A non-steroidal selective glucocorticoid receptor modulator; contradictory results for binding affinity of CpdA compared with dexamethasone

CpdA – 25 mg

Brand:
Cayman
CAS:
14593-25-0
Storage:
-20
UN-No:
Non-Hazardous - /

CpdA is a non-steroidal selective glucocorticoid receptor modulator.{33998} It is an aziridine precursor that can infiltrate cells and is translocated to the nucleus.{33998,33996} It inhibits glucocorticoid receptor dimerization, which prevents transcription of gene targets such as NF-κB and subsequent cytokines through transrepression.{33997} Studies have shown contradictory results for binding affinity of CpdA compared with dexamethasone (Item No. 11015) that were either higher (4-fold, IC50 = 6.4 nM and 25.9 nM, respectively, in L929sA cells) or lower (63-fold, Kd = 81.8 nM and 1.29 nM, respectively, in BWTG3 cells) in whole cell binding assays.{33996,33997}  

 

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Description

A non-steroidal selective glucocorticoid receptor modulator; contradictory results for binding affinity of CpdA compared with dexamethasone, either higher (4-fold, IC50 = 6.4 nM and 25.9 nM, respectively) or lower (63-fold, Kd = 81.8 nM and 1.29 nM, respectively) in whole cell binding assays

Formal name: 4-[1-chloro-2-(methylamino)ethyl]-phenol 1-acetate, monohydrochloride

Synonyms:  Compound A

Molecular weight: 264.1

CAS: 14593-25-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Glucocorticoids & Mineralocorticoids||Research Area|Immunology & Inflammation

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