GSK 1562590 hydrochlorideHigh affinity, selective urotensin II (UT) receptor antagonist CAS# 1003878-07-6 |
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Quality Control & MSDS
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| Cas No. | 1003878-07-6 | SDF | Download SDF |
| PubChem ID | 46909864 | Appearance | Powder |
| Formula | C30H31Cl3N4O4 | M.Wt | 617.95 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | 3-[4-[(1R)-1-[[2-(6,7-dichloro-3-oxo-1,4-benzoxazin-4-yl)acetyl]-methylamino]-2-pyrrolidin-1-ylethyl]phenyl]benzamide;hydrochloride | ||
| SMILES | CN(C(CN1CCCC1)C2=CC=C(C=C2)C3=CC(=CC=C3)C(=O)N)C(=O)CN4C(=O)COC5=CC(=C(C=C54)Cl)Cl.Cl | ||
| Standard InChIKey | XTVXEMMIPYMBLL-SNYZSRNZSA-N | ||
| Standard InChI | InChI=1S/C30H30Cl2N4O4.ClH/c1-34(28(37)17-36-25-14-23(31)24(32)15-27(25)40-18-29(36)38)26(16-35-11-2-3-12-35)20-9-7-19(8-10-20)21-5-4-6-22(13-21)30(33)39;/h4-10,13-15,26H,2-3,11-12,16-18H2,1H3,(H2,33,39);1H/t26-;/m0./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. |
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| 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. |
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| 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. | ||
| Description | High affinity and selective urotensin II (UT) receptor antagonist (pKi values are 9.14, 9.28, 9.34, 9.64 and 9.66 at monkey, human, mouse, cat and rat recombinant receptors respectively). Exhibits selectivity for UT receptors over a range of GPCRs, ion channels, enzymes and neurotransmitter transporters. Supresses human urotensin-II (hU-II)-induced contraction of isolated rat aorta in vitro and ex vivo. Inhibits the hU-II-induced increase in mean blood pressure in vivo. Orally active. |
GSK 1562590 hydrochloride Dilution Calculator
GSK 1562590 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.6183 mL | 8.0913 mL | 16.1825 mL | 32.3651 mL | 40.4563 mL |
| 5 mM | 0.3237 mL | 1.6183 mL | 3.2365 mL | 6.473 mL | 8.0913 mL |
| 10 mM | 0.1618 mL | 0.8091 mL | 1.6183 mL | 3.2365 mL | 4.0456 mL |
| 50 mM | 0.0324 mL | 0.1618 mL | 0.3237 mL | 0.6473 mL | 0.8091 mL |
| 100 mM | 0.0162 mL | 0.0809 mL | 0.1618 mL | 0.3237 mL | 0.4046 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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GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo.[Pubmed:20718751]
Br J Pharmacol. 2010 Sep;161(1):207-28.
BACKGROUND AND PURPOSE: Recently identified antagonists of the urotensin-II (U-II) receptor (UT) are of limited utility for investigating the (patho)physiological role of U-II due to poor potency and limited selectivity and/or intrinsic activity. EXPERIMENTAL APPROACH: The pharmacological properties of two novel UT antagonists, GSK1440115 and GSK1562590, were compared using multiple bioassays. KEY RESULTS: GSK1440115 (pK(i)= 7.34-8.64 across species) and GSK1562590 (pK(i)= 9.14-9.66 across species) are high affinity ligands of mammalian recombinant (mouse, rat, cat, monkey, human) and native (SJRH30 cells) UT. Both compounds exhibited >100-fold selectivity for UT versus 87 distinct mammalian GPCR, enzyme, ion channel and neurotransmitter uptake targets. GSK1440115 showed competitive antagonism at UT in arteries from all species tested (pA(2)= 5.59-7.71). In contrast, GSK1562590 was an insurmountable UT antagonist in rat, cat and hUT transgenic mouse arteries (pK(b)= 8.93-10.12 across species), but a competitive antagonist in monkey arteries (pK(b)= 8.87-8.93). Likewise, GSK1562590 inhibited the hU-II-induced systemic pressor response in anaesthetized cats at a dose 10-fold lower than that of GSK1440115. The antagonistic effects of GSK1440115, but not GSK1562590, could be reversed by washout in rat isolated aorta. In ex vivo studies, GSK1562590 inhibited hU-II-induced contraction of rat aorta for at least 24 h following dosing. Dissociation of GSK1562590 binding was considerably slower at rat than monkey UT. CONCLUSIONS AND IMPLICATIONS: Whereas both GSK1440115 and GSK1562590 represent high-affinity/selective UT antagonists suitable for assessing the (patho)physiological role of U-II, only GSK1562590 exhibited sustained UT residence time and improved preclinical efficacy in vivo.
