Camostat Mesilate Camostat Mesilate是胰蛋白酶样的蛋白酶抑制剂，抑制上皮细胞钠离子通道(ENaC)功能，IC50为50 nM, 对Trypsin, Prostasin 和 Matriptase作用效果稍弱。
S2114	Dronedarone HCl Dronedarone HCl 用于治疗阵发性和持续性房颤或房扑的患者。	Nat Commun, 2016, 7:13023	Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 () and P<0.005 (*).
S3024	Lamotrigine Lamotrigine是一种新型抗惊厥药剂，作用于人类血小板和大鼠脑突触体，抑制5-羟色胺(5-HT)吸收，IC50分别为240 μM和474 μM。
S4016	Ouabain Ouabain是一种选择性的Na⁺/K⁺-ATPase抑制剂，与α2 /α3亚基结合，K_i为41 nM/15 nM。	Antiviral Res, 2016, 132:38-45 Nat Methods, 2015, 12(12):1129-31	Effect of pharmacological agents capable of increasing intracellular calcium concentration on RSV. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with a specific Na+/K+-ATPase inhibitor ouabain at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. Statistical significance between treated and control group were analyzed by t-test (, p < 0.05, *, p < 0.01).
S1965	Primidone Primidone 是一种嘧啶二酮类抗惊厥药。
S3064	Ambroxol HCl Ambroxol HCl是有效的神经性钠离子通道抑制剂，抑制抗TTX的钠离子电流，相位性阻滞，IC50为22.5 μM，抑制对TTX敏感的钠离子电流，IC50为100 μM。Phase 3。
S2041	Dyclonine HCl Dyclonine HCl是Dyclonine的盐酸盐形式，是一种口服麻醉剂。Dyclonine可逆地与神经元细胞膜上活化的钠离子通道结合，减少神经元膜对钠离子的通透性。
S4229	Oxybuprocaine HCl Oxybuprocaine HCl是一种局部麻醉剂，尤其在眼科与耳鼻咽喉科使用。其与钠离子通道结合，可逆地稳定神经元细胞膜，减少其对钠离子的通透性。
S3155	Mepivacaine HCl Mepivacaine 是一种叔胺，用作局部麻醉剂。
S2500	Propafenone HCl Propafenone HCl是一种典型的抗心律失常药物，用于治疗与心跳加速相关的疾病，如心房和心室心律失常。
S4023	Procaine HCl Procaine HCl是一种钠离子通道的，NMDA受体以及乙酰胆碱受体抑制剂， IC50分别为60 μM， 0.296 mM何45.5 μM，也是一种，5-HT3抑制剂，K_D为1.7 μM。	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. p<0.05, *p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
S1619	Prilocaine Prilocaine 是一种氨基酰胺类的局部麻醉剂。它作用于神经元细胞膜上的钠离子通道，限制癫痫发作的扩散。
S4038	Dibucaine HCl Dibucaine HCl是一种局部麻醉剂。
S1391	Oxcarbazepine Oxcarbazepine是一种抗惊厥和稳定情绪的药物。抑制[3H]BTX与sodium channels结合， IC50位160 μM，也抑制²²Na⁺汇入大鼠脑i突触体， IC50约为100 μM。
S4058	Ropivacaine HCl Ropivacaine HCl是一种麻醉剂，通过可逆地抑制钠离子流入来阻断神经纤维上冲动的传导。
S4180	Nefopam HCl Nefopam HCl是一种中枢作用剂，但是是非阿片类的镇痛药，抑制电压门控钠通道，及抑制5-羟色胺，多巴胺和去甲肾上腺素的再吸收。
S4061	Levobupivacaine HCl Levobupivacaine HCl，丁哌卡因的纯净S(-)-对映体,是一种可逆神经元的sodium channel抑制剂，用作长效局部麻醉剂。
S4080	Triamterene Triamterene以电压依赖方式阻断上皮细胞钠离子通道(ENaC)，IC50值为4.5 μM.
S2318	Lappaconitine Lappaconitine (LC) is a natural diterpenoid alkaloid (DTA), acting as a human heart sodium channel blocker and possessing a wide range of biological activities, including anti-arrhythmic, anti-inflammatory, antioxidative, anticancer, epileptiform etc.
S4200	Tolperisone HCl Tolperisone HCl是一种离子通道抑制剂和中枢性肌肉松弛剂。
S4210	Benzocaine Benzocaine 是对氨基苯甲酸乙酯 (PABA), 是一种局部麻醉剂，用作外用止痛药或常用于止咳。
S4669	Benzocaine hydrochloride Benzocaine hydrochloride是一种表面麻醉剂，通过阻止沿着神经纤维及在神经末梢的脉冲传播发挥作用。
S4668	Procaine Procaine是苯甲酸类化合物，具有局部麻醉和抗心律失常的活性。Procaine结合并抑制电压依赖性钠离子通道，因而抑制脉冲起始和传导所需的离子通量。
S4225	Mexiletine HCl Mexiletine HCl 属于IB类抗心律失常药，抑制钠离子通道，降低内流钠电流。
S4235	Phenazopyridine HCl Phenazopyridine HCl是一种局部镇痛剂，已被用于治疗泌尿系统疾病。它是sodium channel protein type 1 subunit alpha的抑制剂。
S3751	Quinidine sulfate Quinidine可抑制电压依赖性钠离子通道，同时也具有抗毒蕈碱和抗疟疾活性。
S3907	Bulleyaconi cine A Bulleyaconitine A (BLA) is an active ingredient of Aconitum bulleyanum plants and classified as an "aconitine-like" alkaloid. It is a potent use-dependent blocker for both Nav1.7 and Nav1.8 Na+ currents.
S4284	Chloroprocaine HCl Chloroprocaine HCl 是手术治疗中的局部麻醉剂。
S2110	Vinpocetine Vinpocetine选择性抑制电压敏感型钠离子通道，用于治疗中风，血管性痴呆和阿尔茨海默症。
S4290	Digoxin Digoxin是一种经典的Na,K-ATPase抑制剂，其对α2β3亚型的选择性高于α1β1亚型，用于治疗心房颤动和心脏衰竭。	J Vasc Surg, 2018, 68(5):1538-1550.e2
S2118	Ibutilide Fumarate Ibutilide Fumarate是第三类抗心律失常药物，主要用于急性新梗阻的心房颤动(房颤)/心房扑动(房扑)，适用于近期发作的房颤或房扑逆转成窦性心律，向内钠电流感应缓慢，这会延长心肌细胞的动作电位和不应期。	Gynecol Oncol, 2018, 151(3):525-532
S4294	Procainamide HCl Procainamide HCl是一种sodium channel的阻断剂，也是DNA甲基转移酶抑制剂，用于心律失常的治疗。
S3911	Veratramine Veratramine, a major alkaloid from Veratrum nigrum L., has distinct anti-tumor and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has a good stability in the gastrointestinal tract during its absorption.
S1828	Proparacaine HCl Proparacaine HCl是电压门控的钠离子通道的拮抗剂，ED50是3.4 mM。

研究领域

产品类型

Sodium Channel

信号通路图

研究领域