ABR-238901

Cat No.:V74342 Purity: ≥98%
ABR-238901 is an orally bioactive S100A8/A9 blocker that can inhibit the interaction of S100A8/A9 with its receptors RAGE (receptor for advanced glycation end products) and TLR4 (toll-like receptor 4).
ABR-238901 Chemical Structure CAS No.: 1638200-22-2
Product category: TLR
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
ABR-238901 is an orally bioactive S100A8/A9 blocker that can inhibit the interaction of S100A8/A9 with its receptors RAGE (receptor for advanced glycation end products) and TLR4 (toll-like receptor 4). ABR-238901 has the potential for myocardial infarction (MI) research.
Biological Activity I Assay Protocols (From Reference)
ln Vivo
MDSCs treated with ABR-238901 (30 mg/kg/day; gavage; for 3 weeks) exhibit decreased angiogenesis as well as IL6 and IL10 levels[1]. When paired with bortezomib (0.6 mg/kg; subcutaneous injection; twice weekly), ABR-238901 (30 mg/kg/day; gavage) decreased the amount of tumor when compared to therapy with either drug alone[1]. In C57BL/6NRJ mice, ABR-238901 (30 mg/kg; intraperitoneal; for the first three days; then, continuing oral daily dosage; for 21 days) causes myocardial ischemia brought on by permanent coronary artery ligation, which progressively deteriorates cardiac function and speeds up left ventricular remodeling. In the initial three days following a myocardial infarction (MI), ABR-238901 treatment reduces inflammatory damage and fosters a healing milieu[2].
Animal Protocol
Animal/Disease Models: C57BL/KaLwRij mice with 5T33MMvv cells[1]
Doses: 30 mg/kg
Route of Administration: Gavage; daily; for 3 weeks
Experimental Results: Caused less angiogenesis. Caused less IL6 and IL10 in myeloid-derived suppressor cells (MDSCs).
References
[1]. Kim De Veirman, et al. Extracellular S100A9 Protein in Bone Marrow Supports Multiple Myeloma Survival by Stimulating Angiogenesis and Cytokine Secretion. Cancer Immunol Res. 2017 Oct;5(10):839-846.
[2]. Goran Marinković, et al. S100A9 Links Inflammation and Repair in Myocardial Infarction. Circ Res. 2020 Aug 14;127(5):664-676.
[3]. A. Schiopu, et al. Short-term blockade of the S100A8/A9 alarmin in the immediate post-myocardial infarction period inhibits acute myocardial inflammation and preserves myocardial repair. European Heart Journal, Volume 38, Issue suppl_1, August 2017, ehx504.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H9BRCLN3O4S
Molecular Weight
394.63
CAS #
1638200-22-2
SMILES
C1=NC(OC)=C(Br)C=C1S(NC1=C(O)C(Cl)=CN=C1)(=O)=O
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: 33.33 mg/mL (84.46 mM)
H2O: < 0.1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5340 mL 12.6701 mL 25.3402 mL
5 mM 0.5068 mL 2.5340 mL 5.0680 mL
10 mM 0.2534 mL 1.2670 mL 2.5340 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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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)
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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.
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