ZK168281
Based on 2 publication(s) in Google Scholar
ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
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- Reinheit: 98.0%
- CAS. Nr.: 186371-96-0
- Formel: C32H46O5
- Molecular Weight:510.70
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Speicherung:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ZK168281
More
Biologische Aktivität
Kd: 0.1 nM (VDR)[1]
ZK168281 resembles more the mouse constitutive androstane receptor (CAR) inverse agonist Androstanol in its ability to recruit corepressor (CoR) proteins. A salt bridge between the CoR and a conserved lysine in helix 4 of the nuclear receptor (NR) is central to this interaction, but also helix 12 was stabilized by direct contacts with residues of the CoR. Fixation of helix 12 in the antagonistic/inverse agonistic conformation prevents an energetically unfavorable free floatation of the C terminus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 186371-96-0
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Appearance Solid
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Molecular Weight 510.70
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Formel C32H46O5
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Color White to off-white
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SMILES
O=C(OCC)/C=C/C1([C@H](O)/C=C/[C@H]([C@H]2CC[C@@]3([H])/C(CCC[C@]23C)=C/C=C4C([C@@H](O)C[C@H](O)C\4)=C)C)CC1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Front Pharmacol
Emodin Protects Sepsis Associated Damage to the Intestinal Mucosal Barrier Through the VDR/ Nrf2 /HO-1 Pathway. [Abstract]2021 Dec 20;12:724511 PMID: 34987380 -
Biochim Biophys Acta Gen Subj
Stage-dependent association of Vitamin D receptor with macrophage polarization in allergic rhinitis. [Abstract]2026 Jun 2;1870(9):130965. PMID: 42235895
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (195.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9581 mL | 9.7905 mL | 19.5810 mL | 48.9524 mL |
| 5 mM | 0.3916 mL | 1.9581 mL | 3.9162 mL | 9.7905 mL | |
| 10 mM | 0.1958 mL | 0.9790 mL | 1.9581 mL | 4.8952 mL | |
| 15 mM | 0.1305 mL | 0.6527 mL | 1.3054 mL | 3.2635 mL | |
| 20 mM | 0.0979 mL | 0.4895 mL | 0.9790 mL | 2.4476 mL | |
| 25 mM | 0.0783 mL | 0.3916 mL | 0.7832 mL | 1.9581 mL | |
| 30 mM | 0.0653 mL | 0.3263 mL | 0.6527 mL | 1.6317 mL | |
| 40 mM | 0.0490 mL | 0.2448 mL | 0.4895 mL | 1.2238 mL | |
| 50 mM | 0.0392 mL | 0.1958 mL | 0.3916 mL | 0.9790 mL | |
| 60 mM | 0.0326 mL | 0.1632 mL | 0.3263 mL | 0.8159 mL | |
| 80 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6119 mL | |
| 100 mM | 0.0196 mL | 0.0979 mL | 0.1958 mL | 0.4895 mL |
ZK168281 Related Classifications
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