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Purity: ≥98%
| Targets |
BMS-192364 targets the interaction between Gα proteins and regulators of G protein signaling (RGS) proteins. RGS proteins are GTPase-activating proteins (GAPs) that accelerate the hydrolysis of GTP to GDP by Gα subunits, thereby terminating G protein signaling. By targeting Gα-RGS interactions, BMS-192364 generates inactive Gα-RGS complexes, effectively modulating G protein signaling. The compound exerts RGS agonist properties by increasing the effect of GAP on Gq proteins. This modulation of G protein signaling pathways affects various downstream effects, including the inhibition of calcium flux. The compound's activity at Gq proteins is particularly relevant for its effects on smooth muscle contraction and other Gq-mediated processes.
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| ln Vitro |
In vitro, BMS-192364 has been shown to target Gα-RGS interactions and inhibit calcium flux. Its activity is typically measured using cell-based assays that assess G protein signaling and calcium mobilization. The compound reduces bladder contractions by modulating Gq protein signaling and increasing the effect of GAP on Gq proteins. These in vitro studies confirm BMS-192364's mechanism of action as a modulator of G protein signaling. However, specific IC50 or EC50 values are not detailed in standard product descriptions. BMS-192364 is a valuable tool for studying G protein signaling pathways.
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| ln Vivo |
In vivo activity data for BMS-192364 is limited, as the compound is primarily used as a research tool in in vitro studies. However, its mechanism of action—modulating G protein signaling—suggests potential in vivo applications in conditions involving smooth muscle dysfunction, such as overactive bladder. The compound could be used in animal models to study the effects of G protein modulation on bladder function and other physiological processes. However, specific in vivo protocols and results are not detailed in standard product descriptions. BMS-192364 is a research compound used to study G protein signaling.
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| Enzyme Assay |
In vitro assays for BMS-192364 measure its effects on Gα-RGS interactions and G protein signaling. These assays typically use cell-based systems or purified proteins. The compound's ability to modulate Gα-RGS interactions can be assessed using techniques such as co-immunoprecipitation, fluorescence resonance energy transfer (FRET), or surface plasmon resonance (SPR). Calcium flux assays are used to measure the compound's effects on Gq-mediated calcium mobilization. Cells loaded with a calcium-sensitive dye are treated with BMS-192364, and the change in fluorescence is measured. These assays confirm the compound's activity as a modulator of G protein signaling.
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| Cell Assay |
In vitro cell-based assays for BMS-192364 are used to study its effects on G protein signaling and cellular function. Cells expressing Gq-coupled receptors are treated with BMS-192364, and calcium mobilization is measured using a fluorescent calcium indicator. The compound's ability to inhibit calcium flux is assessed. Other functional assays can measure the effects on downstream signaling pathways, such as the activation of protein kinase C (PKC) or the mitogen-activated protein kinase (MAPK) pathway. These assays confirm the compound's activity as a modulator of G protein signaling in a cellular context.
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| Animal Protocol |
In vivo animal experiments for BMS-192364 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a modulator of G protein signaling would involve its administration to animal models of smooth muscle dysfunction or other relevant conditions. The compound's effects on bladder contractions, for example, could be assessed in rodent models of overactive bladder. However, specific protocols for BMS-192364 are not detailed.
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| ADME/Pharmacokinetics |
BMS-192364 has a molecular weight of 355.70 g/mol and a molecular formula of C15H9ClF3N3O2. Its IUPAC name is 2-(5-chloro-2-hydroxyphenyl)-5-(4-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-3(2H)-one. It is a white to off-white solid powder with a logP of 3.605. For storage, it is recommended to keep the powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. The compound is stable at ambient temperature for a few days during shipping. It may dissolve in DMSO.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for BMS-192364 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. BMS-192364 is a modulator of G protein signaling, and its toxicity would be related to its effects on G protein-mediated signaling pathways in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling BMS-192364. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References |
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| Additional Infomation |
BMS-192364 is a research compound and is not approved for any clinical or therapeutic use. It is a bio-active small molecule that targets Gα-RGS interactions to generate inactive Gα-RGS complexes. BMS-192364 reduces bladder contractions and exerts RGS agonist properties by increasing the effect of GAP on Gq proteins. It also inhibits calcium flux. The compound was developed by Bristol Myers Squibb and has been investigated for potential therapeutic applications. BMS-192364 is a valuable research tool for studying G protein signaling and its role in various physiological and pathological processes.
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| Molecular Formula |
C15H9CLF3N3O2
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| Molecular Weight |
355.69906
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| Exact Mass |
355.034
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| CAS # |
202822-21-7
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| PubChem CID |
135565394
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| Appearance |
White to off-white solid powder
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| LogP |
3.605
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
521
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XNRWPJIJOVVQRQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H9ClF3N3O2/c16-10-5-6-12(23)11(7-10)22-14(24)20-13(21-22)8-1-3-9(4-2-8)15(17,18)19/h1-7,23H,(H,20,21,24)
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| Chemical Name |
2-(5-chloro-2-hydroxyphenyl)-5-(4-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-3(2H)-one
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| Synonyms |
BMS-192364 BMS 192364 BMS192364 UNII-1NC8D8P7QF.
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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 | 2.8114 mL | 14.0568 mL | 28.1136 mL | |
| 5 mM | 0.5623 mL | 2.8114 mL | 5.6227 mL | |
| 10 mM | 0.2811 mL | 1.4057 mL | 2.8114 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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