MGluR5 inhibitor
- Product Name
- MGluR5 inhibitor
- CAS No.
- 871362-31-1
- Chemical Name
- MGluR5 inhibitor
- Synonyms
- CTEP;CS-1999;RO4956371;CTEP (RO4956371);MGluR5 inhibitor;MGluR5 inhibitor(CTEP);MGluR5 inhibitor USP/EP/BP;Metabotropic glutamate receptors,CTEP,RO4956371,inhibit,mGluR,Inhibitor,RO-4956371;2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine;Pyridine, 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]-
- CBNumber
- CB72645136
- Molecular Formula
- C19H13ClF3N3O
- Formula Weight
- 391.77
- MOL File
- 871362-31-1.mol
MGluR5 inhibitor Property
- Boiling point:
- 523.0±60.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- insoluble in EtOH; insoluble in H2O; ≥19.6 mg/mL in DMSO
- form
- powder
- pka
- 5.01±0.70(Predicted)
- color
- white to beige
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H320Causes eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P330Rinse mouth.
N-Bromosuccinimide Price
- Product number
- SML2306
- Product name
- CTEP
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $155
- Updated
- 2024/03/01
- Product number
- SML2306
- Product name
- CTEP
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $642
- Updated
- 2024/03/01
- Product number
- 28773
- Product name
- CTEP
- Packaging
- 5mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 28773
- Product name
- CTEP
- Packaging
- 50mg
- Price
- $961
- Updated
- 2024/03/01
- Product number
- 28773
- Product name
- CTEP
- Packaging
- 10mg
- Price
- $230
- Updated
- 2024/03/01
MGluR5 inhibitor Chemical Properties,Usage,Production
Biological Activity
ctep is a potent, long-acting, and orally bioavailable inhibitor of metabotropic glutamate receptor 5 (mglu5) with ic50 value of 11.4nm [1].ctep is a negative allosteric modulator of mglu5 and has inverse agonist activity. in the in vitro binding assay, ctep binds to human, mouse and rat mglu5 with kd values of 1.7nm, 1.8nm and 1.5 nm, respectively. in hek293 cells expressing mglu5, ctep inhibits quisqualate-induced ca2+ mobilization and inositol phosphate accumulation with ic50 value of 11.4nm and 6.4nm, respectively. in addition, it shows an ic50 value of 40.1nm in the ip accumulation assay, demonstrating its inverse agonist activity. ctep is proved to be a highly selective inhibitor of mglu5. it shows no significant activity against mglu1, mglu2, mglu3, mglu4, mglu6, mglu7 or mglu8 at concentration up to 10μm [1].in the in vivo vogel conflict drinking test, ctep markedly increases drinking time at doses of 0.3mg/kg. in adult c57bl/6 mice brain, ctep displaces the mglu5 antagonist abp688 in the regions expressing mglu5 by 50% at dose of 77.5 ng/g [1].
Biochem/physiol Actions
CTEP is a high-affinity, orally active, potent and selective metabotropic glutamate receptor 5 (mGlu5 or mGluR5) negative allosteric modulator (NAM) and inverse agonist (human/mouse/rat mGlu5 Kd = 1.7/1.8/1.5 nM; IC50 against quisqualate stimulation = 6.4/16.8/8/8 by IP accumulation or 11.4/42/4/6.9 by Ca2+ mobilization using human/mouse/rat mGlu5 HEK293 transfectants; IC50 = 40.1 nM against constitutive IP level in human mGlu5 HEK293) with >1000-fold selectivity over 103 molecular targets, including all known mGluRs. CTEP is an excellent tool compound for long-term in vivo studies (in mice and rats) with good pharmacokinetic properties (B/P ratio = 2.6, oral bioavailability ~100%, T1/2 ~18 hrs post 4.5 mg/kg p.o. in mice) and reported to display 30- to 100-fold higher in vivo potency than MPEP and fenobam in two rodent behavioral models sensitive to antianxiety drugs.
target
mGlu5 receptor
References
[1] lindemann l, jaeschke g, michalon a, et al. ctep: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. journal of pharmacology and experimental therapeutics, 2011, 339(2): 474-486.
MGluR5 inhibitor Preparation Products And Raw materials
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