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Ro 24-7429

Alias: Ro247429; Ro247429; Ro-247429; Ro 247429;Ro 24-7429; Ro-24-7429;
Cat No.:V8379 Purity: ≥98%
Ro 24-7429 (Ro247429; Ro-247429) is a novel and potent Tat (HIV-1 transactivator protein) antagonistwithanti-HIV, antifibrotic and anti-inflammatory activities.
Ro 24-7429
Ro 24-7429 Chemical Structure CAS No.: 139339-45-0
Product category: HIV
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
Other Sizes

Other Forms of Ro 24-7429:

  • CBFβ-​RUNX1 inhibitor 1
  • Ro5-3335
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist.Another inhibitor of runt-related transcription factor 1 (RUNX1) is Ro24-7429. Ro24-7429 exhibits anti-inflammatory, anti-fibrotic, and anti-HIV properties.
Biological Activity I Assay Protocols (From Reference)
Targets
HIV-1
ln Vitro
Cultured PBMCs are susceptible to dose-dependent apoptosis when exposed to Ro 24-7429 (0.1–5 μM) for three days. Moreover, Ro 24-7429 (1–25 μM) suppresses antigen-induced lymphocyte proliferation and causes apoptosis[1].
In a dose-dependent manner, Ro24-7429 (50-200 μM; 24-72 hours) strongly inhibits the proliferation of A549 and HLF cells. TNF-α-induced up-regulation of RUNX1 mRNA is significantly reduced by 50% after 48 hours with Ro24-7429 treatment at 75 μM[2].
ln Vivo
In the Bleomycin-induced pulmonary fibrosis (PF) mouse model, treatment with Ro24-7429 (17.5-70 mg/kg; i.p.; daily; for 14 or 21 days) significantly reduces lung inflammation and fibrosis. In injured mouse lungs, Ro24-7429 reduces the expression of fibrosis markers[2].
Animal Protocol
Animal Model: Bleomycin-induced male and female C57BL/6J mice (aged 6–8 weeks)[2]
Dosage: 17.5 mg/kg, 35 mg/kg, and 70 mg/kg
Administration: i.p.; daily; for 14 or 21 days
Result: reduced inflammation and lung fibrosis in the PF mouse model induced by bleomycin.
References

[1]. HIV-1 Tat protein and its inhibitor Ro 24-7429 inhibit lymphocyte proliferation and induce apoptosis in peripheral blood mononuclear cells from healthy donors. Cell Immunol. 1996 Apr 10;169(1):40-6.

[2]. Targeting Runt-Related Transcription Factor 1 Prevents Pulmonary Fibrosis and Reduces Expression of Severe Acute Respiratory Syndrome Coronavirus 2 Host Mediators. Am J Pathol. 2021 Jul;191(7):1193-1208.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H13CLN4
Molecular Weight
272.74
Exact Mass
272.0829
Elemental Analysis
C, 61.65; H, 4.80; Cl, 13.00; N, 20.54
CAS #
139339-45-0
Related CAS #
139339-45-0; 2328140-37-8; 30195-30-3;
Appearance
Solid powder
SMILES
CNC1CN=C(C2=CC=CN2)C2C=C(C=CC=2N=1)Cl
InChi Key
LEAKQIXYSHIHCW-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H13ClN4/c1-16-13-8-18-14(12-3-2-6-17-12)10-7-9(15)4-5-11(10)19-13/h2-7,17H,8H2,1H3,(H,16,19)
Chemical Name
3H-1,4-Benzodiazepin-2-amine, 7-chloro-N-methyl-5-(1H-pyrrol-2-yl)-
Synonyms
Ro247429; Ro247429; Ro-247429; Ro 247429;Ro 24-7429; Ro-24-7429;
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~62.5 mg/mL (~229.16 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.63 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 (7.63 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (7.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.


Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saliney: ≥ 2.08 mg/mL (7.63 mM)

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6665 mL 18.3325 mL 36.6650 mL
5 mM 0.7333 mL 3.6665 mL 7.3330 mL
10 mM 0.3666 mL 1.8332 mL 3.6665 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • Antifibrotic and anti-inflammatory effect of Ro24-7429 at day 14 in the bleomycin model of pulmonary fibrosis.[2].Am J Pathol. 2021 Jul;191(7):1193-1208.
  • Antifibrotic and anti-inflammatory effect of Ro24-7429 at day 7 in the bleomycin model of idiopathic pulmonary fibrosis. [2].Am J Pathol. 2021 Jul;191(7):1193-1208.
  • The effect of cytokine stimulation and Ro24-7429 treatment on expression of fibrosis markers in lung epithelial and vascular endothelial cells. [2].Am J Pathol. 2021 Jul;191(7):1193-1208.
  • RUNX1 expression during SARS-CoV-2 infection and the in vitro and in vivo effects of RUNX1 inhibition in human epithelial and endothelial cells. [2].Am J Pathol. 2021 Jul;191(7):1193-1208.
  • Schematic of hypothesis of RUNX1's role in transforming growth factor (TGF)-β1 (blue), tumor necrosis factor (TNF)-α (pink), and shared (purple) signaling and its effects on SARS-CoV-2–related proteins FURIN and angiotensin-converting enzyme 2 (ACE2). [2].Am J Pathol. 2021 Jul;191(7):1193-1208.
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