SR 202
(Synonyms: 米福贝特,SR-202) 目录号 : GC11586
An antagonist of agonist-induced PPARγ transcriptional activity
Cas No.:76541-72-5
Sample solution is provided at 25 µL, 10mM.
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IC50: 140 μM for attenuation of troglitazone-induced peroxisome proliferator-activated receptor gamma (PPAR) transcriptional activity [1]
The phosphonophosphate SR-202 [(S)-(4-chlorophenyl)(dimethoxyphosphoryl)methyl dimethyl phosphate] is a PPAR antagonist, which inhibits both TZD-stimulated recruitment of the coactivator steroid receptor coactivator-1 and TZD-induced transcriptional activity of the receptor. PPAR is a nuclear receptor which regulates glucose metabolism and fatty acid storage.
In vitro: SR-202 is a specific antagonist of PPAR, which shows selectivity both among the PPAR family members and other nuclear receptors. SR-202 also Inhibits PPAR-dependent differentiation of adipocytes. In cell culture, SR-202 efficiently antagonizes hormone- and TZD induced adipocyte differentiation [1].
In vivo:. Decreasing PPAR activity by treatment with SR-202 leads to a reduction of both high fat diet-induced adipocyte hypertrophy and insulin resistance. Treatment with SR-202 also dramatically improves insulin sensitivity in the diabetic ob/ob mice [1]. When wild-type mice are fed a high-fat diet, the plasma levels of TNF-α are raised, and SR-202 treatment protects against this rise [2]..
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Rieusset J, Touri F, Michalik L, Escher P, Desvergne B, Niesor E, Wahli W. A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesity and antidiabetic activity. Mol Endocrinol. 2002 Nov;16(11):2628-44.
[2] Doggrell S. Do peroxisome proliferation receptor-gamma antagonists have clinical potential as combined antiobesity and antidiabetic drugs Expert Opin Investig Drugs. 2003 Apr;12(4):713-6.
| Cas No. | 76541-72-5 | SDF | |
| 别名 | 米福贝特,SR-202 | ||
| 化学名 | (S)-(4-chlorophenyl)(dimethoxyphosphoryl)methyl dimethyl phosphate | ||
| Canonical SMILES | ClC1=CC=C(C=C1)[C@@H](OP(OC)(OC)=O)P(OC)(OC)=O | ||
| 分子式 | C11H17ClO7P2 | 分子量 | 358.65 |
| 溶解度 | Water: 100 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 | 2.7882 mL | 13.9412 mL | 27.8823 mL |
| 5 mM | 0.5576 mL | 2.7882 mL | 5.5765 mL |
| 10 mM | 0.2788 mL | 1.3941 mL | 2.7882 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet