BR102375
目录号 : GC35547
BR102375 是一种用于治疗 2 型糖尿病的 non-TZD (噻唑烷二酮类) PPAR γ 完全激动剂， 其 EC50 值和 Amax比率值分别为 0.28 μM 和 98%。
Cas No.:2366255-59-4
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
BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%[1].
BR102375 (Compound 18) (10 μM) increases gene expression levels relevant to PPARγ activation and enhances glucose uptake under insulin stimulation[1].BR102375 (Compound 18) (10 nM, 100 nM, 1 μM; 6 days, 14 days) shows a concentration-dependent, insulin-sensitive effects on adipogenesis[1]. RT-PCR[1] Cell Line: 3T3-L1 mouse preadipocyte cells
BR102375 (Compound 18) has decent efficacy on mouse diabetes model[1].BR102375 reveals significant suppressive effect on random blood glucose increase(75 mpk, p.o., bid), shows decent effect on insulin resistance on Oral glucose tolerance test (OGTT) and discloses similar findings in body weight gain almost identical to Pioglitazone[1].
[1]. Choung W, et al. Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2019 Jun 19. pii: S0960-894X(19)30407-X.
| Cas No. | 2366255-59-4 | SDF | |
| Canonical SMILES | CCCCC(N1CC2=CC=C(C3=C(C4=NOC(N4)=O)C=CC=C3)C=C2)=NC(C)=C(CC5=NC(C(C)(C)C)=NO5)C1=O | ||
| 分子式 | C31H34N6O4 | 分子量 | 554.64 |
| 溶解度 | Soluble in DMSO | 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 | 1.803 mL | 9.0149 mL | 18.0297 mL |
| 5 mM | 0.3606 mL | 1.803 mL | 3.6059 mL |
| 10 mM | 0.1803 mL | 0.9015 mL | 1.803 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。
Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes
Bioorg Med Chem Lett 2019 Aug 15;29(16):2275-2282.PMID:31253533DOI:10.1016/j.bmcl.2019.06.027
As a potential treatment of type 2 diabetes, a novel PPARγ non-TZD full agonist, compound 18 (BR102375) was identified from the original lead BR101549 by the SAR efforts of the labile metabolite control through bioisosteres approach. In vitro assessments of BR102375 demonstrated its activating potential of PPARγ comparable to Pioglitazone as well as the induction of related gene expressions. Further in vivo evaluation of BR102375 in diabetic rodent models successfully proved its glucose lowering effect as a potential antidiabetic agent, but the anticipated suppression of weight gain was not evident. The X-ray co-crystal analysis of BR102375-PPARγ LBD unexpectedly revealed binding modes totally different from those of BR101549, which was found, instead, closely resembled to those of TZD full agonists.