GSK2330672
(Synonyms: GSK2330672) 目录号 : GC19180
An ASBT inhibitor
Cas No.:1345982-69-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK2330672 is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) which lowers glucose in an animal model of type 2 diabetes and shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes. IC50 value: 42 ± 3 nM [1]Target: hASBTin vitro: GSK2330672 is a highly potent, nonabsorbable ASBT inhibitor with excellent aqueous solubility, selectivity, and developability properties for evaluation in safety studies and ultimately humans. GSK2330672 will be a valuable clinical tool for exploring the therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.[1]in vivo: GSK2330672 results in potent inhibition of ASBT and very low oral absorption in the rat. GSK2330672 shows potent mouse and rat ASBT activity and was stable in GI stability assays. GSK2330672 is stable in the rodent GI tract and potently induced fecal bile acid excretion in mice, leading us to select these three compounds for mechanistic and efficacy studies in vivo in lean rats and Zucker Diabetic Fatty (ZDF) rats, respectively.[1]
References:
[1]. Wu Y, et al. Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114.
[2]. Nunez DJ, et al. Glucose and lipid effects of the ileal apical sodium-dependent bile acid transporter inhibitor GSK2330672: double-blind randomized trials with type 2 diabetes subjects taking metformin. Diabetes Obes Metab. 2016 Mar 4. doi: 10.1111/dom.12656.
[3]. Wang Y, et al. HNF4α Regulates CSAD to Couple Hepatic Taurine Production to Bile Acid Synthesis in Mice. Gene Expr. 2018 Aug 22;18(3):187-196.
| Cas No. | 1345982-69-5 | SDF | |
| 别名 | GSK2330672 | ||
| Canonical SMILES | O=C(O)CC(NCC1=C(OC)C=C(C2=C1)[C@@H](C3=CC=CC=C3)N[C@](CC)(CCCC)CS2(=O)=O)CC(O)=O | ||
| 分子式 | C28H38N2O7S | 分子量 | 546.68 |
| 溶解度 | DMSO : 21.5 mg/mL (39.33 mM) | 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 | 1.8292 mL | 9.1461 mL | 18.2922 mL |
| 5 mM | 0.3658 mL | 1.8292 mL | 3.6584 mL |
| 10 mM | 0.1829 mL | 0.9146 mL | 1.8292 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。