GPR81 agonist 1是一种高效、高选择性的G蛋白偶联受体81（GPR81）激动剂，对人和小鼠GPR81的EC50值分别为58nM和50nM。
Cas No.:1620992-67-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
GPR81 agonist 1 is a highly potent and selective G protein-coupled receptor 81 (GPR81) agonist with EC50 values of 58nM for human and 50nM for mouse GPR81[1]. GPR81, as a lactate receptor, plays an important role in immune regulation[2]. GPR81 agonist 1 can inhibit lipolysis in differentiated 3T3-L1 adipocytes[3]. GPR81 agonist 1 can improve insulin resistance and liver inflammation by inhibiting the NLRP3 inflammasome signaling pathway[4].
In vivo, intraperitoneal injection of GPR81 agonist 1 (10mg/kg) in a breast cancer (BRCA) model mouse significantly reduced PD-L1 expression in tumor tissue but did not reduce tumor volume[5].
References:
[1] Sakurai T, Davenport R, Stafford S, et al. Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing[J]. European journal of pharmacology, 2014, 727: 1-7.
[2] Brown T P, Bhattacharjee P, Ramachandran S, et al. The lactate receptor GPR81 promotes breast cancer growth via a paracrine mechanism involving antigen-presenting cells in the tumor microenvironment[J]. Oncogene, 2020, 39(16): 3292-3304.
[3] Feingold K R, Moser A, Shigenaga J K, et al. Inflammation inhibits GPR81 expression in adipose tissue[J]. Inflammation Research, 2011, 60(10): 991-995.
[4] Zhang Y, Lu Q H, Cao H F, et al. Effects of GPR81 agonist on insulin resistance in rats with nonalcoholic fatty liver disease[J]. Chinese Journal of Applied Physiology, 2021, 37(4): 354-358.
[5] Guo S, Zhou J, Lou P, et al. Potentiated effects of lactate receptor GPR81 on immune microenvironment in breast cancer[J]. Molecular Carcinogenesis, 2023, 62(9): 1369-1377.
GPR81 agonist 1是一种高效、高选择性的G蛋白偶联受体81（GPR81）激动剂，对人和小鼠GPR81的EC50值分别为58nM和50nM[1]。蛋白偶联受体（GPR81）作为乳酸受体，在免疫调节中具有重要作用[2]。GPR81 agonist 1能够抑制分化的3T3-L1脂肪细胞的脂解[3]。GPR81 agonist 1能够通过抑制NLRP3炎症小体信号通路，改善胰岛素抵抗和肝脏炎症[4]。
在体内，GPR81 agonist 1（10mg/kg）通过腹腔注射治疗乳腺癌（BRCA）模型小鼠，显著降低了肿瘤组织中PD-L1的表达，但是没有减小肿瘤体积[5]。
| Animal experiment [1]: | |
Animal models | Balb/c mice |
Preparation Method | 1×106 4T1 GFP mouse BRCA cells were injected subcutaneously into the mammary fat pad region of mice. Tumor size was measured twice weekly using a caliper. After the tumor volume reached 100-200mm3, the mice were randomly assigned to the following two groups: (1)vehicle (saline); (2) GPR81 agonist 1 (10mg/kg). All drugs were administered by intraperitoneal injections as indicated. The investigator was blinded to the treatment groups during the experiment and when assessing the outcome. Mice were monitored daily and euthanized by CO2 asphyxiation and cervical dislocation before any sign of distress. |
Dosage form | 10mg/kg; i.p. |
Applications | Mice treated with GPR81 agonist 1 showed significantly reduced PD-L1 expression; however, there was no significant difference in tumor volume between the two groups of mice. |
References: | |
| Cas No. | 1620992-67-7 | SDF | |
| Canonical SMILES | O=C([C@H]1CC[C@H](C)CC1)NC2=NC(C3=CC=CS3)=C(CC(N4CCN(C)CC4)=O)S2 | ||
| 分子式 | C22H30N4O2S2 | 分子量 | 446.63 |
| 溶解度 | DMSO : 50 mg/mL (111.95 mM; Need ultrasonic) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.239 mL | 11.1949 mL | 22.3899 mL |
| 5 mM | 447.8 μL | 2.239 mL | 4.478 mL |
| 10 mM | 223.9 μL | 1.1195 mL | 2.239 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: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet