SR 142948Highly potent NT receptor antagonist CAS# 184162-64-9 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 184162-64-9 | SDF | Download SDF |
| PubChem ID | 5311451 | Appearance | Powder |
| Formula | C39H51N5O6 | M.Wt | 685.86 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 75 mM in DMSO and to 25 mM in water | ||
| Chemical Name | 2-[[5-(2,6-dimethoxyphenyl)-1-[4-[3-(dimethylamino)propyl-methylcarbamoyl]-2-propan-2-ylphenyl]pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid | ||
| SMILES | CC(C)C1=C(C=CC(=C1)C(=O)N(C)CCCN(C)C)N2C(=CC(=N2)C(=O)NC3(C4CC5CC(C4)CC3C5)C(=O)O)C6=C(C=CC=C6OC)OC | ||
| Standard InChIKey | LWULHXVBLMWCHO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C39H51N5O6/c1-23(2)29-21-26(37(46)43(5)15-9-14-42(3)4)12-13-31(29)44-32(35-33(49-6)10-8-11-34(35)50-7)22-30(41-44)36(45)40-39(38(47)48)27-17-24-16-25(19-27)20-28(39)18-24/h8,10-13,21-25,27-28H,9,14-20H2,1-7H3,(H,40,45)(H,47,48) | ||
| 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 non-peptide neurotensin (NT) receptor antagonist that binds with high affinity (IC50 = 0.32 - 3.96 nM; Ki < 10 nM). Attenuates amphetamine-induced hyperactivity and is orally active in vivo. |
SR 142948 Dilution Calculator
SR 142948 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.458 mL | 7.2901 mL | 14.5802 mL | 29.1605 mL | 36.4506 mL |
| 5 mM | 0.2916 mL | 1.458 mL | 2.916 mL | 5.8321 mL | 7.2901 mL |
| 10 mM | 0.1458 mL | 0.729 mL | 1.458 mL | 2.916 mL | 3.6451 mL |
| 50 mM | 0.0292 mL | 0.1458 mL | 0.2916 mL | 0.5832 mL | 0.729 mL |
| 100 mM | 0.0146 mL | 0.0729 mL | 0.1458 mL | 0.2916 mL | 0.3645 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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X-ray structural characterization of SR 142948, a novel potent synthetic neurotensin receptor antagonist.[Pubmed:9871577]
Bioorg Med Chem Lett. 1998 Mar 17;8(6):653-8.
SR 142948 is an original and extremely potent neurotensin receptor antagonist developed in a promising approach to novel antipsychotic drugs. The X-ray structure was elucidated and compared to SR 48692 and levocabastine, providing new informations about the possible recognition process of NT receptor subtypes.
Neurotensin type 1 receptor-mediated activation of krox24, c-fos and Elk-1: preventing effect of the neurotensin antagonists SR 48692 and SR 142948.[Pubmed:9710257]
FEBS Lett. 1998 Jul 31;432(1-2):88-93.
Stimulation of neurotensin (NT) type 1 receptors (NT1-R) in transfected CHO cells is followed by the activation of mitogen-activated protein kinases and the expression of the early response gene krox24. By making point mutations and internal deletions in the krox24 promoter, we show that proximal serum responsive elements (SRE) are involved in transcriptional activation by NT. In addition, we show that the related early response gene c-fos and the Ets protein Elk-1 are also induced by NT. The involvement of NT1-R in NT-mediated activation of krox24, c-fos and Elk-1 was demonstrated by the preventing effect of the specific antagonists SR 48692 and SR 142948. Finally, we show that the activation of krox24 and Elk-1 on the one hand, and that of c-fos on the other hand, result from independent transduction pathways since the former are pertussis toxin-sensitive whereas the latter is insensitive to pertussis toxin.
Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.[Pubmed:9023294]
J Pharmacol Exp Ther. 1997 Feb;280(2):802-12.
SR 142948A, 2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methylc arbamoyl)-2-isopropylphenyl)-1H-pyrazole3-carbonyl]amino] adamantane-2-carboxylic acid, hydrochloride, a new and extremely potent neurotensin (NT) receptor antagonist, has been characterized in comparison with SR 48692. This selective compound possesses nanomolar affinities for NT receptors, recognizes the two binding sites described for the NT receptor and fully displaces [3H]SR 48692 specific binding. SR 142948A antagonizes the classical in vitro NT effects, i.e., inositol monophosphate formation in HT 29 cells (IC50 = 3.9 nM) or intracellular calcium mobilization in Chinese hamster ovary cells transfected with the human receptor. It dose-dependently (0.04-640 x 10(-3) mg/kg p.o.) inhibits the turning behavior induced by unilateral intrastriatal injection of NT in mice, with the biphasic profile previously seen for SR 48692. At 0.1 mg/kg (i.p.), it completely antagonizes NT-evoked acetylcholine release in the rat striatum. In contrast to SR 48692, SR 142948A (p.o.) blocks both hypothermia and analgesia induced by i.c.v. injection of NT (mice and/or rats) but is unable to modify the dopamine release evoked by NT injection into the ventral tegmental area. In summary, SR 142948A retains the properties of the lead compound SR 48692 (no intrinsic agonist activity, oral bioavailability, long duration of action and good brain access), reveals a wider spectrum of activity than SR 48692 (probably due to the inhibition of NT receptor subtypes) and represents an additional tool for further exploration of the therapeutic potential of this class of compounds.
