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38

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15385	Glibornuride	Potassium Channel	Membrane transporter/Ion channel
	Glibornuride 是对 ATP 敏感的 K+通道 (KATP 通道) 阻滞剂，pKi 为 5.75。Glibornuride 显示抗糖尿病活性。
T9714	Atpenin A5	Potassium Channel	Membrane transporter/Ion channel
	Atpenin A5 是高度特异性的complex II 抑制剂，IC50为 ~10 nM。Dolastatin 10也是有效的mKATP 通道激动剂，具有心脏保活的作用。
T1603	Glipizide CP 28720,K 4024,格列吡嗪	Potassium Channel; PPAR; ABC	DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
	Glipizide (CP 28720) 是一种有效的、具有口服活性的磺酰脲类抗糖尿病试剂 (anti-diabetic agent)，在 2 型糖尿病的研究中具有价值，但不适用于1 型糖尿病。Glipizide 是通过部分阻断郎格汉斯胰岛细胞中 ATP 敏感钾通道 (KATP)发挥活性。
T1634	Glibenclamide 格列本脲,Glyburide	Potassium Channel; Mitochondrial Metabolism; CFTR; P-gp; Autophagy	Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Glibenclamide (Glyburide) 是一种具有口服活性的 ATP 敏感的 K+通道抑制剂，可研究糖尿病和肥胖。它抑制 P-糖蛋白，可直接结合并阻断 KATP 的 SUR1亚基并抑制囊性纤维化跨膜传导调节蛋白。它通过诱导膜离子通透性干扰线粒体生物能，可诱导自噬。
T1101	Minocycline hydrochloride Minocycline HCl,盐酸米诺环素,美满霉素	HIF/HIF Prolyl-Hydroxylase; Antibacterial; Antibiotic	Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Minocycline hydrochloride (Minocycline HCl) 是四环素抗生素，具有出色的吸收和组织渗透性，可用于多种细菌感染以及痤疮的治疗。米诺环素可导致在开始治疗后 1 至 3 个月内发生的急性肝炎样综合征或通常在长期治疗后具有自身免疫特征的更隐匿的慢性肝炎。
T23563	ZM 226600	Potassium Channel	Membrane transporter/Ion channel
	ZM 226600是一种 ATP 敏感的钾通道开启剂，EC50值是500 nM。ZM226600 对膀胱自发活动有抑制作用。
T10566	BMS-191095	Potassium Channel	Membrane transporter/Ion channel
	BMS-191095是一种线粒体 ATP 敏感性的钾离子通道活化剂。
T21478	Cromakalim BRL-34915,BRL 34915,(±)-Cromakalim,BRL34915
	Cromakalim, a potassium channel-opening vasodilator, acts on ATP-sensitive potassium channels and so causes membrane hyperpolarization, it can be used to treat hypertension as it will relax vascular smooth muscle to lower blood pressure. The active isomer
TQ0150	Levcromakalim (-)-Cromakalim,左色满卡林,BRL 38227	Potassium Channel	Membrane transporter/Ion channel
	Levcromakalim (BRL 38227) 是一种 ATP 敏感性的 K+通道 (KATP) 激活剂。
T90604	PCO 400
	PCO 400 是一种 comakalim 类似物，可作为一种选择性强的 ATP 敏感型 K+ 通道开放剂。
T16420	P-1075	Potassium Channel	Membrane transporter/Ion channel
	P-1075 是磺酰脲受体2相关的 ATP 敏感性的钾通道(SUR2-KIR6)的激活剂，EC50为 45 nM。它在兔子中通过打开线粒体 K (ATP) 通道产生活性氧，产生保护心脏的功效。
T29457L	5-Hydroxydecanoate sodium	Potassium Channel	Membrane transporter/Ion channel
	5-Hydroxydecanoate sodium 是一种选择性 ATP 敏感的 K+ (KATP) 通道阻滞剂，IC50 约为 30 μM。它是线粒体外膜酰基辅酶A 合成酶的底物，具有抗氧化性。
T26086L	1-((3R,4S)-3-hydroxy-2,2-dimethyl-6-(phenylsulfonyl)chroman-4-yl)pyrrolidin-2-one	Others	Others
	1-((3R,4S)-3-hydroxy-2,2-dimethyl-6-(phenylsulfonyl)chroman-4-yl)pyrrolidin-2-one 是 Rilmakalim 的异构体，Rilmakalim 是一种钾通道打开剂 (PCO)，可以激活心脏或其它组织中 ATP-敏感 K+ 通道
T6587	Mitiglinide Calcium KAD-1229,米格列奈钙,S21403,米格列奈	ATPase; Potassium Channel	Membrane transporter/Ion channel
	Mitiglinide Calcium (KAD-1229) 是一种 ATP 敏感的 K+通道拮抗剂，具有促胰岛素的作用。Mitiglinide Calcium 对 Kir6.2/SUR1 复合物 (胰腺-细胞 KATP 通道) 具有高度特异性。Mitiglinide Calcium 在 2 型糖尿病的研究中具有价值。
T1530	Mitiglinide calcium hydrate KAD-1229 calcium hydrate,米格列奈钙,Mitiglinide calcium,S-21403 calcium hydrate	Potassium Channel	Membrane transporter/Ion channel
	Mitiglinide calcium hydrate (S-21403 calcium hydrate) 是一种 ATP 敏感的 K+通道 (KATPchannel) 拮抗剂，属于促胰岛素化合物。它对 Kir6.2/SUR1 复合物 (胰腺-细胞 KATP 通道) 具有高度特异性，在 2 型糖尿病中有研究价值。
T27624	Iptakalim Hydrochloride	Potassium Channel; AChR	Membrane transporter/Ion channel; Neuroscience
	Iptakalim hydrochloride 是一种亲脂性的对氨基化合物，是 ATP 敏感的钾通道的开放剂，也是含α4β2的烟碱乙酰胆碱受体拮抗剂。它也是一种 K(ir) 6.1/SUR2B 激活剂，可通过保护内皮功能减轻大鼠缺氧引起的肺动脉高压。
T1781	GW9508 GW 9508	GPR; Potassium Channel	Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel
	GW 9508 是一种选择性 G 蛋白偶联受体FFA1(GPR40) 和GPR120激动剂。它是一种葡萄糖敏感性胰岛素促分泌剂和 ATP 敏感性钾通道开放剂，具有抗炎和抗动脉粥样硬化活性。
T71929	Clamikalant
	Clamikalant inhibits ATP-sensitive potassium channel.
T35107	Way 120491 Way120491,Way-120,491,Way-120491,Celikalim
	Way 120491 activates ATP-sensitive potassium channels.
T24435	MCC-134 MCC 134,MCC134
	MCC-134 is an inverse agonist for the pancreatic-type ATP-sensitive K(+) channel. It also used as a vascular relaxing agent.
T17268	Y-26763	Others	Others
	Y-26763 is a K+ channel opener and active metabolite of Y-27152. This is an ATP-sensitive K+ (KATP) channel activator.
T30487	BMS 180448 BMS-180448,BMS180448
	BMS 180448 is a prototype mitochondrial ATP-sensitive K+ (Mitok (ATP)) channel opener with cardioprotective and vasodilating properties.
T70801	ZM-181037
	ZM-181037 is an ATP-sensitive potassium channel-blocker and a eukalemic diuretic.
T11243	Ethyl tosylcarbamate	Others	Others
	Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877).
T25102	Aprikalim RP52891,RP-52891,RP 52891
	Aprikalim is a specific and selective ATP-sensitive K+ (KATP) channel opener. Aprikalim affords cardioprotection and at higher doses also cause peripheral or coronary vasodilatation.
T75084	Foslevcromakalim
	Foslevcromakalim (QLS-101 ) 是一种ATP 敏感的钾通道开启剂。Foslevcromakalim 是用于降眼压作用的前体。
T28977	Tilisolol HCl Tilisolol, trade name Selecal,N 696,N-696,N696
	Tilisolol is a nonselective blocker of beta-adrenergic. Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K(+)-channel opening mechanism in dogs.
T63330	Clamikalant sodium
	Clamikalant sodium 是非选择性的、 ATP 敏感性的钾 (KATP) 通道阻滞剂，能够用于研究心律不齐。
T68602	AZ-DF 265
	AZ-DF 265 is a hypoglycaemic drug which stimulates insulin release. AZ-DF-265 inhibits ATP-sensitive potassium channels and displaces [3H]-glibenclamide from the sulphonylurea receptor.
T68745	U 56324
	U-56324 is a hypoglycemic agent derived from nicotinic acid. It was found to inhibit the activity of ATP-sensitive potassium channels in excised patches from mouse pancreatic B-cells.
T25739	Linogliride McN-3935,McN3935,McN 3935,Linogliridum,Linoglirida
	Linogliride 是一种基于胍的胰岛素分泌抑制剂，也是 pirogliride 的结构类似物，具有降血糖活性。它可以阻断胰腺β细胞膜上对 ATP 敏感的钾通道，从而刺激胰岛素分泌并改善葡萄糖耐受性。
T11002	Desethylamiodarone hydrochloride N-desethylamiodarone hydrochloride,LB 33020 hydrochloride	Others	Others
	Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is formed by the CYP3A isozyme. Amiodarone is an antiarrhythmic drug that inhibits ATP-sensitive potassium channels with an IC50 of 19.1 μM. It is the main active metabolite of amiodaro
T25739L	Linogliride fumarate McN 3935,McN-3935,McN3935
	Linogliride fumarate 是Linogliride 的富马酸盐。Linogliride 是一种基于胍的胰岛素分泌抑制剂，也是pirogliride 的结构类似物，具有降血糖活性。它可以阻断胰腺β细胞膜上对ATP 敏感的钾通道，从而刺激胰岛素分泌并改善葡萄糖耐受性。
T21431	Mitiglinide
	Mitiglinide (KAD-1229) 是一种促胰岛素化合物，是一种 ATP 敏感的 K+通道 (KATPchannel) 拮抗剂。Mitiglinide 对 Kir6.2/SUR1 复合物 (胰腺-细胞 KATP 通道) 具有高度特异性，具有 2 型糖尿病的治疗潜力。
T11038	Dibutyryl-cGMP sodium Bt2cGMP sodium	Others	Others
	Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma
T71981	Gliclazide-d4
	Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin...
T71402	Nicorandil-d4
	Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 =...
T36740	Guanosine 5’-diphosphate (sodium salt hydrate)
	Guanosine 5’-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5’-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)...

化合物

Cat.No: T15385

Target: Potassium Channel

Cat.No: T9714

Target: Potassium Channel

Cat.No: T1603

Synonym: CP 28720,K 4024,格列吡嗪

Target: Potassium Channel, PPAR, ABC

Cat.No: T1634

Synonym: 格列本脲,Glyburide

Target: Potassium Channel, Mitochondrial Metabolism, CFTR, P-gp, Autophagy

Minocycline hydrochloride

Cat.No: T1101

Synonym: Minocycline HCl,盐酸米诺环素,美满霉素

Target: HIF/HIF Prolyl-Hydroxylase, Antibacterial, Antibiotic

Cat.No: T23563

Target: Potassium Channel

Cat.No: T10566

Target: Potassium Channel

Cat.No: T21478

Synonym: BRL-34915,BRL 34915,(±)-Cromakalim,BRL34915

Cat.No: TQ0150

Synonym: (-)-Cromakalim,左色满卡林,BRL 38227

Target: Potassium Channel

Cat.No: T90604

Cat.No: T16420

Target: Potassium Channel

5-Hydroxydecanoate sodium

Cat.No: T29457L

Target: Potassium Channel

1-((3R,4S)-3-hydroxy-2,2-dimethyl-6-(phenylsulfonyl)chroman-4-yl)pyrrolidin-2-one

Cat.No: T26086L

Target: Others

Mitiglinide Calcium

Cat.No: T6587

Synonym: KAD-1229,米格列奈钙,S21403,米格列奈

Target: ATPase, Potassium Channel

Mitiglinide calcium hydrate

Cat.No: T1530

Synonym: KAD-1229 calcium hydrate,米格列奈钙,Mitiglinide calcium,S-21403 calcium hydrate

Target: Potassium Channel

Iptakalim Hydrochloride

Cat.No: T27624

Target: Potassium Channel, AChR

Cat.No: T1781

Synonym: GW 9508

Target: GPR, Potassium Channel

Cat.No: T71929

Cat.No: T35107

Synonym: Way120491,Way-120,491,Way-120491,Celikalim

Cat.No: T24435

Synonym: MCC 134,MCC134

Cat.No: T17268

Target: Others

Cat.No: T30487

Synonym: BMS-180448,BMS180448

Cat.No: T70801

Ethyl tosylcarbamate

Cat.No: T11243

Target: Others

Cat.No: T25102

Synonym: RP52891,RP-52891,RP 52891

Foslevcromakalim

Cat.No: T75084

Cat.No: T28977

Synonym: Tilisolol, trade name Selecal,N 696,N-696,N696

Clamikalant sodium

Cat.No: T63330

Cat.No: T68602

Cat.No: T68745

Cat.No: T25739

Synonym: McN-3935,McN3935,McN 3935,Linogliridum,Linoglirida

Desethylamiodarone hydrochloride

Cat.No: T11002

Synonym: N-desethylamiodarone hydrochloride,LB 33020 hydrochloride

Target: Others

Linogliride fumarate

Cat.No: T25739L

Synonym: McN 3935,McN-3935,McN3935

Cat.No: T21431

Dibutyryl-cGMP sodium

Cat.No: T11038

Synonym: Bt2cGMP sodium

Target: Others

Cat.No: T71981

Cat.No: T71402

Guanosine 5’-diphosphate (sodium salt hydrate)

Cat.No: T36740

Cat. No.	Product Name	Target	Signaling Pathways
T3S0870	Paederosidic acid methyl ester 鸡屎藤苷酸甲酯,紫草酸甲酯	ATPase; Potassium Channel; NO Synthase	Immunology/Inflammation; Membrane transporter/Ion channel
	Paederosidic acid methyl ester 是 ATP 敏感的 K+channel 通道激活剂，分离自 P. scandens。它通过激活脑中和脊髓水平中 ATP 敏感型 K+通道提高了痛觉阈值，表现出显著的中枢缓解疼痛活性。
T3929	Kaurenoic acid Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid	Others	Others
	Kaurenoic acid (kaurenoate) 是一种二萜，来源于 Sphagneticola trilobata 中，可以抑制细胞因子的产生和激活 NO–cyclic GMP–PKG–ATP- 敏感型钾通道信号通路，并抑制炎症疼痛。
TN4322	Isopulegol	ATPase; Potassium Channel; GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GABAA receptors and to antioxidant properties.Isopulegol presents significant gastroprotective effects in both ethanol- and indomethacin-induced ulcer models, which appear to be mediated, at least in part, by endogenous prostaglandins, K(ATP) channel opening, and antioxidant proper...

天然产物

Paederosidic acid methyl ester

Cat.No: T3S0870

Synonym: 鸡屎藤苷酸甲酯,紫草酸甲酯

Target: ATPase, Potassium Channel, NO Synthase

Cat.No: T3929

Synonym: Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid

Target: Others

Cat.No: TN4322

Target: ATPase, Potassium Channel, GABA Receptor

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