Sch412348

Cat. No.: HY-U00189: FAQs
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Sch412348 is a potent competitive antagonist of the human adenosine A_2A receptor (K_i=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.

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Sch412348 Chemical Structure

CAS No. : 377727-26-9

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Adenosine A₁ receptor (A₁R) Adenosine A_2A receptor (A_2AR) Adenosine A_2B receptor (A_2BR) Adenosine A₃ receptor (A₃R)

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Description	Sch412348 is a potent competitive antagonist of the human adenosine A_2A receptor (K_i=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
IC₅₀ & Target	Ki: 0.6 nM (Adenosine A_2A receptor)^[1]
In Vitro	Sch412348 (SCH 412348) also completely antagonizes cAMP in cells expressing the recombinant human A_2A receptor. Sch412348 is determined to have K_B values of 0.3 nM, respectively at the A_2A receptor; the value are in good agreement with the K_i values determined in radioligand binding assays. A similar functional assay with A_2B receptor-expressing cells is used to demonstrate selectivity over A_2B receptors. In this assay, the K_B value for Sch412348 is 273 nM, indicating that Sch412348 is 910-fold selective for the A_2A receptor over the A_2B receptor^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Sch412348 Related Antibodies
In Vivo	Oral administration of Sch412348 (0.1-1 mg/kg) to rats potentiates 3,4-dihydroxy-L-phenylalanine (L-Dopa)-induced contralateral rotations after 6-hydroxydopamine lesions in the medial forebrain bundle and potently attenuates the cataleptic effects of haloperidol. Sch412348 (1 and 3 mg/kg) dose-dependently attenuates haloperidol-induced catalepsy 1 h [F(3,20)=3.9, p<0.05] and 4 h [F(3,20)=7.5, p<0.01] after dosing. Sch412348 [F(2,51) =10.6, p<0.01] (0.1-1 mg/kg) reduces immobility time in the mouse tail suspension test (TST) at 1 mg/kg. Sch412348 (SCH 412348) significantly increases activity levels in the mouse [F(4,27)=2.9, p<0.05]. Both the 0.3 and 3 mg/kg treatment groups are significantly more active than vehicle-treated mice. The 1 mg/kg group approached significance (p=0.052)^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	465.46
Formula	C₂₂H₂₁F₂N₉O
CAS No.	377727-26-9
SMILES	NC1=NC(N(CCN2CCN(C3=CC=C(F)C=C3F)CC2)N=C4)=C4C5=NC(C6=CC=CO6)=NN15
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (273 KB) Handling Instructions (2659 KB)
References	[1]. Hodgson RA, et al. Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent models of movement disorders and depression. J Pharmacol Exp Ther. 2009 Jul;330(1):294-303. [Content Brief]

Kinase Assay ^[1]	Receptor binding is performed using membranes prepared from cells with recombinant expression of adenosine receptors as follows: human A_2A and HEK 293, rat A_2A and Chinese hamster ovary, human and rat A₁ and Chinese hamster ovary, and human A₃ and HEK 293. Radioligand competition binding assays are performed in 96-well plates in a total assay volume of 200 μL using a final test drug concentration range of between 0.1 and 3 μM. Membranes are diluted in assay buffer, pH 7.4 (A₁ and A_2A, Dulbecco's phosphate-buffered saline with 10 mM MgCl₂; A₃, 50 mM Tris-HCl, 120 mM NaCl, 10 mM MgCl₂). To remove endogenous adenosine from the membrane preparations, 4 U/mL adenosine deaminase is added to the membranes, which are then incubated at room temperature for 15 min. Radioligand is added to a final concentration of 0.5 ([³H]SCH 58261, A_2A), 1 ([³H]DPCPX, A₁), or 0.25 ([¹²⁵I]AB-MECA, A₃) nM. Nonspecific binding is defined by adding 100 nM CGS 15923 (A_2A), 100 nM NECA (A₁), or 100 nM DPCPX (A₃). Plates are incubated at room temperature with agitation for 1.5 h (A_2A and A₁) or 2 h (A₃). Membranes are filtered onto Packard GF-B filter plates and washed in ice-cold assay buffer using a Brandel cell harvester to separate bound and free radioligand. The plates are dried before addition of 45 μL of Microscint 20 to each well. IC₅₀ values are determining by fitting the displacement curves using an iterative curve-fitting program. K_i values are calculated using the Cheng-Prusoff equation^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] Male CD rats weighing 200 to 240 g are used for catalepsy and hypolocomotion studies. Sch412348 is administered orally in 50% polyethylene glycol 400 at a dose volume of 3 to 5 mL/kg. Sch412348 is administered in a volume of 1 mL/kg s.c. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Hodgson RA, et al. Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent models of movement disorders and depression. J Pharmacol Exp Ther. 2009 Jul;330(1):294-303. [Content Brief]

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Sch412348377727-26-9Sch 412348Sch-412348Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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Sch412348

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