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| Targets |
BC-1471 targets STAM-binding protein (STAMBP), a deubiquitinase that removes ubiquitin from proteins. By inhibiting STAMBP, BC-1471 prevents the deubiquitination of its substrates, leading to decreased levels of NALP7. This results in the suppression of IL-1β release, a pro-inflammatory cytokine, after TLR stimulation. This mechanism makes it a potential anti-inflammatory agent.
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| ln Vitro |
In vitro, BC-1471 inhibits STAMBP deubiquitinase activity. It decreases NALP7 protein levels and suppresses IL-1β release after TLR agonism. These effects demonstrate its activity in modulating the inflammasome pathway. Specific IC50 values are not provided in the available sources.
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| ln Vivo |
Specific in vivo activity data for BC-1471 are not provided in the available sources. As a STAMBP inhibitor with effects on IL-1β release, it could have potential in inflammatory diseases. However, no specific in vivo studies are described.
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| Enzyme Assay |
A cell-free assay for BC-1471 would involve measuring its inhibition of STAMBP deubiquitinase activity. In this assay, recombinant STAMBP is incubated with a ubiquitinated substrate in the presence of varying concentrations of the compound. The removal of ubiquitin from the substrate is measured, and the IC50 is calculated. Specific assay conditions are not detailed.
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| Cell Assay |
Cellular assays for BC-1471 typically involve assessing its effects on NALP7 levels and IL-1β release. Cells are treated with the compound and stimulated with a TLR agonist. The levels of NALP7 and IL-1β in the cell culture supernatant are measured. BC-1471 has been shown to decrease NALP7 levels and suppress IL-1β release.
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| Animal Protocol |
In vivo animal experiments for BC-1471 are not described in the available sources. As a research compound with anti-inflammatory potential, it could be evaluated in animal models of inflammation. However, no specific protocols are provided.
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| ADME/Pharmacokinetics |
BC-1471 is a small molecule with a molecular weight of 508.63. Specific pharmacokinetic properties, such as half-life and bioavailability, are not provided in the available sources. The compound is intended for research use.
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| Toxicity/Toxicokinetics |
Toxicity data for BC-1471 are not provided in the available sources. As a research compound, it is intended for research use only and not for human consumption.
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| References | |
| Additional Infomation |
2-[[6-(4-morpholino)-4-oxo-3-(2-phenylethyl)-2-quinazolino]thio]-N-(2-oxacyclopentylmethyl)acetamide is a member of the quinazolino group of compounds.
BC-1471 (CAS: 896683-84-4) is a selective inhibitor of the deubiquitinase STAMBP. It decreases NALP7 protein levels and suppresses IL-1β release after TLR agonism. Its molecular formula is C27H32N4O4S and its molecular weight is 508.63. It is not an approved drug and is strictly for research purposes. |
| Molecular Formula |
C27H32N4O4S
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|---|---|
| Molecular Weight |
508.63
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| Exact Mass |
508.214
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| CAS # |
896683-84-4
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| Related CAS # |
896683-84-4 (racemate);
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| PubChem CID |
16193537
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
784
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NCC1CCCO1)(=O)CSC1N(CCC2=CC=CC=C2)C(=O)C2=C(N=1)C=CC(N1CCOCC1)=C2
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| InChi Key |
GJKRCJKXXVVAMV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H32N4O4S/c32-25(28-18-22-7-4-14-35-22)19-36-27-29-24-9-8-21(30-12-15-34-16-13-30)17-23(24)26(33)31(27)11-10-20-5-2-1-3-6-20/h1-3,5-6,8-9,17,22H,4,7,10-16,18-19H2,(H,28,32)
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| Chemical Name |
2-[6-morpholin-4-yl-4-oxo-3-(2-phenylethyl)quinazolin-2-yl]sulfanyl-N-(oxolan-2-ylmethyl)acetamide
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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 (~98.30 mM)
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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 | 1.9661 mL | 9.8303 mL | 19.6607 mL | |
| 5 mM | 0.3932 mL | 1.9661 mL | 3.9321 mL | |
| 10 mM | 0.1966 mL | 0.9830 mL | 1.9661 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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