| MK3102Novel long-acting DPP-4 inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.16%
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| Cas No. | 1226781-44-7 | SDF | Download SDF |
| Chemical Name | (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine | ||
| Canonical SMILES | CS(N1C=C2CN([C@](CO3)([H])C[C@@](N)([H])[C@@]3([H])C4=C(F)C=CC(F)=C4)CC2=N1)(=O)=O | ||
| Formula | C17H20F2N4O3S | M.Wt | 398.43 |
| Solubility | ≥17.15mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Dipeptidyl peptidase IV (DPP-4) inhibitors improve glycemic control in patients with type 2 diabetes by prolonging the half-life of incretin peptides, which stimulate insulin secretion and decrease glucagon release in a glucose-dependent manner. MK-3102 is a novel long-acting DPP-4 inhibitor.
In vitro: MK-3102 is a competitive, reversible inhibitor of DPP-4 and is more potent than sitagliptin. It is highly selective over all proteases tested, including QPP, FAP, PEP, DPP8, and DPP9. The compound has weak ion channel activity [1].
In vivo: MK-3102 was evaluated for its ability to improve glucose tolerance in lean mice. When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test, it significantly reduced blood glucose excursion in a dosedependent manner from 0.01 mg/kg to 0.3 mg/kg [1].
Clinical trial: MK-3102 is currently in phase 3 clinical trial for type 2 diabetes mellitus. Dose-dependent efficacy in 2 h post meal glucose reduction, fasting plasma glucose reduction, and HbA1c and safety profile similar to that seen with once daily DPP-4 inhibitor such as sitagliptin was observed in a 12-week phase IIB dose-rangefinding study [1].
Reference:[1] Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12.
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（第1张图和第2张图是经旋转后方向恰好相反的两张图，上矢状窦等静脉也显示了）
女患，70岁，大专毕业，我院退休药师。7-8年前患脑梗（具体不详）。记忆力差5-6年，近记忆为著，几次做饭后忘记关火，将炉具的台板（玻璃的）烧裂。近5-6年来，病人每年住院彻底检查治疗1次（主要是使用活血化瘀及营养脑细胞药）。平素，病人双耳听力略差，睡眠欠佳、便秘、尿频，偶从卧位坐起时视蒙。既往有时血压略高，未降压治疗。本次为“通血管”再来住院。查体：血压：140/80mmHg,双耳听力略差，近记忆力差，但智力（MMSE：26分)正常，颅神经未见异常，四肢肌力、感觉未见异常，植物神经未查，双掌颌反射（+），双下肢病理反射均阴性。血常规：淋巴细胞比率略高，余均正常；尿常规、心电图、癌胚抗原均正常；凝血四项：除凝血酶时间略长外均正常；生化全项：除总胆固醇略高外均正常；超声心动图：老年瓣退行性改变，左室舒张功能减退，房膜瘤可能。彩超：双侧颈动脉粥样硬化形成。头MRA:右大脑中动脉及其分支未显示。
问题：1MRI怎么会这样逍遥？病人无肢体瘫，生活自理如常人。
2为明确头MRA:右大脑中动脉及其分支未显示的病因和程度，除做DSA外，还需做什么？
3如不做DSA，给他订类药、阿斯匹林及活血化瘀的中药可不可以？
教。
版主laocao留言:
患者的年龄，病史，症状，辅助检查传上来，便于进一步讨论，谢谢！
