Remogliflozin etabonate
(Synonyms: GSK189075) 目录号 : GC44811
A prodrug form of remogliflozin A
Cas No.:442201-24-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Remogliflozin etabonate is a prodrug form of the sodium-glucose transporter 2 (SGLT2) inhibitor remogliflozin A . Remogliflozin etabonate inhibits human SGLT2 and SGLT1 (Kis = 1.95 and 43.1 μM, respectively). It inhibits increases in plasma glucose levels in a glucose tolerance test in a rat model of diabetes induced by streptozotocin when administered at doses of 3 and 10 mg/ml. Remogliflozin etabonate (10 and 30 mg/kg twice per day for 6 weeks) also increases fasting plasma insulin levels and reduces fasting plasma glucose and triglyceride levels, as well as urinary glucose excretion, in a db/db mouse model of diabetes with hyperinsulinemia and obesity.
| Cas No. | 442201-24-3 | SDF | |
| 别名 | GSK189075 | ||
| Canonical SMILES | CC(C)OC1=CC=C(CC2=C(C)N(C(C)C)N=C2O[C@@H]3O[C@H](COC(OCC)=O)[C@@H](O)[C@H](O)[C@H]3O)C=C1 | ||
| 分子式 | C26H38N2O9 | 分子量 | 522.6 |
| 溶解度 | DMSO: Soluble,Methanol: Soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9135 mL | 9.5675 mL | 19.1351 mL |
| 5 mM | 0.3827 mL | 1.9135 mL | 3.827 mL |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9135 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Remogliflozin etabonate: First Global Approval
Drugs 2019 Jul;79(10):1157-1161.PMID:31201711DOI:10.1007/s40265-019-01150-9.
Remogliflozin, a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor, which is to be administered as Remogliflozin etabonate (Remo™, Remozen™), the prodrug for remogliflozin, recently received its first approval as a treatment for type 2 diabetes mellitus (T2DM) in India. This article summarizes the milestones in the development of Remogliflozin etabonate leading to this first approval for T2DM.
Remogliflozin etabonate in the Treatment of Type 2 Diabetes: Design, Development, and Place in Therapy
Drug Des Devel Ther 2020 Jun 24;14:2487-2501.PMID:32612352DOI:10.2147/DDDT.S221093.
Type 2 diabetes mellitus (T2DM) is an emerging epidemic in Asian countries, especially in India. With the advent of the SGLT2 inhibitor class of drugs demonstrating benefits beyond glycemic control, viz. weight loss, blood pressure reduction, and cardiovascular and renal protection, the management of T2DM has taken a quantum leap. Remogliflozin etabonate (RE) is the latest addition to the SGLT2 inhibitor class of drugs that have been recently approved in India for the management of T2DM. RE is a potent and selective inhibitor of SGLT2 with the unique distinction of being administered as a prodrug, existence of active metabolites, and short half-life necessitating twice-daily dosing. The Phase III study of RE demonstrated it to be an efficacious and safe agent and non-inferior to the currently available SGLT2 inhibitors. This paper reviews not only the pharmacokinetics, pharmacodynamics, clinical efficacy, and safety profile of RE but also its molecular and clinical development program. This review has taken into consideration all available published as well as unpublished literature on RE and discusses the individual studies performed during its development for characterization of pharmacological profile.
Remogliflozin etabonate: a novel SGLT2 inhibitor for treatment of diabetes mellitus
Expert Opin Investig Drugs 2015;24(10):1381-7.PMID:26288025DOI:10.1517/13543784.2015.1061501.
Introduction: Inhibitors of sodium-glucose co-transporter type 2 (SGLT2) represent a new class of anti-hyperglycemic agents with a unique mechanism of action. These drugs lower blood glucose by increasing urinary glucose excretion. Remogliflozin etabonate (RE) is a prodrug of remogliflozin, an SGLT2 inhibitor under development. Areas covered: The following article reviews all of the clinical studies published regarding metabolism, drug interaction, safety and efficacy of RE in healthy subjects, patients with type 1 and type 2 diabetes. Expert opinion: Available data suggest low potential for RE to interact with other drugs affecting the P450 system. Compared with placebo, RE reduces hemoglobin A1c (HbA1c) levels by an average of 0.5 - 1.0% after 12 weeks of therapy in drug-naive patients with type 2 diabetes. Because of its relatively short half-life, RE may be slightly more effective when used twice daily than once daily. One preliminary study also showed that RE decreased plasma glucose levels in type 1 diabetes. Advantages of RE include modest weight loss of ∼ 2 kg, low risk of hypoglycemia, and a trend toward decrease in blood pressure. The commonest adverse effects of RE are genital mycotic infections, urinary tract infections, and dizziness. However, further studies are needed to establish its long-term safety and efficacy, and to determine whether it has specific advantages over currently approved SGLT2 inhibitors.
Review on Characteristics and Analytical Methods of Remogliflozin etabonate: An Update
Mini Rev Med Chem 2022;22(9):1341-1350.PMID:34620050DOI:10.2174/1389557521666211007115611.
Hyperglycemia and its associated disorders like Diabetes mellitus are engulfing the world's population at a faster pace. New-age medications like the SGLT 2 inhibitors have found their place in the run to combat DM. Drugs with these properties have proven to be effective in treating hyperglycemia, obesity, and major cardiac disorders. The interesting fact about these drugs is that they act independently of insulin levels in the patient's body. The fact that they even bypass the side effects shown by currently used anti-diabetic medications has attracted the world's hope to neutralize diabetes mellitus. The invention of Remogliflozin etabonate (RGE), an SGLT 2 inhibitor, has therefore added a silver lining to the gliflozin-family of drugs in the fight against DM. This is due to its least side effects as well as its effective mechanisms to treat hyperglycemia. It can be administered not only as a single entity but also can be co-administered in combination with other anti-hyperglycemic agents. RGE is already sold in the Indian market as REMO-ZEN, by Glenmark Pharmaceuticals. It has been studied thoroughly for its pharmacokinetic and pharmacodynamic profile. It is a benzylpyrazole glucoside. Various analytical methods have been formulated for its detection, quantification, and routine quality control activities. RGE can be studied with the help of UV-visible spectrophotometry, High-Performance Liquid Chromatography (HPLC) and Hyphenated techniques like Liquid Chromatography- Mass Spectroscopy (LC-MS/MS). This review briefs about the overall chemical, pharmacological, pharmacokinetic and pharmacodynamics properties of RGE. It mainly discusses various analytical techniques used for determining and estimating RGE.
Discovery of Remogliflozin etabonate: A potent and highly selective SGLT2 inhibitor
Bioorg Med Chem 2021 Mar 15;34:116033.PMID:33581390DOI:10.1016/j.bmc.2021.116033.
We optimized the structure of an active metabolite (1) of WAY-123783, which was obtained from mouse urine after oral administration, to improve selectivity for SGLT2 and oral bioavailability. O-glucoside derivative 24 (Remogliflozin etabonate) was subsequently identified as a potent, highly selective, and orally available SGLT2 inhibitor.