Cat. No. | Product Name | Target | Signaling Pathways |
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TP1889 |
MCL0020
MCL 0020 |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
MCL0020 是一种有效的选择性黑素皮质素MC4受体拮抗剂,IC50为 11.63 nM。它剂量依赖性减轻束缚应激诱发的厌食症,在体内表现出抗焦虑样活性。 | |||
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。 | |||
T10789 |
Chitosan oligosaccharide
COS,壳聚糖低聚乳酸酯 |
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
Chitosan oligosaccharide (COS) 是 β-(1→4)-连接的 D-氨基葡萄糖的寡聚体,Chitosan oligosaccharide可激活 AMPK ,抑制NF-κB 和 MAPK在内的炎症信号通路。 | |||
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。 | |||
T38220 |
11-cis Retinol
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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... | |||
T11055 |
DL-TBOA
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transporter | Metabolism |
DL-TBOA inhibited [14C] glutamate uptake in COS-1 cells expressing human EAAT1 and EAAT2, with Ki values of 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner, with Ki values of 4.4 μM and 3.2 μM, respectively. DL-TBOA | |||
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。 | |||
T39510 | DL-TBOA ammonium | ||
DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EA... | |||
T37092 |
20-HEPE
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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. | |||
T36130 |
22(S)-hydroxy Cholesterol
22(S)-hydroxy Cholesterol,22β-hydroxy Cholesterol |
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22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22... | |||
T28235 |
OMDM169
OMDM 169,OMDM-169 |
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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 |
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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
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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 ... | |||
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... | |||
T35854 |
9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)
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9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-co... | |||
T38193 |
β-Endorphin (1-27) (human) (trifluoroacetate salt)
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β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in ... |