SB 772077B dihydrochloridePotent Rho-kinase inhibitor; vasodilator CAS# 607373-46-6 |
- SB 216763
Catalog No.:BCC3650
CAS No.:280744-09-4
Quality Control & MSDS
3D structure
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| Cas No. | 607373-46-6 | SDF | Download SDF |
| PubChem ID | 69157798 | Appearance | Powder |
| Formula | C15H20Cl2N8O2 | M.Wt | 415.28 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water and to 100 mM in DMSO | ||
| Chemical Name | [2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethylimidazo[4,5-c]pyridin-7-yl]-[(3S)-3-aminopyrrolidin-1-yl]methanone;dihydrochloride | ||
| SMILES | CCN1C2=C(C=NC=C2C(=O)N3CCC(C3)N)N=C1C4=NON=C4N.Cl.Cl | ||
| Standard InChIKey | HSROPTGRSYJPJY-JZGIKJSDSA-N | ||
| Standard InChI | InChI=1S/C15H18N8O2.2ClH/c1-2-23-12-9(15(24)22-4-3-8(16)7-22)5-18-6-10(12)19-14(23)11-13(17)21-25-20-11;;/h5-6,8H,2-4,7,16H2,1H3,(H2,17,21);2*1H/t8-;;/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 | Potent Rho-kinase (ROCK) inhibitor (IC50 value of approximately 5.6 nM at recombinant human ROCK1 and 2). Decreases pulmonary and systemic arterial blood pressures and increases cardiac output. Exhibits vasodilator activity that is more potent than Y-27632 or Fasudil. |
SB 772077B dihydrochloride Dilution Calculator
SB 772077B dihydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.408 mL | 12.0401 mL | 24.0801 mL | 48.1603 mL | 60.2003 mL |
| 5 mM | 0.4816 mL | 2.408 mL | 4.816 mL | 9.6321 mL | 12.0401 mL |
| 10 mM | 0.2408 mL | 1.204 mL | 2.408 mL | 4.816 mL | 6.02 mL |
| 50 mM | 0.0482 mL | 0.2408 mL | 0.4816 mL | 0.9632 mL | 1.204 mL |
| 100 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.4816 mL | 0.602 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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SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4 -biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain.[Pubmed:16846620]
Neuropharmacology. 2006 Sep;51(3):566-77.
This study utilised the selective 5-ht(5A) receptor antagonist, SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4 -biphenylyl)methyl]propanamide dihydrochloride), to investigate 5-ht5A receptor function in guinea pig brain. SB-699551-A competitively antagonised 5-HT-stimulated [35S]GTPgammaS binding to membranes from human embryonic kidney (HEK293) cells transiently expressing the guinea pig 5-ht5A receptor (pA2 8.1+/-0.1) and displayed 100-fold selectivity versus the serotonin transporter and those 5-HT receptor subtypes (5-HT(1A/B/D), 5-HT2A/C and 5-HT7) reported to modulate central 5-HT neurotransmission in the guinea pig. In guinea pig dorsal raphe slices, SB-699551-A (1 microM) did not alter neuronal firing per se but attenuated the 5-CT-induced depression in serotonergic neuronal firing in a subpopulation of cells insensitive to the 5-HT1A receptor-selective antagonist WAY-100635 (100 nM). In contrast, SB-699551-A (100 or 300 nM) failed to affect both electrically-evoked 5-HT release and 5-CT-induced inhibition of evoked release measured using fast cyclic voltammetry in vitro. SB-699551-A (0.3, 1 and 3 mg/kg s.c.) did not modulate extracellular levels of 5-HT in the guinea pig frontal cortex in vivo. However, when administered in combination with WAY-100635 (0.3 mg/kg s.c.), SB-699551-A (0.3, 1 or 3 mg/kg s.c.) produced a significant increase in extracellular 5-HT levels. These studies provide evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain.
