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Cat. No.: HY-U00189

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Sch412348

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.

For research use only. We do not sell to patients.

CAS No.: 377727-26-9
Formula: C₂₂H₂₁F₂N₉O
Molecular Weight:465.46

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

Sch412348 Chemical Structure

CAS No.: 377727-26-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

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]

All Adenosine Receptor Isoforms :

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. .

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.

Chemical Information

CAS No. 377727-26-9
Molecular Weight 465.46
Formula C₂₂H₂₁F₂N₉O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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