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Cat. No. | Product Name | Target | Signaling Pathways |
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T0334 |
Rosiglitazone
BRL49653,罗格列酮 |
Ferroptosis; TRP/TRPV Channel; PPAR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism |
Rosiglitazone (BRL49653) 是一种 PPARγ 激动剂、TRPC5 激活剂和 TRPM3 抑制剂,具有口服活性。Rosiglitazone 也是一种降糖剂,是噻唑烷二酮类胰岛素增敏剂。 | |||
T6646 |
Rosiglitazone hydrochloride
盐酸罗格列酮,BRL-49653 HCl,Rosiglitazone HCl |
Ferroptosis; TRP/TRPV Channel; PPAR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism |
Rosiglitazone hydrochloride (BRL-49653 HCl) 是一种降血糖药物,通过与脂肪细胞中的 PPAR 受体结合来刺激胰岛素分泌。它对 PPARγ1、PPARγ2 和 PPARγ 的EC50值分别为 30 nM、100 nM 和 60 nM。它也是TRPC5的激活剂和TRPM3的抑制剂。 | |||
T1622 |
Rosiglitazone maleate
BRL 49653C,BRL 49653,马来酸罗格列酮 |
Ferroptosis; TRP/TRPV Channel; PPAR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism |
Rosiglitazone maleate (BRL 49653) 是一种选择性PPARγ激活剂,具有抗糖尿病特性和潜在抗肿瘤活性。它也是TRP 通道调节剂,可抑制 TRPM2、TRPM3 的活性,激活 TRPC5。 | |||
T35717 |
N-desmethyl Rosiglitazone
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N-desmethyl Rosiglitazone is a major metabolite of rosiglitazone , a potent and selective PPARγ ligand present in formulations that have been used to treat type 2 diabetes. Rosiglitazone is metabolized by the cytochrome P450 (CYP) isoform CYP2C8 to form N-desmethyl rosiglitazone. | |||
T61848 |
Rosiglitazone potassium
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Rosiglitazone (BRL 49653) potassium is a potent and selective PPARγ agonist (EC 50: 60 nM, Kd: 40 nM), administered orally. It also serves as an activator of TRPC5 (EC 50: 30 μM) and an inhibitor of TRPM3. This compound, widely used in research, has shown promise in investigating obesity, diabetes, senescence, and ovarian cancer [1] [2] [4] [7]. | |||
T36180 |
Azelaoyl PAF
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Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which promote the differentiation of monocytes via the nuclear receptor PPARγ. One of these substances was recently isolated and purified from oxLDL, and identified as azelaoyl PAF. Azelaoyl PAF is a potent PPARγ agonist which competes for the thiazolidinedione binding site. Azelaoyl PAF is more potent than 15-deoxy-δ12,14-prostaglandin J2, and equipotent with rosiglitazone as a ligand for this receptor. | |||
T61976 |
DS-6930
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DS-6930 是一种有效的和选择性的 PPARγ激动剂(EC50= 41 nM)。DS-6930 可有效降低血浆葡萄糖 (PG)水平,此外,与 Rosiglitazone 相比,具有更少的 PPARγ 相关不良反应。DS-6930 在糖尿病中具有研究价值。 | |||
T37829 |
CAY10573
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The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively. CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound ros... | |||
T36517 |
Resveratrol-3-O-sulfate sodium
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Resveratrol-3-O-sulfate is a metabolite of resveratrol . In U-937 cells stimulated with LPS, resveratrol-3-O-sulfate (1 μM) decreases the expression of IL-1α, IL-1β, and IL-6 by 61.2, 76.6, and 42.2%, respectively, and decreases the release of TNF-α and IL-6 to similar levels as resveratrol. It has antioxidant activity in a Trolox assay, dose-dependently decreases growth of Caco-2 colorectal adenocarcinoma cells when used at concentrations ranging from 10 to 100 μM, and induces apoptosis at conc... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T4S21320 |
ISOGINKGETIN
异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮 |
MMP; Others | Others; Proteases/Proteasome |
ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂,也是一种Pre-mRNA Splicing 抑制剂。 | |||
TN1210 |
2-Hydroxy-1-Methoxyaporphine
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P450 | Metabolism |
2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone. | |||
TN1462 |
Cajanin
2',4',5-三羟基-7-甲氧基异黄酮,木豆异黄酮 |
ERK; MEK; Akt | Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling |
Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol efflux and RCT, it can significantly improve basal glucose uptake in HepG2 cells, its improving effect is concentration dependent, it exhibits effects stronger than that of rosiglitazone, which has been used as an antidiabetic drug. |