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BYK 191023 dihydrochloride

INOS inhibitor,potent and selective CAS# 1216722-25-6

BYK 191023 dihydrochloride

Catalog No. BCC7506----Order now to get a substantial discount!

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BYK 191023 dihydrochloride: 5mg $104 In Stock
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Chemical structure

BYK 191023 dihydrochloride

3D structure

Chemical Properties of BYK 191023 dihydrochloride

Cas No. 1216722-25-6 SDF Download SDF
PubChem ID 56972216 Appearance Powder
Formula C14H16Cl2N4O M.Wt 327.21
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water
Chemical Name 2-[2-(4-methoxypyridin-2-yl)ethyl]-1H-imidazo[4,5-b]pyridine;dihydrochloride
SMILES COC1=CC(=NC=C1)CCC2=NC3=C(N2)C=CC=N3.Cl.Cl
Standard InChIKey ZVNITETZYOKESF-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of BYK 191023 dihydrochloride

DescriptionPotent and selective inhibitor of inducible nitric oxide synthase (iNOS) (IC50 values are 86, 17000, 162000 nM for iNOS, nNOS and eNOS respectively). Acts in an NADPH- and time-dependent manner. Active in vivo, reverses pathological hypotension in the rodent endotoxin model.

BYK 191023 dihydrochloride Dilution Calculator

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BYK 191023 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of BYK 191023 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.0561 mL 15.2807 mL 30.5614 mL 61.1228 mL 76.4035 mL
5 mM 0.6112 mL 3.0561 mL 6.1123 mL 12.2246 mL 15.2807 mL
10 mM 0.3056 mL 1.5281 mL 3.0561 mL 6.1123 mL 7.6404 mL
50 mM 0.0611 mL 0.3056 mL 0.6112 mL 1.2225 mL 1.5281 mL
100 mM 0.0306 mL 0.1528 mL 0.3056 mL 0.6112 mL 0.764 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on BYK 191023 dihydrochloride

IC50: 86 nM for iNOS

NO synthases are enzymes responsible for the generation of nitric oxide from the amino acid L-arginine. Once expressed the inducible NO synthase (iNOS) is active and produces μM concentrations of NO over longer periods. The iNOS expression is stimulated in various cells by proinflammatory signals and is involved in immune defense. BYK191023 is a selective inhibitor of the inducible nitric-oxide synthase (NOS).

In vitro: BYK191023 showed half-maximal inhibition of crudely purified human inducible, neuronal, and endothelial NO synthases at 86 nM, 17 μM, and 162 μM, respectively. The ihibition of inducible NO synthase was competitive with L-arginine, pointing to an interaction of BYK191023 with the catalytic center of the enzyme. BYK191023 did not show any toxicity in various rodent and human cell lines up to high micromolar concentrations [1].

In vivo: Authors tested the in vivo potency of BYK191023 in rat models of lipopolysaccharide-induced systemic inflammation. Delayed administration of BYK191023 suppressed the LPS-induced increase in plasma nitrate/nitrite (NOx) levels with an ED50 of 14.9 μmol/kg/h dose-dependently. In a systemic hypotension model following high-dose lipopolysaccharide challenge, curative administration of BYK191023 at a dose that inhibited 83% of the Nox increase completely prevented the gradual decrease in mean arterial blood pressure observed in control animals [2].

Clinical trial: Up to now, BYK191023 is still in the preclinical development stage.

Reference:
[1] Andreas Strub, Wolf-Rudiger Ulrich, Christian Hesslinger, Manfrid Eltze, Thomas Fuch?, Jochen Strassner, Susanne Strand, Martin D.  Lehner, and Rainer Boer. The Novel Imidazopyridine 2-[2-(4-Methoxy-pyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine (BYK191023) Is a Highly Selective Inhibitor of the Inducible Nitric-Oxide Synthase. Mol Pharmacol 69:328–337, 2006
[2] Martin D.  Lehner, Degenhard Marx, Rainer Boer, Andreas Strub, Christian Hesslinger, Manfrid Eltze, Wolf-Rudiger Ulrich, Frank Schwoebel, Ralph Theo Schermuly, and Johannes Barsig. In Vivo Characterization of the Novel Imidazopyridine BYK191023 [2-[2-(4-Methoxy-pyridin-2-yl)-ethyl]-3Himidazo[4,5-b]pyridine], a Potent and Highly Selective Inhibitor of Inducible Nitric-Oxide Synthase. JPET 317:181–187, 2006

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References on BYK 191023 dihydrochloride

In vivo characterization of the novel imidazopyridine BYK191023 [2-[2-(4-methoxy-pyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine], a potent and highly selective inhibitor of inducible nitric-oxide synthase.[Pubmed:16368897]

J Pharmacol Exp Ther. 2006 Apr;317(1):181-7.

Excessive release of nitric oxide from inducible nitric-oxide synthase (iNOS) has been postulated to contribute to pathology in a number of inflammatory diseases. We recently identified imidazopyridine derivatives as a novel class of potent nitricoxide synthase inhibitors with high selectivity for the inducible isoform. In the present study, we tested the in vivo potency of BYK191023 [2-[2-(4-methoxy-pyridin-2-yl)-ethyl]-3H-imidazo-[4,5-b]pyridine], a selected member of this inhibitor class, in three different rat models of lipopolysaccharide-induced systemic inflammation. Delayed administration of BYK191023 dose-dependently suppressed the lipopolysaccharide-induced increase in plasma nitrate/nitrite (NO(x)) levels with an ED(50) of 14.9 micromol/kg/h. In a model of systemic hypotension following high-dose lipopolysaccharide challenge, curative administration of BYK191023 at a dose that inhibited 83% of the NO(x) increase completely prevented the gradual decrease in mean arterial blood pressure observed in vehicle-treated control animals. The vasopressor effect was specific for endotoxemic animals since BYK191023 did not affect blood pressure in saline-challenged controls. In addition, in a model of lipopolysaccharide-induced vascular hyporesponsiveness, BYK191023 infusion partially restored normal blood pressure responses to norepinephrine and sodium nitroprusside via an l-arginine competitive mechanism. Taken together, BYK191023 is a member of a novel class of highly isoform-selective iNOS inhibitors with promising in vivo activity suitable for mechanistic studies on the role of selective iNOS inhibition as well as clinical development.

Description

Potent and selective inhibitor of iNOS

Keywords:

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