CTEP (RO4956371)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1280 | In Stock |
| 500mg | $1920 | In Stock |
| 1g | $2880 | In Stock |
: Cat #: V1084 CAS #: 871362-31-1 Purity ≥ 98%
Description: CTEP (also called RO4956371; RO 4956371; RO-4956371) is a long-acting and orally bioavailable allosteric antagonist of metabotropic glutamate receptor 5 (mGlu5) receptor with important biological activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 391.77 |
|---|---|
| Molecular Formula | C19H13ClF3N3O |
| CAS No. | 871362-31-1 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 78 mg/mL (199.1 mM)rr |
| Water: <1 mg/mLrr | |
| Ethanol: 10 mg/mL (25.5 mM) | |
| Solubility In Vivo | 30% propylene glycol, 5% Tween 80, 65% D5W: 6 mg/mL |
| SMILES Code | FC(F)(F)OC1=CC=C(N2C(C)=C(C#CC3=CC(Cl)=NC=C3)N=C2C)C=C1 |
| Synonyms | RO-4956371; CTEP; RO4956371; RO 4956371; 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine Chemical Name: 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine SMILES Code: FC(F)(F)OC1=CC=C(N2C(C)=C(C#CC3=CC(Cl)=NC=C3)N=C2C)C=C1 |
| Protocol | In Vitro | CTEP (RO 4956371) inhibits quisqualate-induced Ca2+ mobilization with an IC50 of 11.4 nM and [3H]IP accumulation with an IC50 of 6.4 nM in HEK293 cells stably expressing human mGlu5. CTEP (RO 4956371) inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC50 of 40.1 nM in HEK293 cells stably expressing human mGlu5 |
|---|---|---|
| In Vivo | CTEP (RO 4956371) is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP (RO 4956371) significantly increases drinking time at doses of 0.3 mg/kg and 1.0 mg/kg in the Vogel conflict drinking test in rat, whereas it has no effect at lower doses. The half-life of CTEP (RO 4956371) (oral) is 18 h, and the B/P ratio based on total drug concentrations in plasma and whole brain homogenates is 2.6 in mice. After single oral doses of 4.5 and 8.7 mg/kg CTEP (RO 4956371) formulated as microsuspension in a saline/Tween vehicle administrated to adult C57BL/6 mice is rapidly absorbed and achieves close to maximal exposure after approximately 30 min. Chronic administration in adult mice with a dose of 2 mg/kg p.o. every 48 h for 2 months reaches a minimal CTEP (RO 4956371) brain exposure of 240 ng/g. CTEP (RO 4956371) fully displaces [3H]ABP688 in mouse brain regions known to express mGlu5, and 50% displacement is achieved with doses producing an average compound concentration of 77.5 ng/g measured in whole brain homogenate |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.5525 mL | 12.7626 mL | 25.5252 mL | 51.0504 mL |
| 5mM | 0.5105 mL | 2.5525 mL | 5.1050 mL | 10.2101 mL |
| 10mM | 0.2553 mL | 1.2763 mL | 2.5525 mL | 5.1050 mL |
| 20mM | 0.1276 mL | 0.6381 mL | 1.2763 mL | 2.5525 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Volume
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Molecular Weight*
The dilution calculator equation
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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V1
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.