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| 货号 | 产品名 | 中文名称 | 产品描述 |
|---|---|---|---|
| SJ-MX1026 | Amiloride hydrochloride | 盐酸阿米洛利 |
Amiloride hydrochloride (MK-870 hydrochloride) 是上皮钠通道 (epithelial sodium channel, ENaC) 和尿激酶型纤溶酶原激活物受体 (uTPA) 的抑制剂，Ki=7 μM。Amiloride hydrochloride 是 polycystin-2 (PC2; TRPP2) 通道阻断剂。 |
| SJ-MX2930 | PF 05089771 | PF-05089771 (PF05089771) is a potent and subtype selective NaV1.7 inhibitor (IC50 = 11 nM) and Nav1.8 voltage-gated sodium channel blocker with the potential to be used in the treatment of chronic neuropathic pain. As of June 2014, it has completed phase II clinical trials for wisdom tooth removal and primary erythromelalgia. PF-05089771 binds to a site in the voltage sensing domain and interacts with the voltage-sensor domain (VSD) of domain IV. PF-05089771 exhibits a slow onset of block that is depolarization and concentration dependent, with a similarly slow recovery from block. Furthermore, the onset of block by PF-05089771 develops with similar rates using protocols that bias channels into predominantly fast- or slow-inactivated states, suggesting that channel inhibition is less dependent on the availability of a particular inactivated state than the relative time that the channel is depolarized. | |
| SJ-MX3303 | GS967 | GS967 (also known as GS-458967) is a novel, potent, and selective sodium channel inhibitor exhibiting potent antiarrhythmic effects in various in vitro and in vivo models. It inhibit cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively. The antiarrhythmic mechanism of GS967 has been attributed to preferential suppression of late sodium current. GS967 (10, 100, 300 nM) completely attenuates the effect of ATX-II (10 nM) to increase action potential duration (APD) and APD variability in ventricular myocytes, with an apparent IC50 value of ∼10 nM and decreased the beat-to-beat variability of APD. GS967 selectively suppressed late I(Na) and prevented and/or reduced the incidence of experimentally induced arrhythmias in rabbit myocytes and hearts. | |
| SJ-MX3420 | Nicainoprol | 尼卡普醇 | Nicainoprol, formerly known as CAS-924; RU-42924, is calcium channel antagonist and a putative class I antiarrhythmic agent. Nicainoprol could be useful in the prevention and treatment of arrhythmias associated with acute myocardial infarction. |
| SJ-MX3703 | Cariporide | 卡立泊来德 | Cariporide (HOE-642) 是选择性的 Na+/H+ 交换抑制剂。 |
| SJ-MX3767 | PF-06869206 | PF-06869206 is a novel, potent, selective and orally bioavailable inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM. Sodium-phosphate cotransporter 2a, or NaPi2a (SLC34A1), is a solute-carrier (SLC) transporter located in the kidney proximal tubule that reabsorbs glomerular-filtered phosphate. Inhibition of NaPi2a may enhance urinary phosphate excretion and correct maladaptive mineral and hormonal derangements associated with increased cardiovascular risk in chronic kidney disease-mineral and bone disorder (CKD-MBD). To date, only nonselective NaPi inhibitors have been described. The oral PK profile of inhibitor PF-06869206 in rodents allows for the exploration of the pharmacology of selective NaPi2a inhibition. | |
| SJ-MX2701 | Propoxycaine hydrochloride | 盐酸丙氧卡因；丙氧卡因盐酸盐 | Propoxycaine hydrochloride is the hydrochloride salt form of Propoxycaine, a para-aminobenzoic acid ester with local anesthetic activity. |
| SJ-MX1484 | Diphenidol hydrochloride | 盐酸地芬尼多 | Diphenidol hydrochloride (Difenidol hydrochloride) 是一种非选择性的毒蕈碱 M1-M4 受体 (muscarinic M1-M4 receptor) 拮抗剂，具有抗心律失常活性。Diphenidol hydrochloride 也是神经细胞电压门控离子通道 (Na+，K+，Ca2+) 的有效非特异性阻滞剂。 |
| SJ-MX1293 | Oxcarbazepine | 奥卡西平 | Oxcarbazepine 是一种钠通道 (sodium channel) 阻滞剂。Oxcarbazepine 有效抑制胶质母细胞瘤细胞生长并诱导胶质母细胞瘤细胞凋亡 (apoptosis) 或 G2/M 停滞。具有抗癌和抗惊厥作用。 |
| SJ-MX2481 | Mexiletine hydrochloride | 盐酸美西律 | Mexiletine hydrochloride (KOE-1173 hydrochloride) is a class Ib antiarrhythmic drug. The primary mechanism of action is blocking fast sodium channels, reducing the phase 0 maximal upstroke velocity of the action potential. |
| SJ-MX2521 | Oxybuprocaine hydrochloride | 奥布卡因盐酸盐 | Oxybuprocaine hydrochloride (Benoxinate hydrochloride) 可逆地阻断钠通道 (sodium channels)，并防止角膜，结膜和巩膜中疼痛神经的冲动传播。Oxybuprocaine hydrochloride 专用于眼科和耳鼻喉科。 |
| SJ-MX2652 | Meticrane | 美替克仑 | Meticrane 是一种利尿剂。Meticrane 抑制远曲小管中钠离子和氯离子的重吸收。Meticrane 可于研究原发性高血压。 |
| SJ-MX2699 | Propafenone hydrochloride | 盐酸普罗帕酮 | Propafenone hydrochloride (formerly SA-79; SA79; Rytmonorm; Pronon; Arythmol; Baxarytmon; Cuxafenon; Fenoprain), the hydrochloride salt of Propafenone, is an approved class 1C anti-arrhythmic drug. It acts as a sodium channel protein inhibitor, which has been used to treat illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias. |
| SJ-MX3278 | Mepivacaine hydrochloride | 盐酸甲哌卡因 | Mepivacaine hydrochloride is a local anesthetic. It reversibly blocks inward current of transient Na+, as well as the steady-state K+ outward current. Mepivacaine hydrochloride blocks tandem pore (TASK) and Kv1.5, potassium channels in model systems. |
| SJ-MX3356 | Benzocaine | 苯佐卡因 | Benzocaine (H-4-Abz-OEt; NSC-4688; NSC-41531; trade name Orajel among others), the ethyl ester of p-aminobenzoic acid (PABA), is a local anesthetic that has been widely used as a topical pain reliever or in cough drops. Benzocaine acts by reversibly inactivating voltage-dependent sodium channels. It is the active ingredient in many OTC anesthetic ointments (e.g. products for oral ulcers). It is also used in combination with antipyrine as A/B otic drops to relieve ear pain and to remove earwax. |
| SJ-MX3787 | Mebeverine hydrochloride | 美贝维林盐酸盐 | Mebeverine hydrochloride 是 β-苯乙胺的衍生物，一种增肌剂，可有效阻止肠道蠕动。Mebeverine hydrochloride直接阻断电压控制的钠通道 (voltage-operated sodium channels)，抑制细胞内钙的积累。 |
| SJ-MN0276 | Vinpocetine | 长春西汀 | Vinpocetine(Ethylapovincaminate)是一种长春花生物碱衍生物，可阻断Na通道。Vinpocetine抑制的值为17.17μM。Vinpocetine还是抑制剂，并通过直接靶向抑制依赖性炎症反应，已被广泛用于研究脑血管疾病。 |
| SJ-MN0277 | Ajmaline | 阿义马林 | Ajmaline (Cardiorythmine) 是一种钠通道 (sodium channel) 阻断剂，1A 类抗心律失常剂。Ajmaline 阻断 HERG 电流，在 HEK 细胞的 IC50 为 1 μM，爪蟾卵母细胞为 42.3 μM。Ajmaline 可用于室性心动过速的研究。 |
| SJ-MX1124 | Sodium ionophore III | 钠离子载体III | Sodium ionophore III是适用于测定血液、血浆、血清中的钠活性的Na+载体。 |
| SJ-MX4117 | VX-150 | VX-150 (EOS-62073) 是一种口服生物可利用的前药，可快速转化为其活性部分，相对于其他钠通道亚型（> 400 倍），它是 NaV1.8 的高度选择性抑制剂。 |
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