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18

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T10979	DCPIB	Potassium Channel; Chloride channel	Membrane transporter/Ion channel
	DCPIB 是选择性可逆体积调节性阴离子通道抑制剂，抑制肿胀激活氯电流，在 CPAE 细胞中，IC50值为 4.1 μM。它能够电压依赖性激活钾离子通道 TREK1 和 TRAAK，抑制 TRESK、TASK1 和 TASK3的 IC50值分别为 0.14、0.95 和 50.72 μM。
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。
T8851	I3MT-3 HMPSNE	Hippo pathway	Stem Cells
	I3MT-3 (HMPSNE) 是一种有效的、具有细胞膜渗透性的、选择性的 3-巯基丙酮酸硫转移酶 (3MST)的抑制剂，IC50值为2.7 μM，对其他硫化氢/磺胺制硫酶没有活性。它靶向位于 3MST 活性位点的过硫半胱氨酸残基。
T19840	GSK-F1 PI4KA inhibitor-F1	PI4K	PI3K/Akt/mTOR signaling
	GSK-F1 (PI4KA inhibitor-F1) 是一种新型强效 PI4KA 抑制剂。
T0386L	Ropivacaine LEA-103 HCl,罗哌卡因	Potassium Channel; Sodium Channel	Membrane transporter/Ion channel
	Ropivacaine (LEA-103 HCl) 是有效的钠通道阻断剂，通过可逆地抑制钠离子内流从而引起神经纤维脉冲传导阻滞。Ropivacaine 也是一种 K2P(双孔钾通道)TREK-1的抑制剂，在 COS-7 细胞膜上的 IC50值为 402.7 μM。Ropivacaine 可以用于神经性疼痛的缓解的相关研究。
T67951	JB061	Myosin	Cytoskeletal Signaling
	JB061是一种非肌肉肌球蛋白II抑制剂，针对心肌肌球蛋白、骨骼肌肌球蛋白和平滑肌肌球蛋白II的IC50分别为4.4 μM、9.1 μM和>100 μM。其对ATP酶活性的抑制作用较弱（IC50>200 μM）。此外，JB061对COS-7细胞显示出细胞毒性，IC50值为39 μM。
T6645	Ropivacaine hydrochloride monohydrate Ropivacaine HCl,Ropivacaine HCl monohydrate,LEA 103,盐酸罗哌卡因,盐酸罗哌卡因一水合物,LEA-103 HCl	Potassium Channel; Sodium Channel	Membrane transporter/Ion channel
	Ropivacaine hydrochloride monohydrate (LEA-103 HCl) 是钠通道阻断剂，通过可逆地抑制钠离子内流从而引起神经纤维脉冲传导阻滞。Ropivacaine HCl monohydrate 也是 K2P(双孔钾通道)TREK-1的抑制剂。在动物实验模型中，Ropivacaine HCl monohydrate 可用于神经性疼痛的缓解。
TP2021	[Pro3]-GIP (Rat)
	High affinity rat GIP receptor partial agonist (Kd = 13 nM). Increases cAMP accumulation in COS-7 cells transfected with rat GIP receptor, while also acting as a competitive antagonist of GIP.
T61475	Ropivacaine mesylate
	Ropivacaine mesylate 是一种高效的钠通道 (sodium channel) 阻断剂，通过可逆性抑制钠离子内流 (sodium ion influx)，引致神经纤维脉冲传导阻滞。此外，Ropivacaine 还能抑制 K2P(双孔钾通道)TREK-1，其在 COS-7 细胞膜上的 IC50 值为 402.7 μM。
T38220	11-cis Retinol
	11-cisRetinol is an isomer of vitamin A . It is formed from vitamin A,viaatrans-retinyl ester intermediate, by the enzyme RPE65 in the retinal pigment epithelium and then converted to 11-cis retinal as part of the visual cycle.1,211-cisRetinol is an agonist of salamander and human red rod opsins expressed in COS cells and an inverse agonist of salamander red cone opsin, as well as human red and green cone opsins expressed in COS cells.3It promotes pigment formation in cone, but not rod, photorec...
T37092	20-HEPE
	20-HEPE is a metabolite of eicosapentaenoic acid that is formed via ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. It activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter when used at a concentration of 10 μM. 20-HEPE also activates murine transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks antinociceptive activity in rats.
T28235	OMDM169 OMDM 169,OMDM-169
	OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microM<IC(50)<0.41 microM towards 2-AG hydrolysing activities in
T83733	TIP39 (human, bovine) TFA Tuberoinfundibular Peptide of 39 Residues
	TIP39作为一种神经肽及甲状旁腺激素受体2型(PTH2R)激动剂，在表达重组人或大鼠PTH2R的COS-7细胞中诱导cAMP积累（EC50分别为0.5和0.8 nM），以及在内源性表达PTH2R的F-11细胞中（EC50 = 1.15 nM）。在CFK2大鼠软骨细胞中，TIP39 (1 nM)诱导细胞周期在G0/G1阶段停滞，并减少软骨分化的主要调控因子Sox9的表达。此外，TIP39 (100 pmol/动物)在小鼠强迫游泳测试中减少了不动时间。
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T36232	20-carboxy Arachidonic Acid
	20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-A...
T36555	Tyr-α-CGRP (human) (trifluoroacetate salt)
	Tyr-α-CGRP is an N-terminal extended tyrosinated analogue of α-calcitonin gene-related peptide . It binds to amylin receptors AMY1 and AMY3 in COS-7 cells expressing the human receptors (IC50s = 141 and 1.86 nM, respectively). Tyr-α-CGRP also binds to and stimulates cAMP accumulation in rat L6 myocytes (IC50 = 4 nM; EC50 = 12 nM). It also binds to rat brain and spleen membrane preparations (IC50s = 0.2 and 0.5 nM, respectively), induces positive chronotropic and inotropic effects in isolated rig...
T37413	Calcitonin (salmon) (trifluoroacetate salt)
	Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and ...
T36639	Donecopride (fumarate hydrate)
	Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value...

化合物

Cat.No: T10979

Target: Potassium Channel, Chloride channel

Cat.No: T16420

Target: Potassium Channel

Cat.No: T8851

Synonym: HMPSNE

Target: Hippo pathway

Cat.No: T19840

Synonym: PI4KA inhibitor-F1

Target: PI4K

Cat.No: T0386L

Synonym: LEA-103 HCl,罗哌卡因

Target: Potassium Channel, Sodium Channel

Cat.No: T67951

Target: Myosin

Ropivacaine hydrochloride monohydrate

Cat.No: T6645

Synonym: Ropivacaine HCl,Ropivacaine HCl monohydrate,LEA 103,盐酸罗哌卡因,盐酸罗哌卡因一水合物,LEA-103 HCl

Target: Potassium Channel, Sodium Channel

[Pro3]-GIP (Rat)

Cat.No: TP2021

Ropivacaine mesylate

Cat.No: T61475

Cat.No: T38220

Cat.No: T37092

Cat.No: T28235

Synonym: OMDM 169,OMDM-169

TIP39 (human, bovine) TFA

Cat.No: T83733

Synonym: Tuberoinfundibular Peptide of 39 Residues

Reduced Haloperidol

Cat.No: T37167

20-carboxy Arachidonic Acid

Cat.No: T36232

Tyr-α-CGRP (human) (trifluoroacetate salt)

Cat.No: T36555

Calcitonin (salmon) (trifluoroacetate salt)

Cat.No: T37413

Donecopride (fumarate hydrate)

Cat.No: T36639

Cat. No.	Product Name	Target	Signaling Pathways
T37526	2-Oleoylglycerol 2-Oleoyl Glycerol,2-OG,2-Monoolein	GPR	Endocrinology/Hormones; GPCR/G Protein
	2-Oleoylglycerol 是一种存在于棕榈仁、葵花籽和米糠中的脂质。2-Oleoylglycerol 可当作一种 GPR119 激动剂，具有神经保护作用，可诱导胰高血糖素样肽 1 (GLP-1) 分泌。2-Oleoylglycerol 可用于非酒精性脂肪性肝炎造模。

天然产物

2-Oleoylglycerol

Cat.No: T37526

Synonym: 2-Oleoyl Glycerol,2-OG,2-Monoolein

Target: GPR

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