2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. GSK-2881078

GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness.

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GSK-2881078

GSK-2881078 Chemische Struktur

CAS. Nr. : 1539314-06-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 5 publication(s) in Google Scholar

GSK-2881078 Related Antibodies

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Beschreibung

GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness[1][2][3][4].

In Vitro

GSK-2881078 has EC50s of 4.44 μM and 3.99 × 10−3 μM for reporter gene of androgen inducible yeast and PC3(AR)2 cells (human prostate carcinoma cell), respectively[4].
GSK-2881078 (10−5-10 μM, 24 h) stimulates reporter gene expression dose-dependently in the PC3(AR)2, increasing the relative luminescence units from 140% to 17340%[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK-2881078 Related Antibodies
Klinische Studie
Molekulargewicht

330.33

Formel

C14H13F3N2O2S
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(C(F)(F)F)C2=C(N([C@H](C)CS(=O)(C)=O)C=C2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : ≥ 33 mg/mL (99.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0273 mL 15.1364 mL 30.2728 mL
5 mM 0.6055 mL 3.0273 mL 6.0546 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Reinheit & Dokumentation

Purity: 99.42%

SDS (643 KB)

COA (254 KB) HNMR (193 KB) LCMS (104 KB)

Handling Instructions (2659 KB)
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0273 mL 15.1364 mL 30.2728 mL 75.6819 mL
5 mM 0.6055 mL 3.0273 mL 6.0546 mL 15.1364 mL
10 mM 0.3027 mL 1.5136 mL 3.0273 mL 7.5682 mL
15 mM 0.2018 mL 1.0091 mL 2.0182 mL 5.0455 mL
20 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7841 mL
25 mM 0.1211 mL 0.6055 mL 1.2109 mL 3.0273 mL
30 mM 0.1009 mL 0.5045 mL 1.0091 mL 2.5227 mL
40 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
50 mM 0.0605 mL 0.3027 mL 0.6055 mL 1.5136 mL
60 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2614 mL
80 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9460 mL
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GSK-2881078 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK-28810781539314-06-1GSK2881078GSK 2881078Androgen Receptormuscle weaknessCachexiaSARMyeastPC3(AR)2Inhibitorinhibitorinhibit

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