| Bioactivity | Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7]. |
| Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[1]。Rosiglitazone (0.1-10 μM，72 h) 导致多能 C3H10T1/2 干细胞分化为脂肪细胞[2]。 Rosiglitazone (1 μM，24 h) 激活 PPARγ，后者与 NF-α1 启动子激活神经元中的基因转录[4]。 Rosiglitazone (1 μM，24 小时) 保护 Neuro2A 细胞和海马神经元免受氧化应激，并上调 BCL-2以 NF-α1 依赖性方式表达[4]。 Rosiglitazone (0.01-100 μM，15 分钟) 抑制 TRPM3，IC50 值为 9.5 和4.6 μM 分别抑制硝苯地平和 PregS 诱发的活性[5]。 Rosiglitazone (0.5-50 μM，7 天) 抑制卵巢癌细胞增殖[8]。 Rosiglitazone (5 μM，7 天) 抑制 Olaparib (HY-10162) 诱导的细胞衰老改变并促进 A2780 和 SKOV3 细胞凋亡[8]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Rosiglitazone-d4 相关抗体: |
| In Vivo | Rosiglitazone (口服给药，5 mg/kg，每日一次，连续 8 周) 降低糖尿病大鼠的血糖[6]。 Rosiglitazone (腹腔注射，3 mg/kg/天) 改善血糖香烟烟雾通过激活雄性 Wistar 大鼠 PPARγ 和 RXRα 抑制 M1 巨噬细胞极化引起的气道炎症[7]。 Rosiglitazone (腹腔注射，10 mg/kg，每 2 天一次) 在 A2780 和 SKOV3 小鼠皮下异种移植模型中抑制皮下卵巢癌的生长[8]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 1132641-21-4 |
| Formula | C18H15D4N3O3S |
| Molar Mass | 361.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6. [3]. Haoshen Feng, et al. Rosiglitazone ameliorated airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα. Int Immunopharmacol. 2021 Aug;97:107809. [4]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8. [5]. Zehua Wang, et al. Rosiglitazone ameliorates senescence and promotes apoptosis in ovarian cancer induced by olaparib. Cancer Chemother Pharmacol. 2020 Feb;85(2):273-284. [6]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. [7]. Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30. [8]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220. |
Rosiglitazone-d4
CAS: 1132641-21-4 F: C18H15D4N3O3S W: 361.45
Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective
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