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Home / Biochemicals / Small Molecules

A-794278

SKU : BHB21300039

An Antagonist of mGluR1 and mGluR5

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Mfr.No.	A-435, A-435_10 mg, A-435_25 mg, A-435_5 mg, A-435_50 mg
Description	A-794278 (#A-435) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C18H22N4OS.
Background	A-794278 is a potent, non-competitive antagonist of mGluR1. It is a triazafluorenone derivative that also antagonizes mGluR5 receptors. It demonstrates IC50 values of 4.1 nM and 147 nM for mGluR1 and mGluR5, respectively1. A-794278 binds to a putative allosteric recognition site located within the seven-transmembrane domain of the receptor1,2.Glutamate is the most abundant excitatory neurotransmitter in the central nervous system. It modulates the activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs). mGluRs consist of three groups: I, II, and III with a total of eight subtypes, mGluR1 to mGluR8. mGluR1 plays an important role in the central sensitization of pain and in a variety of functions with potential implications in neurological and psychiatric disorders1,2.
Shipping	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
Concentration	1-100 nM.
Reconstitution	Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Cas Number	869802-57-3
Molecular Weight	342.46
Solubility	Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Target	mGluR1, mGluR5
Source	Synthetic
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 uMol/kg)2.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: 3-cycloheptyl-9-(dimethylamino)pyrido(1,2)thieno(3,4-d)pyrimidin-4-one.

Purity	>98%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: -20°C.

Product Manual	SDS

Reference	Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374. Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374. Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300039-1	A-435_10 mg	10 mg	$373		Add to Cart
BHB21300039-2	A-435_25 mg	25 mg	$649		Add to Cart
BHB21300039-3	A-435_5 mg	5 mg	$235		Add to Cart
BHB21300039-4	A-435_50 mg	50 mg	$912		Add to Cart

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