Rosiglitazone-d₄  (Synonyms: 罗格列酮-d₄; BRL 49653-d₄)

Rosiglitazone-d₄ is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 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].

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.

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.

361.45

C₁₈H₁₅D₄N₃O₃S

1132641-21-4

122320-73-4

罗格列酮-d₄

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [6]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]