RU.521 (Synonyms: RU-320521) |
| Catalog No.GC37570 |
RU.521(RU320521)은 강력하고 선택적인 순환 GMP-AMP 합성효소(cGAS) 억제제로 cGAS의 촉매 도메인에 결합하여 dsDNA가 cGAS를 활성화하는 것을 억제한다. RU.521은 cGAS를 중개하는 신호 전달을 억제하는 IC50 값이 700nM이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2262452-06-0
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');)
RU.521(RU320521)은 강력하고 선택적인 순환 GMP-AMP 합성효소(cGAS) 억제제로 cGAS의 촉매 도메인에 결합하여 dsDNA가 cGAS를 활성화하는 것을 억제한다. RU.521은 cGAS를 중개하는 신호 전달을 억제하는 IC50 값이 700nM이다.
RU.521（10μM）은 인간 메타푸몬바이러스（hMPV）가 16HBE 세포에서의 복제를 억제할 수 있고 RU.521이 존재하는 상황에서 외원적으로 인터렉틴 1 베타（IL-1β）를 추가해도 hMPV의 복제에 영향을 미치지 않는다（IL-1β는 hMPV의 복제를 촉진할 수 있다）[2]. RU.521（700nM）은 cGAS/STING 경로를 억제하여 중성세포 외분비 함정（NETs）이 HUVEC 세포에 가한 손상을 되돌릴 수 있다[3].
RU.521（5mg/kg）은 cGAS-STING 경로를 억제하고 소포체 스트레스（ERS）를 줄여서 폐허혈/재관류（I/R）쥐 모델의 폐손상을 완화시키고 폐 통기 기능을 증진시킬 수 있다[4]. 고혈압 쥐에서의 RU.521（0.4mg/kg）의 뇌내 투여는 쥐의 방실핵（PVN）에서 cGAS와 STING의 표현을 낮추고 LC3II/I 비율과 p62의 표현 수준도 낮췄다[5].
References:
[1] Vincent J, Adura C, Gao P, Luz A, Lama L, Asano Y, Okamoto R, Imaeda T, Aida J, Rothamel K, Gogakos T, Steinberg J, Reasoner S, Aso K, Tuschl T, Patel DJ, Glickman JF, Ascano M. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750. doi: 10.1038/s41467-017-00833-9. Erratum in: Nat Commun. 2017 Nov 23;8(1):1827.
[2] Wu G, Zhang Y, Niu L, Hu Y, Yang Y, Zhao Y. Interleukin-1β promotes human metapneumovirus replication via activating the cGAS-STING pathway. Virus Res. 2024 May;343:199344.
[3] Zhang B, Fang Z, Lin Y, et al. RU. 521 protects against neutrophil extracellular traps-induced vascular endothelial injury by inhibiting cGAS/STING pathway[J]. ||| Bangladesh Journal of Pharmacology|||, 2024, 19(2): 59-64.
[4] Vincent J, Adura C, Gao P, Luz A, Lama L, Asano Y, Okamoto R, Imaeda T, Aida J, Rothamel K, Gogakos T, Steinberg J, Reasoner S, Aso K, Tuschl T, Patel DJ, Glickman JF, Ascano M. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750.
[5] Han C, Qian X, Ren X, Zhang S, Hu L, Li J, Huang Y, Huang R, Ooi K, Lin H, Xia C. Inhibition of cGAS in Paraventricular Nucleus Attenuates Hypertensive Heart Injury Via Regulating Microglial Autophagy. Mol Neurobiol. 2022 Nov;59(11):7006-7024.
| 세포 실험 [1]: | |
세포 라인 | 16HBE 세포 |
제조 방법 | 16HBE 세포는 1, 10, 20μM의 cGAS 억제제 RU.521로 24시간 사전 처리한 후 인간 변성 폐바이러스(hMPV)에 48시간 동안 감염되었습니다. |
반응 조건 | 1, 10 및 20μM, 24시간 동안 |
응용 분야 | 16HBE 세포에 다양한 농도의 억제제를 처리한 후 HMPV의 복제가 현저히 감소했고 10μM RU.521은 현저한 억제 효과를 나타냈습니다. |
| 동물 실험 [2]: | |
동물 모형 | 폐허혈/재관류 (I/R)Sprague-Dawley 쥐 모델 |
제조 방법 | Sprague-Dawley 쥐는 왼쪽 폐문 막힘 재순환 수술을 받아 폐의 I/R 모델을 구축했습니다. 쥐는 복강 내에 cGAS특이 억제제 RU.521, STING 활성제 SR-717 그리고 ERS 억제제 4-페닐부타녈산(4-PBA)을 투여했습니다. |
제형 | 5mg/kg, 1시간 동안, i.p. |
응용 분야 | RU.521은 cGAS-STING 경로를 억제하여 폐허혈/재관류 손상을 완화시킵니다. |
References: | |
| Cas No. | 2262452-06-0 | SDF | |
| Synonyms | RU-320521 | ||
| Canonical SMILES | O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5 | ||
| Formula | C19H12Cl2N4O3 | M.Wt | 415.23 |
| Solubility | DMSO: ≥ 125 mg/mL (301.04 mM) | 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. |
||
| 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 | 2.4083 mL | 12.0415 mL | 24.083 mL |
| 5 mM | 481.7 μL | 2.4083 mL | 4.8166 mL |
| 10 mM | 240.8 μL | 1.2042 mL | 2.4083 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 ddH2O, 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *