Y-33075

CAS# 199433-58-4

Y-33075

Catalog No. BCC2064----Order now to get a substantial discount!

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Chemical structure

Y-33075

3D structure

Chemical Properties of Y-33075

Cas No. 199433-58-4 SDF Download SDF
PubChem ID 9810884 Appearance Powder
Formula C16H16N4O M.Wt 280.33
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Y 39983
Solubility DMSO : 50 mg/mL (178.37 mM; Need ultrasonic and warming)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 4-[(1R)-1-aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide
SMILES CC(C1=CC=C(C=C1)C(=O)NC2=C3C=CNC3=NC=C2)N
Standard InChIKey JTVBXQAYBIJXRP-SNVBAGLBSA-N
Standard InChI InChI=1S/C16H16N4O/c1-10(17)11-2-4-12(5-3-11)16(21)20-14-7-9-19-15-13(14)6-8-18-15/h2-10H,17H2,1H3,(H2,18,19,20,21)/t10-/m1/s1
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 Y-33075

DescriptionY-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.In Vitro:Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII more potently than Y-27632, and the IC50s of Y-27632 and Y-33075 for PKC are 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII are 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-33075 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII is 236 and 225 times those for ROCK, respectively[1]. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983[2]. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions. Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution[3].In Vivo:In rabbits, Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration. In monkeys, Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration[1]. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats[2].

References:
[1]. Hideki Tokushige, et al. Effects of Topical Administration of Y-39983, a Selective Rho-Associated Protein Kinase Inhibitor, on Ocular Tissues in Rabbits and Monkeys Invest. Ophthalmol. Vis. Sci. July 2007 vol. 48no. 7 3216-3222 [2]. Tokushige H, et al. Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats. Curr Eye Res. 2011 Oct;36(10):964-70. [3]. Watabe H, et al. Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries.Jpn J Ophthalmol. 2011 Jul;55(4):411-7. Epub 2011 Jun 11.

Protocol

Kinase Assay [1]
Recombinant ROCK (ROK α/ROCK II), purified protein kinase C (PKC: mixture of α, β, γ isoforms), and recombinant calmodulin-dependent protein kinase II (CaMK II) are used in the assay. ROCK (0.2 U/mL) is incubated with 1 μM [γ-32P] ATP and 10 μg/mL histone as substrates in the absence or presence of various concentrations of Y-27632, Y-33075, or staurosporine at room temperature for 20 minutes in 20 mM MOPS (3-(N-morpholino)propanesulfonic acid) buffer (pH 7.2) containing 0.1 mg/mL bovine serum albumin (BSA), 5 mM dithiothreitol [DTT], 10 mM β-glycerophosphate, 50 μM Na3VO4, and 10 mM MgCl2 in a total volume of 100 μL. PKC (10 ng/mL) is incubated with 1 μM [γ-32P] ATP and 20 μM PKC substrate in the absence or presence of various concentrations of Y-27632, Y-33075, or staurosporine at room temperature for 30 minutes in 20 mM MOPS buffer (pH 7.5) containing 0.1 mg/mL BSA, 10 mM DTT, 10 mM β-glycerophosphate, 50 μM Na3VO4, 2 mM CaCl2, 20 μg/mL phosphatidyl-l-serine, and 10 mM MgCl2 in a total volume of 100 μL. CaMK II (125 U/mL) is incubated with 1 μM [γ-32P] ATP, 10 μM calmodulin, and 20 μM CaMK II substrate, in the absence or presence of various concentrations of Y-27632, Y-33075, or staurosporine at room temperature for 30 minutes in 20 mM MOPS buffer (pH 7.5) containing 0.2 mg/mL BSA, 0.5 mM DTT, 0.1 mM β-glycerophosphate, 50 μM Na3VO4, 1 mM CaCl2, and 5 mM MgCl2 in a total volume of 100 μL. Incubation is terminated by the addition of 100 μL of 0.7% phosphoric acid. A 160 μL portion of the mixture is transferred to Multiscreen-PH plate. A positively charged phosphocellulose filter absorbs the substrate that binds 32P. The filter is washed with 300 μL of 0.5% phosphoric acid and then twice with purified water and then dried. The radioactivity of the dried filter is measured with a liquid scintillation counter. Results are presented as 50% inhibitory concentrations and 95% confidence intervals (CIs)[1].

Cell Assay [2]
In brief, retinal cell suspensions are obtained from dissected retinas of Wistar rats by papain treatment. Retinal ganglion cells (RGCs) are purified by the panning method using anti-rat CD11 antibody for removal of microglia cells and anti-rat Thy-1 antibody for isolation of ganglion cells. The purified RGCs (5000 cells/plate) are seeded into 24-well plates coated by 50 μg/mL of poly-l-lysine and 2 μg/mL of merosin, and are cultured in serum-free neurobasal medium supplemented with 2% B27 supplement, 50 ng/mL BDNF, 50 ng/mL CNTF, 5 μM forskolin, and 1 mM glutamine under a 95% air-5% CO2 atmosphere at 37°C. After completion of 24-hour cultivation, RGCs are cultured in medium with or without 10 μM Y-33075 as the final concentration for 24 hours and morphologically observed by phase-contrast microscopy. The concentration used is determined based on the effect of Y-33075 on trabecular meshwork contraction in vitro. Since this study is conducted in order to confirm whether Y-33075 has a potential of effect on axonal regeneration of RGCs, the effect is unquantitateively evaluated[2].

Animal Administration [2]
In brief, SD rats is anesthetized with an intraperitoneal injection of sodium pentobarbital (0.4 mg/kg body weight), and the optic nerve of one eye is transected 4 to 6 mm posterior to the eyeball, taking care to avoid injury to the ophthalmic artery. The anterior branch of the sciatic nerve is excised and sutured autologously to the optic nerve stump with nylon sutures. The other end of the graft is sutured to the temporalis muscle. A small piece (3 mm × 3 mm) of gelatin sponge soaked with 10 μM Y-33075 or saline as a control is implanted in the space behind the optic stump after optic nerve transection in intact animals. Five μL of 0.12 mM or 1.2 mM Y-33075 solution or saline is administered into the vitreous body to final concentrations of 10 μM or 100 μM, respectively. The concentrations of Y-33075 used is determined as 10 μM that is effective in the in vitro study on axonal regeneration of RGCs, and also as 100 μM in order to confirm the dose response of Y-33075. Six weeks after surgery, rats is anesthetized with an intraperitoneal injection of sodium pentobarbital (0.4 mg/kg body weight), and 4-Di-10ASP is embedded in the transplanted sciatic nerve to retrogradely label RGCs with axonal regeneration into the sciatic nerve. Three days after dye embedding, rats is euthanized and the eyes is enucleated for preparation of retinal flat-mounts. The posterior eyecup is then separated from the vitreous body and postfixed with 4% paraformaldehyde solution in phosphate buffer for around 1 hour at room temperature. Fluorescence micrographs of the labeled cells is imported using a fluorescence microscope connected to a computer. Labeled cells is counted using image analysis software. As a normal group, the subsequent procedure for retrograde labeling with 4-Di-10ASP is performed without grafting sciatic nerve and administering the test drug. Statistical analysis is performed using logarithmically transformed values due to differences in variance among the groups. The statistical significance of differences between the normal and saline groups and the saline and Y-33075 groups is examined by t-test (onesided) and William’s test (one-sided). Findings of p < 0.05 is considered significant[2].

References:
[1]. Hideki Tokushige, et al. Effects of Topical Administration of Y-39983, a Selective Rho-Associated Protein Kinase Inhibitor, on Ocular Tissues in Rabbits and Monkeys Invest. Ophthalmol. Vis. Sci. July 2007 vol. 48no. 7 3216-3222 [2]. Tokushige H, et al. Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats. Curr Eye Res. 2011 Oct;36(10):964-70. [3]. Watabe H, et al. Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries.Jpn J Ophthalmol. 2011 Jul;55(4):411-7. Epub 2011 Jun 11.

Y-33075 Dilution Calculator

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Preparing Stock Solutions of Y-33075

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.5672 mL 17.8361 mL 35.6722 mL 71.3445 mL 89.1806 mL
5 mM 0.7134 mL 3.5672 mL 7.1344 mL 14.2689 mL 17.8361 mL
10 mM 0.3567 mL 1.7836 mL 3.5672 mL 7.1344 mL 8.9181 mL
50 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.4269 mL 1.7836 mL
100 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.7134 mL 0.8918 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 Y-33075

Y-33075 is ROCK (Rho-associated coiled coil-forming protein kinase) inhibitor.

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Description

Y-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.

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