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[CAS NO. 2262452-06-0] RU.521
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-114180 |
| Brand: | MCE |
| CAS: | 2262452-06-0 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 415.23 |
| Molecular Formula | C19H12Cl2N4O3 |
| SMILES | O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5 |
10 Publications Citing Use of MCE
- [1]Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5.
- [2]Neuron. 2022 Nov 4;S0896-6273(22)00961-8.
- [3]Proc Natl Acad Sci U S A. 2022 Oct 25;119(43):e2207280119.
- [4]Mbio. 2021 Oct 12;e0240821.
- [5]J Cereb Blood Flow Metab. 2022 Dec 19;271678X221147056.
- [6]Exp Neurol. 2022: 114269
- [7]Neuropharmacology. 2022 Aug 1;217:109206.
- [8]Cell Death Discov. 2022 May 11;8(1):258.
- [9]Toxicol Lett. 2022 Nov 8;S0378-4274(22)01779-9.
- [10]Dev Comp Immunol. 2022 Oct 10;104567.
Summary
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC 50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS) [1] .
IC50 & Target
IC50: 0.7 μM (dsDNA) [1]
In Vitro
In Vivo
RU.521 (5 mg/kg ; i.p. once) reduces symptoms from sepsis in mice [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male 8-week-old male mice with LPS injection [2] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection; 5 mg/kg once |
| Result: | Increased cardiac function and reduced the inflammatory responses, oxidative stress and apoptosis in hearts of mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 83.33 mg/mL ( 200.68 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4083 mL | 12.0415 mL | 24.0830 mL |
| 5 mM | 0.4817 mL | 2.4083 mL | 4.8166 mL |
| 10 mM | 0.2408 mL | 1.2042 mL | 2.4083 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution
References
- [1] Vincent J, et al. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750.
- [2] Xu Q, et al. Small molecule inhibition of cyclic GMP-AMP synthase ameliorates sepsis-induced cardiac dysfunction in mice. Life Sci. 2020 Nov 1;260:118315.
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