Physicochemical Properties
| Molecular Formula | C11H9CLN2S |
| Molecular Weight | 236.720559835434 |
| Exact Mass | 236.017 |
| CAS # | 1186195-60-7 |
| Related CAS # | MTEP;329205-68-7 |
| PubChem CID | 45073467 |
| Appearance | Light yellow to yellow solid powder |
| LogP | 3.048 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 3 |
| Rotatable Bond Count | 2 |
| Heavy Atom Count | 15 |
| Complexity | 253 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | YCIOJDKGCWAHLR-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C11H8N2S.ClH/c1-9-13-11(8-14-9)5-4-10-3-2-6-12-7-10;/h2-3,6-8H,1H3;1H |
| Chemical Name | 2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole;hydrochloride |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | Compared to MPEP, MTEP is less off-target and has a different selectivity for mGluR5 than mGluR1, while MPEP has no effect on other mGluR subtypes [1]. |
| ln Vivo | The catalepsy coefficient caused by haloperidol (0.5 mg/kg, i.p.) is inhibited by MTEP (0-5 mg/kg, i.p., once) [2]. MTEP (0.3-3 mg/kg, i.p., once) is in control. |
| Animal Protocol |
Animal/Disease Models: Male Wistar rats (215-315 g, 5-9/group) [2] Doses: 1, 3, and 5 mg/kg given Medication method: IP, inducing antidepressant-like effects in C57BL/6J mice [3]. One injection, 60 minutes after haloperidol (0.5 mg/kg/2 ml ip) Experimental Results:Inhibition of haloperidol-induced rigor. Animal/Disease Models: Male C57BL/6J mice (23-25 g) [3] Doses: 0.3, 1 and 3 mg/kg Route of Administration: intraperitoneal (ip) injection, 1 hour before test Experimental Results: Dramatically diminished mice in the tail suspension test Immobility time (Tsim Sha Tsui) increased by 24%, 41% and 48% respectively. The efficacy of MTEP used at doses of 1 and 3 mg/kg was not Dramatically different from that of imipramine (20 mg/kg, i.p.) used as a positive standard. |
| References |
[1]. Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP. CNS Drug Rev. 2006 Summer;12(2):149-66. [2]. MTEP, a new selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5), produces antiparkinsonian-like effects in rats. Neuropharmacology. 2005 Sep;49(4):447-55. [3]. Potential antidepressant-like effect of MTEP, a potent and highly selective mGluR5 antagonist. Pharmacol Biochem Behav. 2005 Aug;81(4):901-6. [4]. Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling. Neuropharmacology. 2004 Sep;47(3):342-50. |
Solubility Data
| Solubility (In Vitro) | H2O : ~20 mg/mL (~84.49 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (422.44 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2244 mL | 21.1220 mL | 42.2440 mL | |
| 5 mM | 0.8449 mL | 4.2244 mL | 8.4488 mL | |
| 10 mM | 0.4224 mL | 2.1122 mL | 4.2244 mL |