| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
BMS753 selectively targets retinoic acid receptor α (RARα) with very high affinity (Ki = 2 nM). It shows no significant activity against RARγ in reporter-based assays or binding assays. Even at concentrations up to 100 nM, BMS753 fails to activate RARβ2. This remarkable subtype selectivity makes BMS753 a valuable tool for dissecting RARα-specific signaling pathways and distinguishing RARα functions from those of other RAR subtypes.
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| ln Vitro |
In WT cells and RARγ-/- cells, BMS 753 reduces RARβ transcript levels, but does not activate RARa-/- cells [1].
In vitro, BMS753 acts as a potent and specific agonist for RARα with a Ki of 2 nM. It does not display significant effects on RARγ in reporter-based assays or in binding assays measuring displacement of labeled retinoic acid. Even at concentrations up to 100 nM, BMS753 cannot activate RARβ2. This selectivity profile allows researchers to specifically activate RARα without confounding effects from other RAR subtypes. |
| ln Vivo |
In vivo, BMS753 is used to study the specific roles of RARα in various physiological and pathological processes including cancer biology, developmental biology, and dermatology. By selectively activating RARα, the compound helps elucidate the contribution of this receptor subtype to retinoid signaling in vivo. Detailed animal study protocols are available in the primary literature.
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| Enzyme Assay |
Not specifically documented for BMS753. For RAR agonists, cell-free binding assays typically measure the displacement of radiolabeled retinoic acid from RARα using purified receptor preparations. The Ki value of 2 nM is determined through such competition binding studies. Selectivity profiling against RARβ and RARγ is performed using similar binding assays or reporter-based assays.
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| Cell Assay |
In vitro cell-based assays for BMS753 include reporter gene assays using RARα-responsive reporter constructs to measure transcriptional activation. The compound's ability to activate RARα specifically can be assessed in cells expressing different RAR subtypes. Differentiation assays in various cell types may be used to study RARα-mediated effects. Concentration ranges typically span from low nanomolar to higher concentrations.
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| Animal Protocol |
In vivo studies with BMS753 are conducted in animal models to study RARα-specific functions in cancer, development, and dermatology. The compound may be administered via various routes depending on the experimental design. Specific dosing regimens and animal models are detailed in the primary literature. The compound provides a valuable tool for therapeutic targeting of RAR pathways.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BMS753 are not extensively documented. The compound is a small molecule with molecular weight 351.4 and formula C21H21NO4. It is soluble in DMSO (35.14 mg/mL). Storage recommendations include -20°C for 3 years as powder or 4°C for 2 years. Detailed PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BMS753 are not provided in the available literature. As a research compound, it is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. The compound is supplied for research purposes only.
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| References |
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| Additional Infomation |
BMS 753 is a homoselective retinoic acid receptor α (RARα) agonist.
BMS753 is also known as BMS 753. The IUPAC name is not provided in the available sources. The compound is classified as a Metabolic Enzyme compound. It is used in cancer biology, developmental biology, and dermatology research to investigate the specific roles of RARα in cellular regulation. The compound is a valuable tool for dissecting retinoid receptor subtype functions. |
| Molecular Formula |
C21H21NO4
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|---|---|
| Molecular Weight |
351.4
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| Exact Mass |
351.147
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| CAS # |
215307-86-1
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| PubChem CID |
9884820
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| Appearance |
White to off-white solid powder
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| LogP |
3.848
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
601
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KFBPBWUZXBYJDG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21NO4/c1-20(2)15-10-7-13(11-16(15)21(3,4)19(20)26)17(23)22-14-8-5-12(6-9-14)18(24)25/h5-11H,1-4H3,(H,22,23)(H,24,25)
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| Chemical Name |
4-[(1,1,3,3-tetramethyl-2-oxoindene-5-carbonyl)amino]benzoic acid
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| Synonyms |
BMS-753; BMS 753; BMS753
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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 (~142.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 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 25.0 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.92 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.92 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 | 2.8458 mL | 14.2288 mL | 28.4576 mL | |
| 5 mM | 0.5692 mL | 2.8458 mL | 5.6915 mL | |
| 10 mM | 0.2846 mL | 1.4229 mL | 2.8458 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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