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Cat. No.: HY-145906

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D4R antagonis-2

D4R antagonist-2 is a potent and selective D4R antagonist with an IC₅₀ of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease.

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

CAS No.: 2846077-70-9
Formula: C₂₁H₂₃ClF₂N₂O₂
Molecular Weight:408.87

Storage:

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

Data Sheet (269 KB)

D4R antagonis-2 Chemical Structure

CAS No.: 2846077-70-9

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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
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

D₄ Receptor

6.87 μM (IC₅₀)

All Dopamine Receptor Isoforms :

In Vitro

D4R antagonist-2 (compound 11a) shows good activity with an K_i of 299.4 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

D4R antagonist-2 displays very favorable in vitro PK parameters and is brain pentrent (K_p=2.9)^[1]. b>Pharmacokinetic Parameters of D4R antagonist-2 in rats^[1].

rat cassette (0.25 mpk)	11a
CL (ml/min/kg)	22.0
T_1/2 (h)	4.4
C₀ (ng/ml)	91
V_ss (L/kg)	5.5
AUC (h*ng/mL)	747

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

rats^[1]
Dosage:
Administration:

i.v.
Result:

Displayed very favorable in vitro PK parameters and was brain pentrent (K_p=2.9).

Chemical Information

CAS No. 2846077-70-9
Molecular Weight 408.87
Formula C₂₁H₂₃ClF₂N₂O₂
SMILES

CC1=C(C=CC=C1NC(CN2CCC(CC2)OCC3=CC=C(C(F)=C3)F)=O)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 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]. Tolentino KT,et al. Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists. Bioorg Med Chem Lett. 2022; 61:128615. [Content Brief]

Calculators

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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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