GSK561679 free base · Synonyms: Verucerfont

Verucerfont is a corticotropin-releasing factor receptor 1 antagonist.

For research use only. Not for human or veterinary use.

Target CRFR

Research area Neurological Disease Endocrinology

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK561679 structure

CAS No.: 885220-61-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 498.00	BP-02097-25mg	In stock	Get quote
50 mg	USD 989.00	BP-02097-50mg	In stock	Get quote
100 mg	USD 1,650.00	BP-02097-100mg	In stock	Get quote
250 mg	USD 2,380.00	BP-02097-250mg	In stock	Get quote
500 mg	USD 2,850.00	BP-02097-500mg	In stock	Get quote
1 g	Inquire	BP-02097-1g	In stock	Inquire

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Description

Verucerfont (GSK561679) is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.

Biological activity

In Vivo Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316?311, and pexacerfont (P<0.001 for all comparisons collapse across time-points); the latter three treatments in turn do not differ from each other. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, P<0.001). Accordingly, detailed Post hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6?h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline)

Identifiers

SMILES: CC[C@H](NC1=CC(C)=NC2=C(C(C)=NN12)C1=C(C)C=C(OC)C=C1)C1=NC(C)=NO1
InChIKey: VKHVAUKFLBBZFJ-SFHVURJKSA-N

Specifications

MW (average): 406.4808
Formula: C₂₂H₂₆N₆O₂
CAS No.: 885220-61-1
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 83.33 mg/mL

Documents

References

[1]. Schwandt ML, et al. The CRF1 Antagonist Verucerfont in Anxious Alcohol-Dependent Women: Translation of Neuroendocrine, But not of Anti-Craving Effects. Neuropsychopharmacology. 2016 Nov;41(12):2818-2829.

Same research area

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