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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| D413676-5mg |
5mg |
现货 ![]() |
| |
| D413676-25mg |
25mg |
现货 ![]() |
|
| 别名 | 多扎格列汀 |
|---|---|
| 英文别名 | HY-109030 | AKOS030527745 | Sinogliatin | (2S)-2-[3-(2-chlorophenoxy)-5-oxo-2H-pyrrol-1-yl]-N-[1-[(2R)-2,3-dihydroxypropyl]pyrazol-3-yl]-4-methylpentanamide | MFCD22376579 | 1191995-00-2 | BD167920 | DB15123 | HMS5552 | HMS-5552 | KBioSS_000661 | (S)-2-(4 |
| 规格或纯度 | Moligand™, ≥98% |
| 英文名称 | Dorzagliatin |
| 生化机理 | Dorzagliatin(HMS-5552、RO-5305552、Sinogliatin)是一种双效葡萄糖激酶(GK)激活剂,可改善 2 型糖尿病患者的血糖控制和胰岛β细胞功能。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 变构调节剂 |
| 作用机制 | 葡萄糖激酶的异构调节剂 |
| 产品介绍 |
Information Dorzagliatin Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a dual-acting glucokinase (GK) activator that improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes. Targets glucokinase |
| 纯度 | ≥98% |
| ALogP | 2.366 |
|---|---|
| hba_count | 4 |
| HBD Count | 3 |
| Rotatable Bond | 10 |
| PubChem SID | 504771642 |
|---|---|
| 分子类型 | 小分子 |
| IIUPAC Name | (2S)-2-[3-(2-chlorophenoxy)-5-oxo-2H-pyrrol-1-yl]-N-[1-[(2R)-2,3-dihydroxypropyl]pyrazol-3-yl]-4-methylpentanamide |
| INCHI | 1S/C22H27ClN4O5/c1-14(2)9-18(22(31)24-20-7-8-26(25-20)11-15(29)13-28)27-12-16(10-21(27)30)32-19-6-4-3-5-17(19)23/h3-8,10,14-15,18,28-29H,9,11-13H2,1-2H3,(H,24,25,31)/t15-,18+/m1/s1 |
| InChi Key | HMUMWSORCUWQJO-QAPCUYQASA-N |
| Smiles | CC(C)CC(C(=O)NC1=NN(C=C1)CC(CO)O)N2CC(=CC2=O)OC3=CC=CC=C3Cl |
| Isomeric SMILES | CC(C)C[C@@H](C(=O)NC1=NN(C=C1)C[C@H](CO)O)N2CC(=CC2=O)OC3=CC=CC=C3Cl |
| 关联CAS | 1191995-00-2 |
| MeSH Entry Terms | (2S)-2-(4-(2-Chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((2R)-2,3-dihydroxypropyl)-1H-pyrazol-3-yl)-4-methylpentanamide;Dorzagliatin;HMS5552;sinogliatin |
| 分子量 | 462.93 |
| Reaxy-Rn | 19545796 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19545796&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 92 mg/mL (198.73 mM); Ethanol: 92 mg/mL (198.73 mM); Water: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 92 |
| DMSO(mM) Max Solubility | 198.734149871471 |
| Water(mg / mL) Max Solubility | <1 |
| 分子量 | 462.900 g/mol |
| XLogP3 | 1.600 |
| 氢键供体数Hydrogen Bond Donor Count | 3 |
| 氢键受体数Hydrogen Bond Acceptor Count | 6 |
| 可旋转键计数Rotatable Bond Count | 10 |
| 精确质量Exact Mass | 462.167 Da |
| 单同位素质量Monoisotopic Mass | 462.167 Da |
| 拓扑极表面积Topological Polar Surface Area | 117.000 Ų |
| 重原子数Heavy Atom Count | 32 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 691.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 2 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | 警告 |
| 危险声明 |
H302: 吞食有害 H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。 P302+P352: 如皮肤沾染:用水充分清洗。 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 |
| 1. Grimsby J, Sarabu R, Corbett WL, Haynes NE, Bizzarro FT, Coffey JW, Guertin KR, Hilliard DW, Kester RF, Mahaney PE et al.. (2003) Allosteric activators of glucokinase: potential role in diabetes therapy.. Science, 301 (5631): (370-3). [PMID:12869762] |
| 2. Wang P, Liu H, Chen L, Duan Y, Chen Q, Xi S. (2017) Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus.. J Diabetes Res, 2017 (5812607). [PMID:28191470] |
| 3. Bloomgarden Z. (2019) Glucokinase and the potential of glucokinase activation in type 2 diabetes.. J Diabetes, 11 (8): (626-627). [PMID:31013387] |
| 4. Zhu XX, Zhu DL, Li XY, Li YL, Jin XW, Hu TX, Zhao Y, Li YG, Zhao GY, Ren S et al.. (2018) Dorzagliatin (HMS5552), a novel dual-acting glucokinase activator, improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes: A 28-day treatment study using biomarker-guided patient selection.. Diabetes Obes Metab, 20 (9): (2113-2120). [PMID:29707866] |
| 5. Toulis KA, Nirantharakumar K, Pourzitaki C, Barnett AH, Tahrani AA. (2020) Glucokinase Activators for Type 2 Diabetes: Challenges and Future Developments.. Drugs, 80 (5): (467-475). [PMID:32162273] |
| 6. Sharma P, Singh S, Sharma N, Singla D, Guarve K, Grewal AS. (2022) Targeting human Glucokinase for the treatment of type 2 diabetes: an overview of allosteric Glucokinase activators.. J Diabetes Metab Disord, 21 (1): (1129-1137). [PMID:35673438] |