| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
RIG012 targets the Retinoic Acid Inducible Gene I (RIG-I) innate immune receptor. RIG-I is a cytosolic pattern recognition receptor that detects viral RNA and initiates innate immune responses. RIG012 functions as a potent antagonist of RIG-I, blocking RIG-I-initiated signaling and suppressing downstream type I interferon (e.g., IFN-β) and interferon-stimulated gene expression. The compound also inhibits inflammatory responses induced by SARS-CoV-2 RNA.
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| ln Vitro |
The visible range is absorbed by a strong chromophore (λmax of 470 nm) present in RIG012. Significant hyperchromic shift to greater intensity value occurs in RIG012's 470 nm absorption band after interacting with RIG-I [1]. In co-transfected HEK293T cells with reporter and temporary terminals, RIG012 (1, 1.25, 1.5, 2, 2.5, 3, 4 μM) exhibits a strong dose-regulated suppression of RIG-I signaling [1]. IFN-β and ISG hRsad2 expression in A549 cells were potently and dose-regulatedly inhibited at 1.25, 2.25, 4.5, 9, and 18 μM [1].
RIG012 demonstrates potent inhibitory activity against RIG-I with an IC50 of 0.71 μM in the NADH-coupled ATPase assay. It effectively blocks RIG-I-initiated signaling and inhibits the transcriptional induction of CXCL10, IFN-β 1, and IRF9, while reducing IL6 mRNA levels. RIG012 inhibits IFN-β and ISG hRsad2 expression. The compound contains a strong chromophore that absorbs in the visible range (λmax of 470 nm), and upon interacting with RIG-I, a significant hyperchromic shift occurs in its 470 nm absorption band. |
| ln Vivo |
In vivo studies have evaluated RIG012 in models of RIG-I-mediated inflammatory responses. RIG012 treatment modulates the RLR-signaling pathway and downstream interferon and interferon-stimulated gene expression. The compound has been investigated in the context of SARS-CoV-2-induced inflammatory responses. Pharmacokinetic data for RIG012 have been acquired using mass spectrometry. Further in vivo characterization is ongoing to define its full pharmacological profile.
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| Enzyme Assay |
The NADH-coupled ATPase assay is used to measure RIG012's inhibition of RIG-I enzymatic activity. Recombinant RIG-I protein is incubated with ATP in assay buffer. RIG012 is added at varying concentrations, and ATP hydrolysis is measured by monitoring NADH oxidation at 340 nm. The decrease in absorbance is proportional to ATPase activity. IC50 values are calculated from dose-response curves. This assay provides a quantitative measure of RIG012's potency against the RIG-I ATPase domain.
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| Cell Assay |
Cellular activity of RIG012 is evaluated in RIG-I-expressing cell lines stimulated with RIG-I agonists such as poly(I:C) or synthetic RNA ligands. Cells are pre-treated with RIG012 at escalating concentrations, then stimulated to activate RIG-I signaling. IFN-β and ISG expression are measured by qRT-PCR or ELISA. CXCL10 and IL6 mRNA levels are assessed to evaluate the compound's ability to block downstream inflammatory responses.
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| Animal Protocol |
In vivo pharmacological evaluation of RIG012 involves administration to mouse models of RIG-I-mediated inflammation or viral infection. The compound is typically administered via intraperitoneal injection or oral gavage at various doses. Blood and tissue samples are collected to measure cytokine and interferon levels. RIG-I pathway activation is assessed by measuring IFN-β and ISG expression in target tissues. Efficacy is evaluated by monitoring inflammatory responses and disease progression.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of RIG012 have been characterized using mass spectrometry-based methods. The compound has a molecular formula of C23H21NO3 and a molecular weight of 359.42. It is soluble in DMSO (72 mg/mL) and ethanol (6 mg/mL), but insoluble in water. For in vivo administration, oral formulations include CMC-Na suspension (≥5 mg/mL) and injection formulations using DMSO/PEG300/Tween 80/saline or DMSO/corn oil. Powder is stable at -20°C for 3 years.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of RIG012 indicates that it is well-tolerated in preclinical studies at efficacious doses. As a RIG-I antagonist, the compound is designed to modulate immune responses rather than induce cytotoxicity. The compound is for research use only and not intended for therapeutic use in humans. Comprehensive toxicity profiling, including acute and repeated-dose studies, would be required for clinical development.
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| References | |
| Additional Infomation |
RIG012 was first reported in ACS Chemical Biology (2020) by David C. Rawling et al. It is a potent RIG-I antagonist that blocks RIG-I-mediated signaling and suppresses downstream type I interferon and interferon-stimulated gene expression. The compound has been cited in Nature Medicine for its top-tier quality. RIG012 is a valuable tool for studying RIG-I biology, innate immune responses, and inflammatory diseases. It supports research in medicinal chemistry, molecular pharmacology, and early-stage evaluation of potential therapeutic strategies in oncology and inflammation.
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| Molecular Formula |
C23H21NO3
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| Molecular Weight |
359.417746305466
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| Exact Mass |
359.15
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| Elemental Analysis |
C, 76.86; H, 5.89; N, 3.90; O, 13.35
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| CAS # |
2642218-43-5
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| PubChem CID |
154717119
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| Appearance |
Orange to red solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
680
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C2C(=C(OCC3=CC=CC=C3)C(=O)C3=CC=CC=C32)C(CC)(CC)C1=O
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| InChi Key |
OEWZCENSPLZNPQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H21NO3/c1-3-23(4-2)18-19(24-22(23)26)16-12-8-9-13-17(16)20(25)21(18)27-14-15-10-6-5-7-11-15/h5-13H,3-4,14H2,1-2H3
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| Chemical Name |
4-(benzyloxy)-3,3-diethyl-2H-benzo[g]indole-2,5(3H)-dione
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| Synonyms |
RIG012; RIG-012; RIG 012
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~92.73 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7823 mL | 13.9113 mL | 27.8226 mL | |
| 5 mM | 0.5565 mL | 2.7823 mL | 5.5645 mL | |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7823 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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