2. Vitamin D Related/Nuclear Receptor
  3. VD/VDR
  4. ZK168281

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.

For research use only. We do not sell to patients.

ZK168281 Chemical Structure

ZK168281 Chemical Structure

CAS No. : 186371-96-0

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1 mg USD 950 In-stock
5 mg USD 1950 In-stock
10 mg USD 3200 In-stock
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Based on 1 publication(s) in Google Scholar

ZK168281 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE ZK168281

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

Kd: 0.1 nM (VDR)[1]
In Vitro

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.

ZK168281 Related Antibodies
Molecular Weight

510.70

Formula

C32H46O5
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9581 mL 9.7905 mL 19.5810 mL
5 mM 0.3916 mL 1.9581 mL 3.9162 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.43%

COA (246 KB) RP-HPLC (176 KB)

Handling Instructions (2659 KB)
References

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
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ZK168281 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:

ZK168281186371-96-0ZK 168281ZK-168281VD/VDRVitamin DVitamin D receptorVDRCoAinteractionNR25-carboxylicesterInhibitorinhibitorinhibit

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