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Dagrocorat (hydrochloride)

CAT: 0804-HY-16718A-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-16718A-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes) . Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis[1].
CAS Number
1044535-61-6
Product Name Alternative
PF-00251802 (hydrochloride)
UNSPSC
12352005
Target
Cytochrome P450; Glucocorticoid Receptor
Type
Reference compound
Related Pathways
Immunology/Inflammation; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Endocrinology; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/dagrocorat-hydrochloride.html
Purity
99.85
Solubility
DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O[C@@]1(C(F)(F)F)C[C@]2([H])[C@](C3=CC=C(C(NC(C=CC=N4)=C4C)=O)C=C3CC2)(CC1)CC5=CC=CC=C5.[H]Cl
Molecular Formula
C29H30ClF3N2O2
Molecular Weight
531.01
References & Citations
[1]Ripp SL, et al. In Vitro and In Vivo Investigation of Potential for Complex CYP3A Interaction for PF-00251802 (Dagrocorat), a Novel Dissociated Agonist of the Glucocorticoid Receptor. Clin Pharmacol Drug Dev. 2018;7 (3) :244-255.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CYP2; CYP3

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