SR 48692
- Product Name
- SR 48692
- CAS No.
- 146362-70-1
- Chemical Name
- SR 48692
- Synonyms
- Meclinertant;2-CARBOXYLIC ACID;CS-334;SR 48692;merclinertant;meclinertant, CID 119192;2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid;2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]tricyclo[3.3.1.13,7]decane-2-carboxylic acid;Tricyclo[3.3.1.13,7]decane-2-carboxylic acid, 2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-
- CBNumber
- CB11396891
- Molecular Formula
- C32H31ClN4O5
- Formula Weight
- 587.07
- MOL File
- 146362-70-1.mol
SR 48692 Property
- Density
- 1.50
- storage temp.
- -20°C
- solubility
- DMSO: ≥2mg/mL (warmed)
- form
- powder
- color
- white to beige
Safety
- WGK Germany
- 3
- RTECS
- YD1988500
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0278
- Product name
- SR 48692
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $131
- Updated
- 2024/03/01
- Product number
- SML0278
- Product name
- SR 48692
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $521
- Updated
- 2024/03/01
- Product number
- 20124
- Product name
- SR 48692
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 20124
- Product name
- SR 48692
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $122
- Updated
- 2024/03/01
- Product number
- 20124
- Product name
- SR 48692
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $230
- Updated
- 2024/03/01
SR 48692 Chemical Properties,Usage,Production
Uses
SR 48692 has been used as a neurotensin?high-affinity receptor 1 (NTSR1) antagonist:
- to explore the function of NTSR1 in glioblastoma (GBM) cells
- to determine the roles of neurotensin (NT) in the regulation of bile acid?(BA) uptake, in vivo
- to explore the involvement of NTSR1 versus NTSR2 in mice
Definition
ChEBI: 2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-3-pyrazolyl]-oxomethyl]amino]-2-adamantanecarboxylic acid is a N-acyl-amino acid.
Biological Activity
ki: 8.6 nm for ht-29 cellssr 48692 is a nonpeptide neurotensin antagonist.neurotensin is a tridecapeptide and is distributed in both the central and peripheral nervous systems. neurotensin shows a wide spectrum of biological activities resulting in fulfilling a dual function as a neurotransmitter/neuromodulator in the brain and working as a hormone/cellular mediator in peripheral tissues.
Biochem/physiol Actions
SR 48692 is a high affinity, orally bioavailable and selective nonpeptide NT1 neurotensin receptor antagonist that antagonizes neurotensin-induced calcium mobilization with a pA2 of 8.13 in HT-29 human colon carcinoma cell line, and blocks the ability of neurotensin to increase GABA levels in the prefrontal cortex.
in vitro
sr 48692 was found to inhibit the binding of [3h]- or [125i]-neurotensin to membrane preparations from mouse brains and ht-29 cells. in ht-29 cells, sr 48692 also antagonized the neurotensin-induced mobilization of intracellular calcium, which was consistent with previous findings. moreover, in rat cerebellar slices, sr 48692 could block the cyclic gmp level increase in a dose-dependent manner [1].
in vivo
sr 48692 could antagonize the increase in rat brain mesolimbic dopamine turnover which was induced by the systemically active neurotensin peptide ei. whereas, sr 48692 did not antagonize ei-induced decrease in mouse body temperature and spontaneous locomotor activity [1].
storage
Store at +4°C
References
[1] pugsley ta,akunne hc,whetzel sz,demattos s,corbin ae,wiley jn,wustrow dj,wise ld,heffner tg. differential effects of the nonpeptide neurotensin antagonist, sr 48692, on the pharmacological effects of neurotensin agonists. peptides.1995;16(1):37-44.
[2] zerbib f,piche t,charles f,galmiche jp,bruley des varannes s. sr 48692, a specific neurotensin receptor antagonist, has no effect on oesophageal motility in humans. aliment pharmacol ther.2004 apr 15;19(8):931-9.
SR 48692 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from SR 48692 manufacturers
- Product
- SR 48692 146362-70-1
- Price
- US $20.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 1000kg
- Release date
- 2024-03-27