| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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Purity: ≥98%
| Targets |
The primary target of SR142948A is the neurotensin (NT) receptor. It acts as a potent non-peptide neurotensin receptor antagonist. Neurotensin is a neuropeptide involved in the regulation of dopamine pathways, pain, and body temperature. By blocking the neurotensin receptor, SR142948A inhibits the effects of neurotensin, including hypothermia and analgesia. The compound has an IC50 of 0.32-3.96 nM and a Ki of less than 10 nM.
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| 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].
SR142948A is a potent neurotensin receptor antagonist with an IC50 of 0.32-3.96 nM and a Ki of less than 10 nM. It affects the expression of c-Fos, an immediate early gene that is a marker of neuronal activation. The compound has properties of an antipsychotic agent, suggesting that it may modulate dopamine signaling pathways. It blocks hypothermia and analgesia induced by neurotensin. |
| 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].
SR142948A blocks hypothermia and analgesia induced by neurotensin in animal models. It affects the expression of c-Fos, indicating modulation of neuronal activity. The compound has properties of an antipsychotic agent, suggesting potential efficacy in psychiatric disorders. Specific in vivo efficacy data are not detailed in the available sources beyond these pharmacological effects. |
| Enzyme Assay |
The neurotensin receptor binding assay for SR142948A involves incubating the compound with membrane preparations from cells expressing the neurotensin receptor and a radiolabeled neurotensin ligand (e.g., [¹²⁵I]-neurotensin). After incubation at 4°C for an appropriate period, bound and free ligands are separated by filtration, and the radioactivity is counted. The IC50 or Ki for displacement of the radioligand is calculated from the competition curve.
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| Cell Assay |
Cellular assays for SR142948A would typically involve measuring its effects on neurotensin-induced signaling in cells expressing the neurotensin receptor. This could include measuring intracellular calcium mobilization, cAMP levels, or activation of downstream signaling pathways such as MAPK. The compound's ability to block neurotensin-induced c-Fos expression can also be assessed in neuronal cell cultures. Specific protocols are not detailed in the available sources.
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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. To evaluate the in vivo effects of SR142948A, rodents are typically administered the compound (e.g., intraperitoneally or orally) and then challenged with neurotensin. Body temperature is measured to assess the blockade of neurotensin-induced hypothermia. Pain sensitivity is assessed using standard analgesic tests (e.g., hot plate or tail flick) to evaluate the blockade of neurotensin-induced analgesia. The expression of c-Fos in specific brain regions can be measured by immunohistochemistry to assess neuronal activation. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for SR142948A are not provided in the available sources. The compound is a small molecule with a molecular weight of 685.86. Standard pharmacokinetic studies would typically involve administering the compound to rodents and measuring plasma and brain concentrations over time using LC-MS/MS to determine key PK parameters.
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| Toxicity/Toxicokinetics |
Specific toxicity data for SR142948A are not provided in the available sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[3-(dimethylamino)propyl-methylamino]-oxymethyl]-2-propyl-2-ylphenyl]-3-pyrazolyl]-oxymethyl]amino]-2-adamantane carboxylic acid is an N-acyl amino acid.
SR142948A is a potent non-peptide neurotensin receptor antagonist. It has an IC50 of 0.32-3.96 nM and a Ki of less than 10 nM for the neurotensin receptor. It affects the expression of c-Fos and has properties of an antipsychotic agent. The compound blocks hypothermia and analgesia induced by neurotensin. It has a CAS number of 184162-64-9 and is supplied for research purposes. |
| Molecular Formula |
C39H51N5O6
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|---|---|
| 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
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| 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
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| LogP |
6.287
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| Hydrogen Bond Donor Count |
2
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| 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)
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| 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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