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28

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T0075	Nicorandil SG-75,尼可地尔	Potassium Channel	Membrane transporter/Ion channel
	Nicorandil (SG-75) 是一种有效的钾通道激活剂，靶向血管核苷二磷酸依赖性 K+通道和心脏 ATP 敏感 K+通道 (KATP)。Nicorandil 是一种烟酰胺酯，具有血管舒张和心脏保护作用，并具有治疗心绞痛和缺血性心脏病的潜力。
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。
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。
T5391	Bepridil hydrochloride CERM 1978,盐酸苄普地尔	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Bepridil hydrochloride (CERM 1978) 是一种钙通道阻滞剂，还抑制 Na+/Ca2+ 交换(NCX)、钠通道和心脏肌膜 KATP 通道，具有抗心绞痛的作用。
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。
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。
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。
T0451	Minoxidil 米诺地尔,U10858	Potassium Channel; COX	Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
	Minoxidil (U10858) 是一种是 ATP 敏感的钾通道 (KATP) 开放剂，可作为有效的口服降压药和外周血管舒张药，促进血管扩张并促进头发的生长。Minoxidil 还是一种大豆脂氧合酶的有效抑制剂，IC50为 20 μM。
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。
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。
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。
T15667	KRN4884	Others	Others
	KRN 4884 is an opener of the K+ channel. KRN 4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM), in the presence of intracellular ATP (1 mM).
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.
T17269	Y-27152	Others	Others
	Y-27152 is a prodrug of the KATP (Kir6) channel opener Y-26763 and is a long-acting K+ channel opener.
T23169	PNU 37883 hydrochloride	Others	Others
	Kir6 (KATP) channel antagonist
T16267	Naminidil BMS 234303-01	Others	Others
	Naminidil is an opener of cyanoguanidine KATP.
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。
T13949	U89232	Others	Others
	U-89232 is an opener of the cardioselective KATP channel.
T31627	Englitazone sodium CP-72,467-2,D03996,CP-72467-2,Englitazone sodium (USAN)
	Englitazone sodium is an antidiabetic agent and a novel NSCA and KATP channel blocker.
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.
T17094	Tifenazoxide NN414	Others	Others
	Tifenazoxide is an effective and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has an anti-diabetic effect, can inhibit glucose-stimulated insulin release in vitro and in vivo.
T37733	AMP-PNP tetralithium
	Non-hydrolyzable AMP analog. Kir6 (KATP) channel blocker. Inhibits fast axonal transport and stabilizes the interaction of membranous organelles with microtubules. Brady (1985) A novel brain ATPase with properties expected for the fast axonal transport motor. Nature 317 73 PMID:2412134 \|Yount et al (1971) Adenylyl imidodiphosphate, an adenosine triphosphate analog containing a P-N-P linkage. Biochemistry 10 2484 PMID:4326768 \|Hehl and Neumcke (1994) KATP channels of mouse skeletal muscle: mechan...
T60428	Cibenzoline
	Cibenzoline 是一种抗心律失常药，通过直接影响成孔 Kir6.2 亚基而不是 SUR1 亚基来抑制 KATP 通道。 Cibenzoline 几乎不具有抗胆碱能活性。 Cibenzoline 显着降低与心肌收缩力下降密切相关的LVPG。 Cibenzoline 具有研究肥厚型梗阻性心肌病的潜力[1][2]。
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...
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。
T72460	Dimethyl L-glutamate Dimethyl glutamate
	Dimethyl L-glutamate (Dimethyl glutamate), 一种可透膜的谷氨酸类似物，可刺激葡萄糖诱导的胰岛素 (insulin) 释放。Dimethyl L-glutamate 抑制KATP 通道的活性。Dimethyl L-glutamate 抑制E. gracilis 生长并导致细胞异常分裂。Dimethyl L-glutamate 可用于糖尿病、葡萄糖转运、磷酸化和进一步代谢的研究。
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...

化合物

Iptakalim Hydrochloride

Cat.No: T27624

Target: Potassium Channel, AChR

Cat.No: T0075

Synonym: SG-75,尼可地尔

Target: Potassium Channel

Cat.No: T1781

Synonym: GW 9508

Target: GPR, Potassium Channel

5-Hydroxydecanoate sodium

Cat.No: T29457L

Target: Potassium Channel

Bepridil hydrochloride

Cat.No: T5391

Synonym: CERM 1978,盐酸苄普地尔

Target: Calcium Channel

Cat.No: T1603

Synonym: CP 28720,K 4024,格列吡嗪

Target: Potassium Channel, PPAR, ABC

Cat.No: T15385

Target: Potassium Channel

Cat.No: TQ0150

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

Target: Potassium Channel

Cat.No: T0451

Synonym: 米诺地尔,U10858

Target: Potassium Channel, COX

Mitiglinide Calcium

Cat.No: T6587

Synonym: KAD-1229,米格列奈钙,S21403,米格列奈

Target: ATPase, Potassium Channel

Cat.No: T1634

Synonym: 格列本脲,Glyburide

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

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

Cat.No: T15667

Target: Others

Cat.No: T17268

Target: Others

Cat.No: T17269

Target: Others

PNU 37883 hydrochloride

Cat.No: T23169

Target: Others

Cat.No: T16267

Synonym: BMS 234303-01

Target: Others

Clamikalant sodium

Cat.No: T63330

Cat.No: T13949

Target: Others

Englitazone sodium

Cat.No: T31627

Synonym: CP-72,467-2,D03996,CP-72467-2,Englitazone sodium (USAN)

Cat.No: T25102

Synonym: RP52891,RP-52891,RP 52891

Cat.No: T17094

Synonym: NN414

Target: Others

AMP-PNP tetralithium

Cat.No: T37733

Cat.No: T60428

Cat.No: T71981

Cat.No: T21431

Dimethyl L-glutamate

Cat.No: T72460

Synonym: Dimethyl glutamate

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat. No.	Product Name	Target	Signaling Pathways
T3427	Polydatin Piceid,虎杖苷,Polydotin Peceid	Apoptosis; Mitophagy; NF-κB; Autophagy	Apoptosis; Autophagy; NF-κB
	Polydatin (Piceid) 是从传统中药虎杖根中提取的一种天然产物，在多个实验模型中具有抗炎作用。它可抑制 G6PD，并诱导氧化和内质网应激。
T3876	Loureirin B 龙血素B,龙血素 B	PAI-1; ERK; Potassium Channel; JNK	MAPK; Membrane transporter/Ion channel; Metabolism
	Loureirin B 是从剑叶龙血树中分离到的一种黄酮，是 PAI-1抑制剂，IC50值为 26.10 μM。它抑制 KATP，以及 ERK 和 JNK 的磷酸化，具有抗糖尿病的功效。
TMA0805	Lupanine	ATPase; Potassium Channel; Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Lupanine has a weak sedative effect on the central nervous system, interaction with specific drugs used for treatment of the CNS and for analgesic activity. Lupanine improves glucose homeostasis by influencing KATP-channels of pancreatic beta cells.
T73764	L-Palmitoylcarnitine TFA
	L-Palmitoylcarnitine TFA 是一种长链酰基肉碱和脂肪酸代谢产物，在缺血期间积聚于肌膜并扰乱膜脂环境。L-Palmitoylcarnitine TFA 通过与Kir6.2的相互作用抑制KATP 通道活性，而不影响单通道电导。

天然产物

Cat.No: T3427

Synonym: Piceid,虎杖苷,Polydotin Peceid

Target: Apoptosis, Mitophagy, NF-κB, Autophagy

Cat.No: T3876

Synonym: 龙血素B,龙血素 B

Target: PAI-1, ERK, Potassium Channel, JNK

Cat.No: TMA0805

Target: ATPase, Potassium Channel, Calcium Channel

L-Palmitoylcarnitine TFA

Cat.No: T73764

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