SSR 146977 hydrochloridePotent and selective NK3 antagonist CAS# 264618-38-4 |
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Quality Control & MSDS
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| Cas No. | 264618-38-4 | SDF | Download SDF |
| PubChem ID | 90488827 | Appearance | Powder |
| Formula | C35H43Cl3N4O2 | M.Wt | 658.11 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol | ||
| Chemical Name | 3-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-1,1-dimethylurea;hydrochloride | ||
| SMILES | CN(C)C(=O)NC1(CCN(CC1)CCCC2(CCCN(C2)C(=O)C3=CC=CC=C3)C4=CC(=C(C=C4)Cl)Cl)C5=CC=CC=C5.Cl | ||
| Standard InChIKey | HYPKKQPFHSNZBY-GXUZKUJRSA-N | ||
| Standard InChI | InChI=1S/C35H42Cl2N4O2.ClH/c1-39(2)33(43)38-35(28-13-7-4-8-14-28)19-23-40(24-20-35)21-9-17-34(29-15-16-30(36)31(37)25-29)18-10-22-41(26-34)32(42)27-11-5-3-6-12-27;/h3-8,11-16,25H,9-10,17-24,26H2,1-2H3,(H,38,43);1H/t34-;/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 and selective NK3 receptor antagonist (Ki values are 0.26 and 19.3 nM in CHO cells expressing the human NK3 and NK2 receptor respectively). Also inhibits senktide-induced inositol monophosphate formation and intracellular calcium mobilization (IC50 = 10 nM). |
SSR 146977 hydrochloride Dilution Calculator
SSR 146977 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.5195 mL | 7.5975 mL | 15.195 mL | 30.3901 mL | 37.9876 mL |
| 5 mM | 0.3039 mL | 1.5195 mL | 3.039 mL | 6.078 mL | 7.5975 mL |
| 10 mM | 0.152 mL | 0.7598 mL | 1.5195 mL | 3.039 mL | 3.7988 mL |
| 50 mM | 0.0304 mL | 0.152 mL | 0.3039 mL | 0.6078 mL | 0.7598 mL |
| 100 mM | 0.0152 mL | 0.076 mL | 0.152 mL | 0.3039 mL | 0.3799 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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Biochemical and pharmacological activities of SSR 146977, a new potent nonpeptide tachykinin NK3 receptor antagonist.[Pubmed:12056557]
Can J Physiol Pharmacol. 2002 May;80(5):482-8.
SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. In Chinese hamster ovary cells expressing the human tachykinin NK3 receptor, SSR 146977 inhibited the binding of radioactive neurokinin B to NK3 receptors (Ki = 0.26 nM), senktide (10 nM) induced inositol monophosphate formation (IC50 = 7.8-13 nM), and intracellular calcium mobilization (IC50 = 10 nM). It antagonized [MePhe7]neurokinin B induced contractions of guinea pig ileum (pA2 = 9.07). Senktide (30 nM) induced firing rate increase of noradrenergic neurons in the guinea pig locus coeruleus and dopaminergic neurons in the guinea pig substantia nigra was also blocked by SSR 146977 (50 and 100 nM, respectively). In vivo, in the respiratory system, SSR 146977 inhibited bronchial hyperresponsiveness to acetylcholine, bronchial microvascular permeability hypersensitivity to histamine (doses of 0.1-1 mg/kg i.p.), and cough (doses of 0.03-1 mg/kg i.p.) provoked by citric acid in guinea pigs. In the central nervous system, SSR 146977 inhibited turning behaviour (ID50 = 0.2 mg/kg i.p. and 0.4 mg/kg p.o.) and prevented the decrease of locomotor activity (10 and 30 mg/kg i.p) mediated by the stimulation of NK3 receptors in gerbils. In guinea pigs, SSR 146977 antagonized senktide-induced acetylcholine release in the hippocampus (0.3 and 1 mg/kg i.p) and norepinephrine release in the prefrontal cortex (0.3 mg/kg i.p.). It also prevented haloperidol-induced increase of the number of spontaneously active dopamine A10 neurons (1 and 3 mg/kg i.p.).
