| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In synovial fibroblasts, RVX-297 (1-30 μM; 24 hours) decreases the expression of pro-inflammatory genes [1]. Similar to pan-BET inhibitors that non-selectively bind BET BD, RVX-297 displaces BET proteins from sensitive gene promoters and inhibits the recruitment of active RNA polymerase II [1]. In vitro, RVX-297 decreases the gene expression of inflammatory mediators. In a dose-dependent way, RVX-297 suppresses the induction of the IL-6 gene in human U937 macrophages, mice primary B cells derived from the spleen, mouse BMDM, and THP-1 monocytes. With an IC50 of 0.4-3 μM, RVX-297 suppresses the expression of IL-1β in LPS-stimulated mouse BMDM. RVX-297 has an IC50 of 0.4 μM for inhibiting MCP-1 expression in unstimulated human PBMC. RVX-297 suppresses T cell antigen stimulation and IL-17 expression induction [1].
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| ln Vivo |
In an arthritic model caused by collagen in rats, RVX-297 (25–75 mg/kg; oral; once daily for 6 days) prevents disease advancement [1]. In mice with collagen-induced arthritis, RVX-297 (75–150 mg/kg) prevents the arthritis model's pathogenic advancement [1]. LPS-treated mice produce less cytokines when RVX-297 is administered [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: synovial fibroblasts Tested Concentrations: 1-30 μM Incubation Duration: 24 hrs (hours) Experimental Results: IL-6 and VCAM-1 gene expression was downregulated in synovial fibroblasts. |
| Animal Protocol |
Animal/Disease Models: Female Lewis rat, 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis) [1]
Doses: 25, 50 and 75 mg/kg Route of Administration: Po; one time/day for 6 Day Experimental Results: Prevents swelling and inflammation of ankle and knee joints. |
| References |
| Molecular Formula |
C24H29N3O4
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|---|---|
| Molecular Weight |
423.504766225815
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| Exact Mass |
423.215
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| CAS # |
1044871-04-6
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| PubChem CID |
135567084
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| Appearance |
White to light brown solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
639
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(C1C(C)=CC(C2=NC3C=C(C=C(C=3C(N2)=O)OC)OC)=CC=1C)CCN1CCCC1
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| InChi Key |
PQZDYFRDRHRZGF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H29N3O4/c1-15-11-17(12-16(2)22(15)31-10-9-27-7-5-6-8-27)23-25-19-13-18(29-3)14-20(30-4)21(19)24(28)26-23/h11-14H,5-10H2,1-4H3,(H,25,26,28)
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| Chemical Name |
2-[3,5-dimethyl-4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,7-dimethoxy-3H-quinazolin-4-one
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| Synonyms |
RVX-297 RVX297 RVX 297
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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 : ~50 mg/mL (~118.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3613 mL | 11.8064 mL | 23.6128 mL | |
| 5 mM | 0.4723 mL | 2.3613 mL | 4.7226 mL | |
| 10 mM | 0.2361 mL | 1.1806 mL | 2.3613 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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