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RU.521

Name: RU.521
Brand: TargetMol
SKU: T5486
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: RU320521) Copy Product Info

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Synonyms: RU320521

Catalog No. T5486 Copy Product Info

Purity: 99.78%

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RU.521 (RU3205217) is a selective cyclic GMP-AMP synthetase (cGAS) inhibitor (mouse: IC50=0.11 μM), (human: IC50=2.94 μM). RU.521 is an inhibitor of the receptor activated by dsDNA (IC50=700 nM). RU.521 inhibits cGAS-mediated interferon upregulation. RU.521 reduces constitutive interferon expression in macrophages derived from a mouse model of Aicardi-Goutieres syndrome.

Cas No. 2262452-06-0

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Pack Size	Price	USA Stock	Global Stock
1 mg	$38	In Stock	In Stock
2 mg	$56	In Stock	In Stock
5 mg	$97	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$276	In Stock	In Stock
50 mg	$392	-	In Stock
100 mg	$579	-	In Stock
1 mL x 10 mM (in DMSO)	$97	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.78%

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	RU.521 (RU3205217) is a selective cyclic GMP-AMP synthetase (cGAS) inhibitor (mouse: IC50=0.11 μM), (human: IC50=2.94 μM). RU.521 is an inhibitor of the receptor activated by dsDNA (IC50=700 nM). RU.521 inhibits cGAS-mediated interferon upregulation. RU.521 reduces constitutive interferon expression in macrophages derived from a mouse model of Aicardi-Goutieres syndrome.
Targets & IC50	dsDNA:700 nM, H69AR cells:32.9 μM, THP-1-Dual cells:38.4 μM (CC50)
In vitro	METHODS: Human THP1-Dual cells were treated with RU.521 for 24 hours, and the cytotoxicity was determined using the CCK-8 assay. RESULTS: RU.521 inhibited cell growth (CC50=38.4 μM). [1]
In vivo	METHODS: To study the effect of RU.521 on sepsis, mice were intraperitoneally injected with RU.521 (5 mg/kg) (injected with LPS) in a single dose. RESULTS: RU.521 enhanced cardiac function, reduced cardiac inflammation, oxidative stress and apoptosis, and alleviated the symptoms of sepsis in mice. [2]
Synonyms	RU320521
Cell Research	Small-molecule compounds were serially diluted to concentrations spanning the range tested in the response curves were added to 6.7?×?10^5 RAW-Blue macrophages plated 16?h prior in 96-well dishes, then harvested 72?h after compound addition. ATP was measured using CellTiter Glo Viability Assay using 50?μM Tamoxifen as a positive control for cytotoxicity. Viability values were generated using vehicle (DMSO) or the first dose as 100% and Tamoxifen as 0%. Outliers were removed.
Animal Research	the chronically elevated levels of cytokines observed in Trex1 null mice are a consequence of constitutively activated cGAS, due to the inability to eliminate aberrantly localized self-DNA. We harvested BMDMs from 6–8-week old Trex1 ?/? mice, treated them with each compound, and measured expression levels of IFNB1 by quantitative reverse transcription PCR (qRT-PCR). Treatment of primary BMDMs with RU.521 or its analogs reduced IFNB1 expression, indicating their effectiveness in suppressing intrinsic DNA-dependent, constitutively-activated type I interferon expression in cells deficient of a cytoplasmic DNA exonuclease.

Chemical Properties

Molecular Weight	415.23
Formula	C₁₉H₁₂Cl₂N₄O₃
Cas No.	2262452-06-0
Smiles	Cc1nn(c(O)c1C1OC(=O)c2ccccc12)-c1nc2ccc(Cl)c(Cl)c2[nH]1
Relative Density.	1.73 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 126.3 mg/mL (304.17 mM), Sonication is recommended.

In Vivo Formulation

5% DMSO+40% PEG300+5% Tween 80+50% Saline: 2 mg/mL (4.82 mM)

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4083 mL	12.0415 mL	24.0830 mL	120.4152 mL
5 mM	0.4817 mL	2.4083 mL	4.8166 mL	24.0830 mL
10 mM	0.2408 mL	1.2042 mL	2.4083 mL	12.0415 mL
20 mM	0.1204 mL	0.6021 mL	1.2042 mL	6.0208 mL
50 mM	0.0482 mL	0.2408 mL	0.4817 mL	2.4083 mL
100 mM	0.0241 mL	0.1204 mL	0.2408 mL	1.2042 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.