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Home / Biochemicals / Small Molecules

ML297 (VU0456810)

SKU : BHB21300221

A Potent and Selective Activator of GIRK1/2 Channels

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Alomone Labs

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Mfr.No.	M-215, M-215_10 mg, M-215_25 mg, M-215_5 mg, M-215_50 mg
Description	ML297 (#M-215) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C17H14F2N4O
Synonyms	Synthetic
Background	ML297 is a potent activator of GIRK channels; it shows a preference for the GIRK1/GIRK2 subunit combination compared to GIRK1/GIRK4 and is inactive on GIRK2/GIRK3 and a number of other potassium channels. ML297 is a useful tool to selectively probe GIRK1/2 channels function in vitro and in vivo. These properties make ML-297 the first and only molecule of its type to selectively probe GIRK1-containing GIRKs and hence it enables the studying of the role of GIRK1-containing GIRKs in numerous normal and pathophysiological conditions1.G protein-gated inwardly rectifying potassium (GIRK) channels hyperpolarize neurons in response to the activation of many G-protein coupled receptors. They are members of the large super-family of inwardly rectifying K+ channels (Kir), in which the inward current is significantly greater than the outward current. Their specific biochemical properties generate a slow inhibitory postsynaptic current that provides a sustained form of inhibition of neuronal activity2.GIRK channel activity has an important role in physiological responses, including pain perception and memory modulation. Moreover, abnormal GIRK function is implicated in altering neuronal excitability and cell death that may be important in the pathophysiology of human diseases such as epilepsy, Down's syndrome, Parkinson's disease and drug addiction. GIRK channels may therefore prove to be valuable new therapeutic targets for treating these health problems2.GIRK1-GIRK2 heterotetramers are believed to be the predominant form of GIRK channels expressed in brain3.
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	0.1-10 uM
Reconstitution	Soluble in DMSO. It is recommended to prepare a <=10 mM stock in fresh DMSO prior to dilution in an aqueous solution. Centrifuge all products before handling (10000 x g 5 min).
Cas Number	1443246-62-5
Molecular Weight	328.32
Solubility	Soluble in DMSO. It is recommended to prepare a <=10 mM stock in fresh DMSO prior to dilution in an aqueous solution. Centrifuge all products before handling (10000 x g 5 min).
Target	GIRK1/2, GIRK1-containing GIRK channels
Activity	ML297 is a potent and selective activator of GIRK1/2 channels (EC50=160-233 nM)1,2. ML-297 is selective for GIRK1/2 over GIRK1/3 and GIRK1/4 heteromers (with EC50 of 914 nM and 887 nM, respectively), and inactive on non-GIRK1-containing channels1-2. Active in vivo3.
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 Cited Application: Electrophysiology Chemical Name: 1-(3,4-difluorophenyl)-3-(5-methyl-2-phenylpyrazol-3-yl)urea

Purity	>99% (HPLC)
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: Store at -20°C for several months. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.

Product Manual	SDS

Reference	Wen, W. et al. (2013) Bioorg. Med. Chem. Lett. 23, 4562. Lüscher, C. and Slesinger, P.A. (2010) Nat. Rev. Neurosci. 11, 301. Rifkin, R.A. et al. (2019) Trends Pharmacol. Sci. 38, 378. Wen, W. et al. (2013) Bioorg. Med. Chem. Lett. 23, 4562. Lüscher, C. and Slesinger, P.A. (2010) Nat. Rev. Neurosci. 11, 301. Kaufmann, K. et al. (2013) ACS Chem. Neurosci. 4, 1278.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300221-1	M-215_10 mg	10 mg	$373		Add to Cart
BHB21300221-2	M-215_25 mg	25 mg	$742		Add to Cart
BHB21300221-3	M-215_5 mg	5 mg	$235		Add to Cart
BHB21300221-4	M-215_50 mg	50 mg	$1184		Add to Cart

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