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BMK-C205

Chemical Structure : BMK-C205

CAS No.: 2950971-22-7

BMK-C205 (BMK-C 205)

Catalog No.: PC-21195Not For Human Use, Lab Use Only.

BMK-C205 (BMK-C 205) is a potent, selective corticotropin-releasing hormone receptor 1 (CRF1R) antagonist with IC50 of 74 nM in calcium mobilization assays, blocks hypothalamus-pituitary-adrenal (HPA) axis activation.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BMK-C205 (BMK-C 205) is a potent, selective corticotropin-releasing hormone receptor 1 (CRF1R) antagonist with IC50 of 74 nM in calcium mobilization assays, blocks hypothalamus-pituitary-adrenal (HPA) axis activation.
BMK-C205 displays >100-fold selectivity over CRF2R.
BMK-C205 exhibits minimal inhibition against five major CYP450 isoforms at a concentration of 10  μM.
BMK-C205 (30 mg/kg, orally administered for 3 days) shows in vivo antidepressant response in mice, without causing hyperactivity, significantly decreases adrenocorticotropic hormone (ACTH) and corticosterone (CORT) levels in treated mice.

Physicochemical Properties

M.Wt 488.43
Formula C23H30BrN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

8-(4-bromo-2,6-dimethoxyphenyl)-N-butyl-N-(cyclopropylmethyl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine

References

1. Hoyoung Kim, et al. Exp Mol Med. 2023 Sep 1. doi: 10.1038/s12276-023-01082-1.

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