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AR-A 2

Cat. No. M29344
AR-A 2 Structure
Synonym:

AR-A 000002

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Quality Control & Documentation
Biological Activity

AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.

Chemical Information
Molecular Weight 448.6
Formula C27H36N4O2
CAS Number 220051-79-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Chan-Ping You, et al. Biomolecules. Androgen Receptor as an Emerging Feasible Biomarker for Breast Cancer

[2] Yuan Zhang, et al. Allergy. Advances and highlights in allergic rhinitis

[3] Ying Song, et al. Circ Res. Heterodimerization With 5-HT2BR Is Indispensable for β2AR-Mediated Cardioprotection

[4] Ayesha A Shafi, et al. Pharmacol Ther. Androgen receptors in hormone-dependent and castration-resistant prostate cancer

[5] Fabio V Fonseca, et al. Mol Cell. S-nitrosylation is required for β2AR desensitization and experimental asthma

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  Catalog
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Keywords: AR-A 2, AR-A 000002 supplier, 5-HT Receptor, inhibitors, activators


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