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  3. RVX-297

RVX-297 

Cat. No.: HY-114504 Purity: 96.59%
Handling Instructions

RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.

For research use only. We do not sell to patients.

RVX-297 Chemical Structure

RVX-297 Chemical Structure

CAS No. : 1044871-04-6

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5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
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25 mg USD 850 In-stock
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50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2].

IC50 & Target[2]

BRD2 (BD1)

3.76 μM (IC50)

BRD2 (BD2)

0.08 μM (IC50)

BRD3 (BD1)

2.34 μM (IC50)

BRD3 (BD2)

0.05 μM (IC50)

BRD4 (BD1)

1.16 μM (IC50)

BRD4 (BD2)

0.02 μM (IC50)

BRDT (BD1)

2.69 μM (IC50)

In Vitro

RVX-297 (1-30 μM; 24 hours) decreases proinflammatory gene expression in synovial fibroblasts[1].
RVX-297 displaces BET proteins from the promoters of sensitive genes and disrupted recruitment of active RNA polymerase II, a property shared with pan-BET inhibitors that nonselectively bind BET BDs[1].
RVX-297 reduces gene expression of inflammatory mediators in vitro. RVX-297 suppresses IL-6 gene induction in human U937 macrophages, mouse primary B cells isolated from the spleen, mouse BMDMs, and THP-1 monocytes in a dose-dependent manner. RVX-297 represses IL-1β expression in LPS-stimulated mouse BMDMs, with an IC50 of 0.4-3 μM. RVX-297 inhibits MCP-1 expression in unstimulated human PBMCs with an IC50 of 0.4 μM. RVX-297 inhibits antigen stimulation of T cells and the induction of IL-17 expression[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: Synovial fibroblasts
Concentration: 1-30 μM
Incubation Time: 24 hours
Result: Downregulated IL-6 and VCAM-1 gene expression in synovial fibroblasts.
In Vivo

RVX-297 (25-75 mg/kg; p.o.; per day for 6 day) inhibits progression of pathology in the rat collagen-induced arthritis model[1].
RVX-297 (75-150 mg/kg) inhibits progression of pathology in the mouse collagen-induced arthritis model[1].
RVX-297 suppresses cytokine production in LPS-treated mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats are 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis)[1]
Dosage: 25, 50, and 75 mg/kg
Administration: P.o.; per day for 6 days
Result: Prevented swelling and inflammation of the ankle and knee joints.
Molecular Weight

423.50

Formula

C₂₄H₂₉N₃O₄

CAS No.
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
In Vitro: 

DMSO : 50 mg/mL (118.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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 4.7225 mL
10 mM 0.2361 mL 1.1806 mL 2.3613 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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RVX-297
Cat. No.:
HY-114504
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