| Size | Price | |
|---|---|---|
| 5mg |
Purity: ≥98%
SR 142948A is a novel non-peptide Neurotensin receptor antagonist used in scientific research. SR 142948A is a potent neurotensin receptor antagonist that affects the expression of c-Fos and has properties of antipsychotic agent. It blocks hypothermia and analgesia induced by neurotensin. It blocks the increase in the concentration of Ca+2 induced by the activation of phospholipase C in CHO cell model. SR-142948 has been used to study the role of neurotensin in the regulation of dopamine receptor activity and glutamate signalling in the brain, and in animal studies SR-142948 blocked the effects of stimulant drugs, including MDMA.
| ln Vitro |
In CHO-hNT1-R cells, SR 142948 (1 µM; 90 minutes) suppresses the expression of c-fos and krox24 [1]. By preventing the binding of [125I-Tyr3]NT to h-NTR1-CHO and HT 29 cell membranes, SR 142948 (0-1 µM; 1) demonstrates strong anti-clamp activity [2]. Its IC50 values are 1.19 and 0.32 nM, respectively. The depletion of anti-h-NTR1-CHO is clamped by SR 142948 (0-1 µM; 30 min) concentration and the intracellular calcium stimulation of single anti-h-NTR1-CHO cells is stimulated by SR 142948 (1, 10 nM; 60-80 sec)[2].
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| ln Vivo |
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single dose) partially but significantly blocked NT conduction in hyposomnia (impedance) at doses SR 142948 (90-10 mg/kg; facial; single dose) 2 mg) in an induced manner that prevents the enhanced ACh release produced by NT (100 nM) [2]. SR 142948 (2 µg/kg; chamber; single dose) inhibits NT (10 pg/mouse)-induced turning behavior [2].
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| Animal Protocol |
Animal/Disease Models: Female Swiss albino CD1 mouse (25-30 g; striatal injection 10 pg/mouse NT)[2]./kg 53% and mouse 4mg/kg 54%)[2].
Doses: 2 µg/kg Route of Administration: Oral; single. Experimental Results: Within 1-2 hrs (hrs (hours)) after administration, the flipping behavior was inhibited and had the largest and significant antagonistic effect. |
| References |
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| Additional Infomation |
2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[3-(dimethylamino)propyl-methylamino]-oxomethyl]-2-propan-2-ylphenyl]-3-pyrazolyl]-oxomethyl]amino]-2-adamantanecarboxylic acid is a N-acyl-amino acid.
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| Molecular Formula |
C39H51N5O6
|
|---|---|
| Molecular Weight |
685.8522
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| Exact Mass |
685.384
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| CAS # |
184162-64-9
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| Related CAS # |
SR 142948 dihydrochloride
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| PubChem CID |
5311451
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| Appearance |
White to off-white solid powder
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| Density |
1.29g/cm3
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| Boiling Point |
824.7ºC at 760 mmHg
|
| Flash Point |
452.5ºC
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| Vapour Pressure |
8.51E-29mmHg at 25°C
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| Index of Refraction |
1.636
|
| LogP |
6.287
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
50
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| Complexity |
1170
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LWULHXVBLMWCHO-UHFFFAOYSA-N
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| InChi Code |
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)
|
| 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
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| Synonyms |
SR142948A; SR-142948A; SR 142948A; SR-142948-A; SR 142948 A; 2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methylcarbamoyl)-2-isopropylphenyl)-1H-pyrazole3-carbonyl]amino] adamantane-2-carboxylic acid hydrochloride, SR 142948 hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4580 mL | 7.2902 mL | 14.5804 mL | |
| 5 mM | 0.2916 mL | 1.4580 mL | 2.9161 mL | |
| 10 mM | 0.1458 mL | 0.7290 mL | 1.4580 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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