| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
MIF (Kd = 68.6 nM)
Macrophage migration inhibitory factor (MIF), a ubiquitous protein released by ischemic heart tissue. BTZO-1 binds to MIF with a Kd of 68.6 nM, and the N-terminal Pro1 of MIF is necessary for this interaction. BTZO-1 activates the GST Ya gene ARE by interacting with MIF. |
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| ln Vitro |
BTZO-1 (0-330 nM; 24 hours) suppressed serum deprivation-induced cardiomyocyte death in a dose-dependent manner, the minimum effective concentration (MEC1.5), or the concentration of a sample required to give a 50% increase in cell viability, is 16 nM[1].
In cardiomyocytes, BTZO-1 (0.37 μM; 21 hours) increases the levels of the mRNA and protein for GST Ya and HO-1[1]. BTZO-1 binds to MIF with a Kd of 68.6 nM. It activates ARE-mediated gene expression and induces expression of cytoprotective proteins such as heme oxygenase-1 (HO-1). In cardiomyocytes, BTZO-1 (0.37 μM; 21 hours) increases the levels of mRNA and protein for GST Ya and HO-1. BTZO-1 (0-330 nM; 24 hours) suppresses serum deprivation-induced cardiomyocyte death in a dose-dependent manner with a minimum effective concentration (MEC1.5) of 16 nM. |
| ln Vivo |
In vivo activity data for BTZO-1 is limited as the compound is primarily used as a research tool for studying cardioprotection and oxidative stress. The compound's ability to bind MIF and activate ARE-mediated gene expression suggests potential therapeutic applications in cardiovascular diseases where oxidative stress plays a key role.
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| Enzyme Assay |
In vitro enzyme assays for BTZO-1 involve measuring its binding affinity for MIF using surface plasmon resonance or other binding assays. MIF protein is immobilized, and increasing concentrations of BTZO-1 are passed over the surface. The binding affinity (Kd = 68.6 nM) is determined from the binding kinetics. Activation of ARE-mediated gene expression is measured using reporter gene assays.
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| Cell Assay |
In vitro cellular assays for BTZO-1 involve treating cardiomyocytes or other cell types with the compound and measuring cell viability, oxidative stress markers, and gene expression. Cells are treated with various concentrations of BTZO-1, and cardiomyocyte death is assessed under serum deprivation conditions. Expression of GST Ya and HO-1 is measured by qPCR or Western blot.
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| Animal Protocol |
In vivo animal studies for BTZO-1 are limited as the compound is primarily used as a research tool for in vitro applications. The compound's cardioprotective effects could be studied in animal models of myocardial ischemia or oxidative stress. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic properties.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BTZO-1 is limited. The compound has a molecular weight of 240.28 and a molecular formula of C13H8N2OS. It is soluble in DMSO (approximately 10 mg/mL) and ethanol (approximately 4 mg/mL). BTZO-1 should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 6 months.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of BTZO-1 are limited. The compound is a cardioprotective agent that activates ARE-mediated gene expression and suppresses oxidative stress-induced cardiomyocyte apoptosis. Comprehensive toxicological evaluation is needed before clinical development. The compound's mechanism of action suggests a favorable safety profile.
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| References | |
| Additional Infomation |
BTZO-1 is a cardioprotective compound that binds to Macrophage migration inhibitory factor (MIF) with a Kd of 68.6 nM and activates the glutathione S-transferase Ya subunit (GST Ya) gene's antioxidant response element (ARE). It induces expression of cytoprotective proteins such as HO-1 and suppresses oxidative stress-induced cardiomyocyte apoptosis. BTZO-1 is a valuable research tool for studying cardioprotection and oxidative stress.
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| Molecular Formula |
C13H8N2OS
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| Molecular Weight |
240.28042
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| Exact Mass |
240.036
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| Elemental Analysis |
C, 64.98; H, 3.36; N, 11.66; O, 6.66; S, 13.34
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| CAS # |
99420-15-2
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| Related CAS # |
99420-15-2
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| PubChem CID |
9837640
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| Appearance |
White to off-white solid powder
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| LogP |
2.718
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
342
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C(=O)N=C(S2)C3=CC=CC=N3
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| InChi Key |
GBAKVEWPYUIGHN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8N2OS/c16-12-9-5-1-2-7-11(9)17-13(15-12)10-6-3-4-8-14-10/h1-8H
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| Chemical Name |
2-pyridin-2-yl-1,3-benzothiazin-4-one
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| Synonyms |
BTZO-1; BTZO1; BTZO 1
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| HS Tariff Code |
2934.99.03.00
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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: ~10 mg/mL (~41.6 mM)
Ethanol: ~4 mg/mL (~16.7 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 | 4.1618 mL | 20.8091 mL | 41.6181 mL | |
| 5 mM | 0.8324 mL | 4.1618 mL | 8.3236 mL | |
| 10 mM | 0.4162 mL | 2.0809 mL | 4.1618 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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