SR 48692 |
| Catalog No.GC13242 |
nonpeptide neurotensin antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 146362-70-1
Sample solution is provided at 25 µL, 10mM.
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SR 48692 is an orally bioavailable allosteric antagonist of the neurotensin receptor NTS1 (Kd = 3.4 nM).[1],[2] SR 48692 inhibits high affinity neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as well as rat mesencephalic cells and HT-29 cells with IC50 values ranging from 0.99 to 30.3 nM.[1] It blocks neurotensin-induced intracellular calcium mobilization in HT-29 cells with a Ki value of 7.4 nM. SR 48692 (10 μM) inhibits NCI-H209 and NCI-H345 cell proliferation by approximately 70 and 80%, respectively.[3] In vivo, SR 48692 (10 μg per day) reduces tumor volume and cell proliferation in an NCI-H209 mouse xenograft model. SR 48692 (80 μg/kg, p.o.) reduces contralateral turning induced by neurotensin administration in mice by 85%.[1]Daily administration of SR 48692 for five days in rats delays sensitization to the locomotor activating effects of cocaine during three additional cocaine challenges when given seven days prior to cocaine delivery but not under a cotreatment regimen.[4]
Reference:
[1]. Gully, D., Canton, M., Boigegrain, R., et al. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc. Natl. Acad. Sci. U.S.A. 90(1), 65-69 (1993).
[2]. Labbé-Jullié, C., Botto, J.-M., Mas, M.-V., et al. [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: Characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor. Mol. Pharmacol. 47(5), 1050-1056 (1995).
[3]. Moody, T.W., Chiles, J., Casibang, M., et al. SR48692 is a neurotensin receptor antagonist which inhibits the growth of small cell lung cancer cells. Peptides 22(1), 109-115 (2001).
[4]. Horger, B.A., Taylor, J.R., Elsworth, J.D., et al. Preexposure to, but not cotreatment with, the neurotensin antagonist SR 48692 delays the development of cocaine sensitization. Neuropsychopharmacology 11(3), 215-222 (1994).
| Cas No. | 146362-70-1 | SDF | |
| Chemical Name | (1R,2R,3R,5S,7S)-2-(1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamido)adamantane-2-carboxylic acid | ||
| Canonical SMILES | ClC1=CC=C2C(N3N=C(C=C3C(C(OC)=CC=C4)=C4OC)C(N[C@]5(C(O)=O)[C@H]6C[C@H]7C[C@H]5C[C@H](C7)C6)=O)=CC=NC2=C1 | ||
| Formula | C32H31ClN4O5 | M.Wt | 587.07 |
| Solubility | DMSO: 20 mM | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7034 mL | 8.5169 mL | 17.0337 mL |
| 5 mM | 0.3407 mL | 1.7034 mL | 3.4067 mL |
| 10 mM | 0.1703 mL | 0.8517 mL | 1.7034 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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