- MTEP hydrochloride
- MPEP
- mGlu2 agonist
- Dipraglurant
- CTEP (RO4956371)
| LY341495Metabotropic glutamate receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | U87 cell lines |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions | 72h; 1 μM |
Applications | It is well established that U87 cells proliferate in a glutamate-dependent manner and drugs LY341495, an inhibitor of metabotropic glutamate receptor have been shown to inhibit proliferation of glioma cells. The result shown that Iressa in combination with LY341495 is effective in inhibiting proliferation. |
| Animal experiment [2]: | |
Animal models | Male 6-week-old Sprague-Dawley rats |
Dosage form | 3 mg/kg; intraperitoneal injection |
Applications | We tested the anti-immobility effect of LY341495 in the forced swim test (FST). LY341495 significantly decreased the immobility behavior (F(3,36)=3.05; P<0.05, n="10" each).="" a="" post="" hoc="" analysis="" showed="" that="" rats="" exposed="" to="" 3="" mg/kg="" of="" ly341495="" had="" a="" significantly="" shorter="" immobility="" time=""><0.05). to="" investigate="" the="" behavioral="" relevance="" of="" ampa="" receptor="" transmission="" during="" the="" test,="" nbqx="" was="" injected="" 30="" min="" before="" the="" test.="" nbqx="" had="" a="" significant="" effect="" on="" the="" ly341495-induced="" reduction="" in="" the="" immobility="" time="" (f(3,36)="3.60;"><0.05, n="10" each).="" a="" post="" hoc="" analysis="" showed="" that="" nbqx="" at="" doses="" of="" 3="" and="" 10="" mg/kg="" significantly="" prevented="" the="" anti-immobility="" effect="" of="" ly341495=""><> |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Yelskaya Z, Carrillo V, Dubisz E, et al. Synergistic Inhibition of Survival, Proliferation, and Migration of U87 Cells with a Combination of LY341495 and Iressa[J]. PloS one, 2013, 8(5): e64588. [2] Koike H1, Chaki S2. Requirement of AMPA receptor stimulation for the sustained antidepressant activity of ketamine and LY341495 during the forced swim test in rats. Behav Brain Res. 2014 Sep 1;271:111-5. doi: 10.1016/j.bbr.2014.05.065. Epub 2014 Jun 5. | |
LY341495 Dilution Calculator
calculate
LY341495 Molarity Calculator
calculate
| Cas No. | 201943-63-7 | SDF | Download SDF |
| Synonyms | LY 341495; LY-341495 | ||
| Chemical Name | (1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid | ||
| Canonical SMILES | C1C(C1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O | ||
| Formula | C20H19NO5 | M.Wt | 353.38 |
| Solubility | Limited solubility, soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
LY341495 is a highly potent and selective antagonist of group II metabotropic glutamate receptors with IC50 values of 21 nM and 14 nM for mGlu2 and mGlu3 receptors, respectively [1].
Glutamate is the major excitatory neurotransmitter that regulates neuronal plasticity and maintains fast synaptic transmission. The aberrant glutamate pathway has been found in a serious of neurological?problems, such as cognitive disorders, epilepsy and AD. As a selective inhibitor of group II metabotropic glutamate receptors (including mGlu2 and mGlu3), LY341495 acts as a competitive antagonist to regulate the transmission of glutamate [1 and 2].
In the functional assays, LY341495 at concentrations of 0.1 μM and 30 nM completely reversed the ACPD-induced inhibition of cAMP formation which was stimulated by forskolin in mGlu2 expressing cells and mGlu3 expressing cells, respectively. In RGT cells expressing group III mGlu receptors (mGlu4, 6, 7 and 8), LY341495 showed significant reversion of L-AP4-inhibited cAMP formation stimulated by forskolin. For mGlu4a, 7a and 8, the IC50 value of LY341495 were 22, 0.99 and 0.173 μM, respectively, which were 5 to 1000-fold higher than that for mGlu2 and mGlu3. For the group I mGlu receptors (mGlu1a and 5a), the IC50 values were 6.8 and 8.2 μM, respectively. Besides that, LY341495 was found to reversibly eliminate the long-term synaptic depression induced by DHPG in rats’ hippocampal slices [1 and 2].
In animal experiments, LY341495 was found to have effects on the post-training recognition memory. It was reported that the administration of LY341495 at different doses showed different efficacies on rats’ recognition memory. Rats treated with LY341495 at doses of 0.3, 1 and 3 mg/kg displayed a significant lower level of discrimination while LY341495 at doses of 0.05 and 0.1 mg/kg exerted a reversion of the recognition memory extinction and showed no impairment of the recognition memory [3].
References: [1] Kingston A E, Ornstein P L, Wright R A, et al. LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology, 1998, 37(1): 1-12.[2] Fitzjohn S M, Bortolotto Z A, Palmer M J, et al. The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology, 1998, 37(12): 1445-1458.[3] Pitsikas N, Kaffe E, Markou A. The metabotropic glutamate 2/3 receptor antagonist LY341495 differentially affects recognition memory in rats. Behavioural brain research, 2012, 230(2): 374-379.
