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N-desmethyl Enzalutamide (N-desmethyl MDV 3100)

Katalog-Nr.GC32907

N-Desmethyl-Enzalutamid (N-Desmethyl MDV 3100) ist der aktive Metabolit von Enzalutamid. N-Desmethyl-Enzalutamid (N-Desmethyl MDV 3100) ist der aktive Metabolit von Enzalutamid. N-Desmethyl-Enzalutamid (N-Desmethyl MDV 3100) weist eine Ähnliche primÄre und sekundÄre Pharmakodynamik wie Enzalutamid auf und zirkuliert in ungefÄhr denselben Plasmakonzentrationen wie Enzalutamid.

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N-desmethyl Enzalutamide (N-desmethyl MDV 3100) Chemische Struktur

Cas No.: 1242137-16-1

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10mM (in 1mL DMSO)
122,00 $
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5mg
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10mg
166,00 $
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50mg
573,00 $
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100mg
974,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of N-desmethyl Enzalutamide (N-desmethyl MDV 3100)

N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

N-desmethyl Enzalutamide is an active metabolite that is thought to contribute to the clinical effects of Enzalutamide because it demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as Enzalutamide. The carboxylic acid metabolite is pharmacologically inactive and circulates at approximately 25 % lower plasma concentrations than Enzalutamide[1].

[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.

Chemical Properties of N-desmethyl Enzalutamide (N-desmethyl MDV 3100)

Cas No. 1242137-16-1 SDF
Canonical SMILES S=C(N1C2=CC(F)=C(C(N)=O)C=C2)N(C3=CC=C(C(C(F)(F)F)=C3)C#N)C(C(C)1C)=O
Formula C20H14F4N4O2S M.Wt 450.41
Löslichkeit DMSO : ≥ 48 mg/mL (106.57 mM) 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 of N-desmethyl Enzalutamide (N-desmethyl MDV 3100)

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2202 mL 11.101 mL 22.202 mL
5 mM 0.444 mL 2.2202 mL 4.4404 mL
10 mM 0.222 mL 1.1101 mL 2.2202 mL
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In vivo Formulation Calculator (Clear solution) of N-desmethyl Enzalutamide (N-desmethyl MDV 3100)

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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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