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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1044535-61-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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