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BMS-763534

Cat. No. M7676

All AbMole products are for research use only, cannot be used for human consumption.

BMS-763534 Structure

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Quality Control & Documentation
Biological Activity

BMS-763534 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 = 0.26 & 0.4 nM against 150 pM ovine CRF for binding rat & human CRF-R1, respectively), potency (IC50 = 1.0 nM against 0.3 nM CRF-stimulated ATCH secretion from primary rat anterior pituitary cells), and selectivity, displaying little affinity toward porcine CRF-R2/CRF2 and 46 other receptor/channel/transporter proteins (IC50 >10 μM). BMS-763534 inhibits CRF-stimulated cAMP production in human Y-79 retinoblastoma cells in cultures (pA2 = 9.47) and exhibits anxiolytic efficacy in a rat situational anxiety model in vivo (0.5-3 mg/kg p.o.).

Chemical Information
Molecular Weight 414.83
Formula C18H21ClF2N4O3
CAS Number 1188407-40-0
Solubility (25°C) DMSO: 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Wen-Yuan Wu, et al. Corticotrophin-Releasing Factor Modulates the Facial Stimulation-Evoked Molecular Layer Interneuron-Purkinje Cell Synaptic Transmission in vivo in Mice

[2] Hong-Wei Wang, et al. Corticotrophin-Releasing Factor Modulates Cerebellar Purkinje Cells Simple Spike Activity in Vivo in Mice

[3] Naiyu Zheng, et al. A simplified and completely automated workflow for regulated LC-MS/MS bioanalysis using cap-piercing direct sampling and evaporation-free solid phase extraction

[4] Nicholas J Lodge, et al. Pharmacological and behavioral characterization of the novel CRF1 antagonist BMS-763534

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Keywords: BMS-763534 supplier, inhibitors, activators

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