Cerivastatin-d3 sodium

CAS: 916314-45-9 F: C26H30D3FNNaO5 W: 484.55

Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-l

Contact QiTai

This product is for research use only, not for human use. We do not sell to patients.

Bioactivity	Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect[1][2].
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]。Cerivastatin sodium (5-50 ng/mL；3 天；MDA-MB-231 细胞) 处理诱导 MDA-MB-231 细胞增殖的剂量依赖性降低 (在 25 ng/mL 时抑制高达 40%)[2]。Cerivastatin sodium (25 ng/mL；18-36 小时；MDA-MB-231 细胞) 处理 36 小时后诱导细胞周期停滞在 G 1/S 期.较短的孵育时间 (18 小时) 未观察到这种停滞[2]。Cerivastatin sodium (25 ng/mL；18 小时；MDA-MB-231 细胞) 处理诱导显著的 p21Waf1/Cip1 水平增加[2]。Cerivastatin sodium (25 ng/mL；12 小时；MDA-MB-231 细胞) 处理增加MDA-MB-231 细胞中的 p21 转录本[2]。Cerivastatin sodium (10-25 ng/mL；18 小时) 通过 Matrigel 抑制 MDA-MB-231 细胞的侵袭[2]。Cerivastatin sodium (25 ng/mL；18-36 小时) 使 RhoA 和 Ras 从细胞膜离域到胞质溶胶并诱导形态学变化[2]。Cerivastatin sodium (25 ng/mL；4-36 小时) 以 RhoA 抑制依赖性方式诱导 NFκB 失活，导致尿激酶和金属蛋白酶 9 表达降低，同时增加 IκB[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Cerivastatin-d3 sodium 相关抗体:
In Vivo	Cerivastatin sodium 吸收良好，在口服给药后 1-3 小时内达到最大血浆浓度。在循环中，Cerivastatin sodium 与血浆蛋白高度结合 (99.5%)，消除半衰期为 2-4 小时。Cerivastatin sodium 主要在肝脏中代谢为三种极性代谢物。其中两种代谢物具有活性，但与母体药物相比程度较小，第三种代谢物无活性。所有代谢物的血浆浓度都大大低于母体药物的血浆浓度。代谢物通过尿液 (20-25%) 和粪便 (66-73%) 消除，而基本上没有母体化合物排出[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	916314-45-9
Formula	C26H30D3FNNaO5
Molar Mass	484.55
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]. Denoyelle C, et al. Cerivastatin, an inhibitor of HMG-CoA reductase, inhibits the signaling pathways involved in the invasiveness and metastatic properties of highly invasive breast cancer cell lines: an in vitro study. Carcinogenesis. 2001 Aug;22(8):1139-48. [3]. Stein E, et al. Cerivastatin, a New Potent Synthetic HMG Co-A Reductase Inhibitor: Effect of 0.2 mg Daily in Subjects With Primary Hypercholesterolemia. J Cardiovasc Pharmacol Ther. 1997 Jan;2(1):7-16. [4]. Furberg CD, et al. Withdrawal of cerivastatin from the world market. Curr Control Trials Cardiovasc Med. 2001;2(5):205-207.

Beclomethasone 17-Propionate-d5