| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
BMS614 selectively targets retinoic acid receptor α (RARα) with high affinity (Ki = 2.5 nM). It is a neutral antagonist, meaning it blocks agonist-induced coactivator recruitment without significantly affecting corepressor binding. The compound shows no significant effect on NCoR binding and only moderately decreases SMRT binding to RAR. This selectivity for RARα over other RAR subtypes makes BMS614 a valuable tool for dissecting RARα-specific signaling pathways.
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| ln Vitro |
In vitro, BMS614 antagonizes agonist-induced coactivator recruitment to RARα. It displays no significant effect on nuclear receptor corepressor (NCoR) binding but moderately decreases SMRT binding to RAR. The compound restores the expression of Bcl2. As a RARα-selective antagonist with a Ki of 2.5 nM, it is used in biochemical and cell-based assays to study RARα-mediated transcriptional regulation.
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| ln Vivo |
In vivo, BMS614 is orally active. It has been used to study the role of RARα signaling in various physiological and pathological processes. The compound's oral bioavailability makes it suitable for convenient administration in preclinical studies. However, detailed in vivo efficacy data and specific animal study protocols are not extensively documented in the available literature.
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| Enzyme Assay |
Not specifically documented for BMS614. For RAR antagonists, cell-free binding assays typically measure the displacement of radiolabeled retinoic acid from RARα using purified receptor preparations. Coactivator and corepressor recruitment assays may be performed using biochemical methods such as fluorescence polarization or AlphaScreen to assess antagonist activity. Binding affinity (Ki = 2.5 nM) is determined through competition binding studies.
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| Cell Assay |
In vitro cell-based assays for BMS614 may include reporter gene assays using RARα-responsive reporter constructs to measure transcriptional activity. The compound's ability to block agonist-induced transcription can be assessed in cells expressing RARα. Effects on coactivator and corepressor recruitment can be studied using cellular co-immunoprecipitation or imaging approaches.
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| Animal Protocol |
In vivo studies with BMS614 are likely conducted in mouse or rat models to study RARα signaling. The compound is orally active, allowing for convenient oral administration. Specific dosing regimens and animal models are detailed in the primary literature. The compound is used in research areas including cancer biology, developmental biology, and dermatology.
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| ADME/Pharmacokinetics |
BMS614 is orally active, indicating favorable oral bioavailability. As a small molecule with molecular weight approximately 452.5 (C29H24N2O3), it is suitable for oral administration. Detailed PK parameters such as half-life, Cmax, and AUC are available in the primary literature. The compound is supplied for research purposes only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BMS614 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 and is not for human or veterinary use.
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| References | |
| Additional Infomation |
BMS 195614 is a carboxamide formed by the condensation of the carboxyl group of 5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthyl-2-carboxylic acid with the amino group of p-aminobenzoic acid. It is a neutral retinoic acid receptor (RAR) α-selective antagonist (Ki = 2.5 nM). It has no significant effect on the binding of nuclear receptor co-inhibitor (NCoR); it moderately reduces the binding of SMRT to RAR. It antagonizes agonist-induced co-activator (CoA) recruitment. It functions as a retinoic acid receptor α-antagonist. It belongs to the quinoline, benzoic acid, and secondary carboxamide classes.
BMS614 is also known as BMS-195614 and BMS 614. It is a neutral RARα-selective antagonist with a Ki of 2.5 nM. The compound is orally active and restores Bcl2 expression. It is used as a tool compound to study RARα-specific functions in retinoid signaling pathways. The compound is available from various research chemical suppliers. |
| Molecular Formula |
C29H24N2O3
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|---|---|
| Molecular Weight |
448.52
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| Exact Mass |
448.178
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| CAS # |
182135-66-6
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| PubChem CID |
445091
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
607.3±55.0 °C at 760 mmHg
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| Flash Point |
321.1±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.693
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| LogP |
7.05
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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 |
4
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| Heavy Atom Count |
34
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| Complexity |
797
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WGLMBRZXZDAQHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H24N2O3/c1-29(2)14-13-23(21-15-19-5-3-4-6-26(19)30-17-21)24-16-20(9-12-25(24)29)27(32)31-22-10-7-18(8-11-22)28(33)34/h3-13,15-17H,14H2,1-2H3,(H,31,32)(H,33,34)
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| Chemical Name |
4-[(5,5-dimethyl-8-quinolin-3-yl-6H-naphthalene-2-carbonyl)amino]benzoic acid
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| Synonyms |
BMS-614; BMS 614; BMS-614
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2296 mL | 11.1478 mL | 22.2955 mL | |
| 5 mM | 0.4459 mL | 2.2296 mL | 4.4591 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2296 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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