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Dagrocorat hydrochloride (Synonyms: PF-00251802 hydrochloride)

Catalog No.GC63872

Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor.

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Dagrocorat hydrochloride Chemical Structure

Cas No.: 1044535-61-6

Size Price Stock Qty
5 mg
$765.00
In stock
10 mg
$1,260.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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].

Dagrocorat hydrochloride is metabolized by cytochrome P450 (CYP)3A to an N-oxide metabolite. Dagrocorat hydrochloride is a reversible inhibitor of several CYPs, such as CYP3A and CYP2D6[1].

[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.

Chemical Properties

Cas No. 1044535-61-6 SDF Download SDF
Synonyms PF-00251802 hydrochloride
Formula C29H30ClF3N2O2 M.Wt 531.01
Solubility DMSO : 100 mg/mL (188.32 mM; ultrasonic and warming and heat to 60°C) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.8832 mL 9.416 mL 18.832 mL
5 mM 0.3766 mL 1.8832 mL 3.7664 mL
10 mM 0.1883 mL 0.9416 mL 1.8832 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Reviews

Review for Dagrocorat hydrochloride

Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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