GPR81 agonist 1 |
Catalog No.GC61625
One-Click Copy Product Info
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GPR81 agonist 1은 인간 GPR81에 대해 EC50 값이 58 nM이고 쥐 GPR81에 대해 50 nM인 고효능 및 선택성 G 단백질 연결 수용체 81(GPR81) 작용제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1620992-67-7
Sample solution is provided at 25 µL, 10mM.
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GPR81 agonist 1은 인간 GPR81에 대해 EC50 값이 58 nM이고 쥐 GPR81에 대해 50 nM인 고효능 및 선택성 G 단백질 연결 수용체 81(GPR81) 작용제이다. GPR81은 젖산 수용체로서 면역 조절에 중요한 역할을 한다[2]. GPR81 agonist 1은 분화된 3T3-L1 지방세포에서 지방분해를 억제할 수 있다[3]. GPR81 agonist 1은 NLRP3 인플라마좀 신호전달 경로를 억제해서 인슐린 저항성 및 간 염증을 개선할 수 있다[4].
체내 실험에서 유방암(BRCA) 모델 쥐에게 복강 내 주사로 GPR81 agonist 1(10 mg/kg)을 투여한 후 종양 조직 내 PD-L1 발현을 현저하게 감소시켰지만 종양 부피는 감소시키지 못하였다[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.
| 동물 실험 [1]: | |
동물 모형 | Balb/c 쥐 |
제조 방법 | 1×10⁶개의 4T1 GFP 쥐 BRCA 세포를 쥐의 유방 지방 패드 영역에 피하 주사하였습니다. 캘리퍼스를 사용해서 주 2회 종양 크기를 측정하였습니다. 종양 부피가 100-200 mm³에 도달한 후 쥐를 다음 두 그룹으로 무작위 배정하였습니다: (1) 용매(생리식염수); (2) GPR81 작용제 1(10 mg/kg). 모든 약물은 지시된 대로 복강 내 주사로 투여하였습니다. 실험 기간 동안 및 결과 평가할 때 연구자는 처리 그룹에 대해 블라인드 처리되었습니다. 쥐는 매일 관찰되었고 고통 징후가 나타나기 전에 CO₂ 질식 및 경추 탈위법으로 안락사하였습니다. |
제형 | 10mg/kg; i.p. |
응용 분야 | GPR81 agonist 1로 처리된 쥐는 PD-L1 발현이 현저하게 감소하였지만 두 그룹의 쥐 간 종양 부피에는 유의한 차이가 없었습니다. |
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 | ||
| Formula | C22H30N4O2S2 | M.Wt | 446.63 |
| Solubility | DMSO : 50 mg/mL (111.95 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)