Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T26324 |
VU0071063
VU 0071063,VU-0071063 |
Potassium Channel | Membrane transporter/Ion channel |
VU0071063 是特异的Kir6.2/SUR1开启剂 (EC50=7.44 μM),可用于研究Kir6.2 /SUR1在大脑和胰腺中的表达。它可以诱导 β 细胞膜电位的超极化从而抑制胰岛素的分泌。 | |||
T0816 |
Acetohexamide
Acetohexamid,醋磺环已脲,Dymelor,醋磺己脲,Gamadiabet |
Potassium Channel; NADPH | Membrane transporter/Ion channel; Metabolism |
Acetohexamide (Acetohexamid) 是磺脲类试剂,可刺激胰腺分泌胰岛素,能够用于 2 型糖尿病的相关研究。 | |||
T16110 |
ML418
|
Potassium Channel | Membrane transporter/Ion channel |
ML418 是可透过血脑屏障的钾离子通道Kir7.1选择性阻滞剂,IC50值为 310 nM。它有效抑制Kir6.2/SUR1,对 Kir7 的选择性高于其他 Kir 通道。 | |||
T0371 |
Gliquidone
AR-DF 26,格列喹酮,Glurenorm |
Potassium Channel | Membrane transporter/Ion channel |
Gliquidone (AR-DF 26) 是一种磺酰脲类的抗糖尿病药物,可用于2型糖尿病的研究。 | |||
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。 | |||
T0127 |
Glimepiride
Glimperide,HOE-490,格列美脲 |
Potassium Channel | Membrane transporter/Ion channel |
Glimepiride (HOE-490) 是一种中长效的磺酰脲类抗糖尿病化合物,其 ED50=182 μg/k。 | |||
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。 | |||
T35635 |
rac-trans-4-hydroxy Glyburide
|
||
rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide .1,2It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50values of 0.95 and 100 nM, respectively.2 1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes ... | |||
T17240 | VU041 | Others | Others |
VU041 is an inhibitor of Anopheles gambiae and Aedes aegypti inward rectifier potassium 1 channels (IC50: 2.5 μM and 1.7 μM, respectively). VU041 inhibits appreciably is mammalian Kir2.1 (IC50: 12.7 μM) and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. | |||
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. | |||
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]。 |