2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor
  3. Glucocorticoid Receptor
  4. ZK 216348

ZK 216348  (Synonyms: (+)-ZK 216348)

Cat. No.: HY-123352 Purity: 98.59%
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ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.

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

ZK 216348 Chemical Structure

ZK 216348 Chemical Structure

CAS No. : 669073-68-1

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5 mg USD 350 In-stock
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25 mg USD 1120 In-stock
50 mg USD 1750 In-stock
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Based on 1 publication(s) in Google Scholar

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ZK 216348 Related Antibodies

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Description

ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects[1][2].

IC50 & Target

IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor)[1]
In Vitro

In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC50 of 89 nM and 52 nM, respectively[1].
Participation of an active GR in the antiinflammatory response of ZK 216348 is further investigated in Caco-2 cells, where the TNF-α-induced expression of the proinflammatory cytokine IL-8 is suppressed in the presence of ZK 216348[2].

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

ZK 216348 Related Antibodies
In Vivo

ZK 216348 (1-30  mg/kg; subcutaneous injection; for 24 hours; NMRI mice and Wistar rats) treatment inhibits ear edema in both mice and rats. A markedly superior side-effect profile is found in ZK 216348 with regard to increases in blood glucose, spleen involution, and, to a lesser extent, skin atrophy[1].

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

Animal Model: NMRI mice (26-28 g) and Wistar rats (140-160 g) injection with Croton oil[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg and 30  mg/kg
Administration: Subcutaneous injection; for 24 hours
Result: Inhibited ear edema in mice and rats.
Molecular Weight

476.45

Formula

C24H23F3N2O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CC=C(C=C2C(C)=NO1)NC(C(C(F)(F)F)(O)CC(C)(C3=C4C(CCO4)=CC=C3)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (419.77 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 2.0989 mL 10.4943 mL 20.9886 mL
5 mM 0.4198 mL 2.0989 mL 4.1977 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
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 (sealed storage, away from moisture and light). 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 2.0989 mL 10.4943 mL 20.9886 mL 52.4714 mL
5 mM 0.4198 mL 2.0989 mL 4.1977 mL 10.4943 mL
10 mM 0.2099 mL 1.0494 mL 2.0989 mL 5.2471 mL
15 mM 0.1399 mL 0.6996 mL 1.3992 mL 3.4981 mL
20 mM 0.1049 mL 0.5247 mL 1.0494 mL 2.6236 mL
25 mM 0.0840 mL 0.4198 mL 0.8395 mL 2.0989 mL
30 mM 0.0700 mL 0.3498 mL 0.6996 mL 1.7490 mL
40 mM 0.0525 mL 0.2624 mL 0.5247 mL 1.3118 mL
50 mM 0.0420 mL 0.2099 mL 0.4198 mL 1.0494 mL
60 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8745 mL
80 mM 0.0262 mL 0.1312 mL 0.2624 mL 0.6559 mL
100 mM 0.0210 mL 0.1049 mL 0.2099 mL 0.5247 mL
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ZK 216348 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:

ZK 216348669073-68-1(+)-ZK 216348ZK216348ZK-216348Glucocorticoid ReceptorNonsteroidalantiinflammatorytransactivation-mediatedside effectsprogesteronemineralocorticoidInhibitorinhibitorinhibit

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