| Cat. No. |
Product Name |
CAS No. |
Information |
| H9515 |
UPF-523
|
168560-79-0 |
UPF-523 (AIDA) is a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. |
| H9308 |
RO0711401
|
714971-87-6 |
RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM. |
| H3644 |
VU6012962
|
2313526-86-0 |
VU6012962 (VU-6012962) is a potent, orally bioavailable and CNS penetrant mGlu7 negative allosteric modulator with IC50 of 0.35 uM; VU6012962 is highly selective for mGlu7 versus the other seven mGlu receptor subtypes and across large ancillary pharmacology panels; decreases anxiety in the elevated zero maze (EZM) assay in mice. |
| H3643 |
VU6010608
|
2165325-42-6 |
A potent, highly selective, CNS penetrant mGlu7 negative allosteric modulator with IC50 of 0.76 uM; shows no activity against mGlu1,2,3,4,5,6,8, as well as a penel of 68 GPCRs, ion channels and transporters (IC50>10 uM); blocks long-term potentiation (LTP) at SC-CA1 synapses in mice brain slices induced by high frequency stimulation. |
| H3642 |
VU6005649
|
2137047-43-7 |
A potent, CNS penetrant, dual mGlu7/8 positive allosteric modulator with EC50 of 0.65/2.6 uM, respectively; displays no activity for mGlu4 (EC50>10 uM); shows modest but significant pro-cognitive effects on associative learning in wild type mice. |
| H3641 |
VU6001376
|
1968546-34-0 |
VU6001376 (VU 6001376, VU-6001376) is a potent, selective, positive allosteric modulator of mGlu4 with EC50 of 28 nM, 49% Glu Max, shows no activity against other 7 mGlu receptors; demonstrates efficacy in reversing haloperidol induced catalepsy in a rodent preclinical model of Parkinson's disease. |
| H3640 |
VU0652957
|
1976050-09-5 |
VU0652957 (VU2957, Valiglurax) is a potent, selective mGlu4 positive allosteric modulator (PAM) with EC50 of 64.6 nM in calcium mobilization human mGlu4/Gqi5 assays; showes excellent pharmacokinetics across species (low CLps, %F > 35%), an acceptable CYP profile (>30 uM vs. 3A4, 2D6 and 2C9, 12.5 uM vs. 2C19 and 1.5 uM vs. 1A2), no CYP induction or timedependent inhibition and excellent metabolite coverage across species; also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours). |
| H3639 |
VU0477573
|
1946021-40-4 |
A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM; shows no activity against the other mGlu receptor subtypes (>10 uM); exhibits full occupancy of the MPEP site, does not completely inhibit maximal effects of mGlu5 agonists on intracellular calcium mobilization, inositol phosphate (IP) accumulation, or inhibition of synaptic transmission at the hippocampal Schaffer collateral-CA1 synapse; acts as a full NAM when measuring effects on mGlu5-mediated ERK1/2 phosphorylation; shows robust efficacy, comparable to the mGlu5 NAM MTEP, in models of anxiolytic activity. |
| H3638 |
VU0424238
|
1396337-04-4 |
VU0424238 (Auglurant) is a potent, selective, orally active mGlu5 negative allosteric modulator with Ki of 4.4 nM, displays >900-fold selectivity for mGlu5 versus the other mGlu receptors; demonstrates 50% receptor occupancy at an oral dose of 0.8 mg/kg in rats and an intravenous dose of 0.06 mg/kg in baboons. |
| H3637 |
VU0422288
|
1630936-95-6 |
VU0422288 is a potent, selective, CNS-penetrant pan-Group III mGlu positive allosteric modulator with IC50 of 110/146/130 nM for mGlu8/7/4, respectively, displays >30-fold selectivity over groups I and II mGlus (mGlu1/2/3/5/6). |
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