Cat #: EK-250_KIT
Size: 12 Vials
Form: Lyophilized
A-794278 Cat #: A-435
Size:
5 mg
Source: Synthetic
MW: 342.46
Purity: >98%
Effective concentration
1-100 nM.
Activity
A-794278 is a potent and selective noncompetitive mGluR1 antagonist, acting on mGluR1 and mGluR5 with IC50 values of 4.1 nM and 147 nM, respectively1. In vivo it shows analgesic properties, significantly attenuating spontaneous post-operative pain behavior in rats (ED50 = 50 μmol/kg)2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C. Protect from light and moisture.
Reconstitution
Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
A-850002 Cat #: A-390
Size:
5 mg
Source: Synthetic
MW: 336.41
Purity: >99%
Effective concentration
1 nM – 1 µM.
Activity
A-850002 inhibits mGluR1 in rat primary cerebellar granule neurons with an IC50 of 27 nM1 and human mGluR1 expressed in 1321N1 cells with an IC50 of 43 nM2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
CFMTI Cat #: C-365
Size:
5 mg
Source: Synthetic
MW: 349.4
Purity: >96%
Effective concentration
10 nM – 10 µM.
Activity
CFMTI is a selective and potent allosteric antagonist of mGluR1 receptors. It inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a with IC50 values of 2.6 and 2.3 nM, respectively. It is highly selective for mGluR1 over mGluR5 (2000-fold), and does not affect mGluR subtypes and other receptors at 10 µM1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
CPCCOEt Cat #: C-370
Size:
5 mg
Source: Synthetic
MW: 247.25
Purity: >98%
Effective concentration
10-200 µM.
Activity
CPCCOEt is a selective, non-competitive antagonist of mGluR1 receptors, inhibiting hmGluR1b with IC50 of 6.5 µM, whilst having no effect at 100 µM on a range of other receptor subtypes1. It was shown to inhibit synaptic activation of mGluR1 in Purkinje cell cerebellar slices with IC50 of 37µM2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C. Protect from light and moisture.
Reconstitution
Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
DM-PPP Cat #: D-255
Size:
5 mg
Source: Synthetic
MW: 309.19
Purity: >97%
Effective concentration
1 nM – 1 µM.
Activity
DM-PPP is a selective and non-competitive antagonist of mGluR1 receptors. It inhibits the receptor in CHO cells with an IC50 of 15.8 nM1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
FPTQ Cat #: F-185
Size:
5 mg
Source: Synthetic
MW: 305.3
Purity: >97%
Effective concentration
10 nM – 10 µM.
Activity
FPTQ is a selective allosteric antagonist of the mGluR1 receptors, inhibiting [3H]FTIDC binding with Ki of 14 nM, and inhibiting L-glutamate evoked Ca2+ mobilization with IC50 of 3.6 nM in CHO cells expressing human mGluR11. It specifically binds mGluR1 in the rat brain2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
FTIDC Cat #: F-190
Size:
5 mg
Source: Synthetic
MW: 358.4
Purity: >97% (HPLC)
Effective concentration
1-100 nM.
Activity
FTIDC is a potent and selective allosteric antagonist of the mGluR1 receptor, shown to inhibit L-glutamate-induced Ca2+ mobilization in human and mouse mGluR1a-expressing CHO cells (IC50 values of 5.8 nM and 3.1 nM, respectively), while having a 1000-fold weaker activity against human and rat mGluR5 (IC50 values of 6.2 µM and 9.9 µM, respectively)1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
JNJ 16259685 Cat #: J-110
Size:
5 mg
Source: Synthetic
MW: 325.41
Purity: >97%
Effective concentration
1 nM – 1 µM.
Activity
JNJ 16259685 is a potent and selective non-competitive antagonist of mGluR1 receptors, inhibiting human mGluR1 and mGluR5 mediated glutamate-induced Ca2+ mobilization with IC50 values of 1.21 nM and 28.3 µM, respectively, whilst having no effect on a range of other receptor subtypes at over 10 µM1.
It is systemically active, occupying central mGluR1 receptors in the rat cerebellum and thalamus (ED50 = 40 and 14 µg/kg, respectively) when administered subcutaneously1. JNJ 16259685 inhibits synaptic activation of mGluR1 in Purkinje cells in cerebellar slices with IC50 of 19 nM2.
It is systemically active, occupying central mGluR1 receptors in the rat cerebellum and thalamus (ED50 = 40 and 14 µg/kg, respectively) when administered subcutaneously1. JNJ 16259685 inhibits synaptic activation of mGluR1 in Purkinje cells in cerebellar slices with IC50 of 19 nM2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at +4°C.
Reconstitution
Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
LY 456236 hydrochloride Cat #: L-235
Size:
5 mg
Source: Synthetic
MW: 317.77
Purity: >98% (HPLC)
Effective concentration
100 nM – 10 µM.
Activity
LY 456236 hydrochloride is an antagonist of mGluR1, selective over mGluR5 receptors (IC50 values of 143 nM and >10 μM, respectively)1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.
Reconstitution
Up to 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Store up to three months at -20°C.
LY456066 Cat #: L-240
Size:
5 mg
Source: Synthetic
MW: 341.47
Purity: >99%
Effective concentration
1 nM – 1 µM.
Activity
LY456066 is a potent antagonist of mGluR1 receptors. It inhibits human mGluR1 receptors expressed in CHO cells with an IC50 of 28 nM1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
MK-5435 Cat #: M-265
Size:
5 mg
Source: Synthetic
MW: 368.39
Purity: >98%
Effective concentration
10 nM – 10 µM.
Activity
MK-5435 is a potent and selective allosteric mGluR1 antagonist, inhibiting human and rat mGluR1 with IC50 of 4.3 and 3.6 nM, respectively. It is selective over mGluR5 (IC50 = 1.5 µM), mGluR2 and mGluR8 (IC50 = 10 µM), and has no affinity for the quisqualic binding site (IC50 >10 µM). in vivo, following an oral dose of 1 mg/kg, plasma and brain concentrations in mice were 0.17 µM and 0.45 nmol/g respectively, at 30 min post-dose1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
NPS 2390 Cat #: N-340
Size:
5 mg
Source: Synthetic
MW: 307.4
Purity: >98%
Effective concentration
10 nM – 1 uM.
Activity
NPS 2390, a quinoxaline derivative, is a potent and selective non-competitive antagonist of Group I mGluRs, acting on mGluR1 and mGluR5 with IC50 values of to 5.2 and 82 nM, respectively, while having no effect on mGluR2, mGluR8 and other targets at 30 μM1-3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
-20°C.
For more information, please refer to individual certificate of analysis for each product.
For research purposes only, not for human use