| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Inducible nitric oxide synthase (iNOS). BYK191023 is a potent and selective inhibitor of iNOS with IC50 values of 86 nM for iNOS, 17 μM for nNOS, and 162 μM for eNOS. It is an L-arginine competitive inhibitor and acts in a NADPH- and time-dependent manner.
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| ln Vitro |
BYK191023 inhibits iNOS with an IC50 of 86 nM, showing >20-fold selectivity over nNOS (IC50 = 17 μM) and eNOS (IC50 = 162 μM). It is an L-arginine competitive inhibitor and acts in a NADPH- and time-dependent manner. The compound interacts with the catalytic center of the enzyme.
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| ln Vivo |
In vivo activity data for BYK191023 is limited as the compound is primarily used as a research tool for studying iNOS function. The compound's potent and selective iNOS inhibition makes it a valuable tool for studying the role of iNOS in inflammation, immune responses, and various diseases. Further in vivo studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme assays for BYK191023 involve measuring its inhibition of iNOS, nNOS, or eNOS activity. NOS enzymes are incubated with L-arginine, NADPH, and various concentrations of BYK191023. Nitric oxide production is measured by detecting nitrite using the Griess reaction or by measuring the conversion of radiolabeled L-arginine to citrulline. IC50 values are determined from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for BYK191023 involve treating cells that express iNOS (such as macrophages) with the compound and measuring nitric oxide production. Cells are stimulated with LPS or cytokines to induce iNOS expression, treated with various concentrations of BYK191023, and nitric oxide production is measured by detecting nitrite in the culture medium. The compound's ability to inhibit iNOS in cellular contexts is assessed.
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| Animal Protocol |
In vivo animal studies for BYK191023 typically involve administration to rodent models of inflammation, sepsis, or other conditions where iNOS plays a role. Efficacy is assessed by measuring nitric oxide levels, inflammatory markers, or disease severity. The compound's potent and selective iNOS inhibition makes it a valuable tool for studying iNOS function in vivo.
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| ADME/Pharmacokinetics |
BYK191023 Dihydrochloride has a molecular weight of 327.21 and a molecular formula of C14H16Cl2N4O. It is an imidazopyridine-class, L-arginine competitive inhibitor of iNOS. The compound is soluble in water (32.72 mg/mL). Further pharmacokinetic studies are needed to fully characterize its profile.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of BYK191023 are limited. The compound is a potent and selective inhibitor of iNOS with >20-fold selectivity over nNOS and eNOS. This selectivity may contribute to a favorable safety profile. Comprehensive toxicological evaluation is needed before clinical development. The compound should be handled with appropriate safety precautions.
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| References |
:Mol. Pharmacol.69(1),328-337(2006).
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| Additional Infomation |
BYK191023 Dihydrochloride is a potent, highly selective, L-arginine competitive inhibitor of inducible nitric oxide synthase (iNOS) with an IC50 of 86 nM for iNOS, compared to 17 μM for nNOS and 162 μM for eNOS. It is an imidazopyridine-class inhibitor that acts in a NADPH- and time-dependent manner. BYK191023 is a valuable research tool for studying iNOS function in inflammation and immune responses.
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| Molecular Formula |
C14H16CL2N4O
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|---|---|
| Molecular Weight |
327.2
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| Exact Mass |
326.07
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| Elemental Analysis |
C, 51.39; H, 4.93; Cl, 21.67; N, 17.12; O, 4.89
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| CAS # |
1216722-25-6
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| Related CAS # |
1216722-25-6 (HCl);608880-48-4;
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| PubChem CID |
56972216
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
289
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=NC(=C1)CCC2=NC3=C(N=CC=C3)N2.Cl.Cl
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| InChi Key |
ZVNITETZYOKESF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14N4O.2ClH/c1-19-11-6-8-15-10(9-11)4-5-13-17-12-3-2-7-16-14(12)18-13;;/h2-3,6-9H,4-5H2,1H3,(H,16,17,18);2*1H
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| Chemical Name |
2-[2-(4-methoxypyridin-2-yl)ethyl]-1H-imidazo[4,5-b]pyridine;dihydrochloride
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| Synonyms |
BYK 191023 Dihydrochloride BYK-191023 Dihydrochloride BYK191023 Dihydrochloride
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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 | 3.0562 mL | 15.2812 mL | 30.5623 mL | |
| 5 mM | 0.6112 mL | 3.0562 mL | 6.1125 mL | |
| 10 mM | 0.3056 mL | 1.5281 mL | 3.0562 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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