| Size | Price | Stock | Qty |
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| Targets |
ZK216348 targets the glucocorticoid receptor (GR), a nuclear receptor that regulates gene transcription in response to glucocorticoids. As a selective GR agonist, it mimics the anti-inflammatory effects of corticosteroids but is designed to have a more favorable side-effect profile. It also binds to progesterone and mineralocorticoid receptors, though with lower affinity.
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| ln Vitro |
ZK 216348 inhibits TNF-α and IL-12 in human peripheral blood mononuclear cells (PBMC) at IC50 values of 89 nM and 52 nM, respectively [1]. In Caco-2 cells, the role of active GR in ZK 216348's anti-inflammatory response was investigated further. ZK 216348 was found to inhibit the expression of IL-8, a pro-inflammatory cytokine that is induced by TNF-α [2].
In vitro, ZK216348 acts as a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. It shows anti-inflammatory activity comparable to prednisolone. The compound's activity is assessed using receptor binding assays and functional assays measuring glucocorticoid receptor-mediated gene transactivation and transrepression. |
| ln Vivo |
In NMRI mice and Wistar rats, treatment with ZK 216348 (1–30 mg/kg; subcutaneous injection; 24 hours) reduced ear edema. Compared to other treatments, ZK 216348 has a much better adverse effect profile that includes elevated blood sugar, splenic degeneration, and, to a lesser degree, skin atrophy [1].
In vivo, ZK216348 has been studied for the treatment of experimental colitis. It has anti-inflammatory activity comparable to prednisolone for both systemic and topical application. The compound induces less transactivation-mediated side effects, suggesting a potentially improved safety profile compared to traditional glucocorticoids. |
| Enzyme Assay |
In vitro receptor binding assays for ZK216348 are performed using membrane preparations expressing human glucocorticoid, progesterone, and mineralocorticoid receptors. Radioligand competition binding assays are used to measure the compound's affinity for these receptors, and IC50 values are calculated from competition curves. Functional assays measure glucocorticoid receptor-mediated transcriptional activity.
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| Cell Assay |
In vitro cellular assays for ZK216348 are performed using cells expressing the glucocorticoid receptor, such as immune cells or reporter cell lines. Cells are treated with the compound, and glucocorticoid receptor-mediated gene expression is measured by qRT-PCR or reporter gene assays. Anti-inflammatory activity is assessed by measuring the inhibition of pro-inflammatory cytokine production.
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| Animal Protocol |
Animal/Disease Models: NMRI mice (26-28 g) and Wistar rats (140-160 g) injected with croton oil [1] Doses: 1 mg/kg, 3 mg/kg, 10 mg/kg and 30 mg/kg given Medication method: subcutaneous injection; 24-hour
Experimental Results: inhibit ear edema in mice and rats. In vivo animal experiments for ZK216348 are conducted in models of inflammatory diseases, such as experimental colitis. A typical protocol involves oral or topical administration of the compound to animals with induced colitis, followed by assessment of disease severity, histological analysis of colon tissues, and measurement of inflammatory markers. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of ZK216348 have been characterized in preclinical studies. The compound has a molecular weight of 476.45, molecular formula C24H23F3N2O5, and a purity of 99.93%. It is a nonsteroidal compound with a relative density of 1.39 g/cm3 (predicted). Further PK details are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
The toxicity profile of ZK216348 has been evaluated in preclinical studies. As a selective glucocorticoid receptor agonist, it is designed to induce less transactivation-mediated side effects compared to traditional glucocorticoids. Specific toxicity data, including organ-specific effects and dose-limiting toxicities, are typically assessed in standard toxicology studies to support its development as a therapeutic agent.
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| References |
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| Additional Infomation |
ZK216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with anti-inflammatory activity similar to prednisolone. It has been investigated for the treatment of inflammatory bowel disease (IBD). The compound is a research tool for studying glucocorticoid receptor-mediated signaling and inflammation.
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| Molecular Formula |
C24H23F3N2O5
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| Molecular Weight |
476.45
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| Exact Mass |
476.155
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| CAS # |
669073-68-1
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| Related CAS # |
(-)-ZK 216348
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| PubChem CID |
9805004
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.590
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| LogP |
4.39
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
845
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=NOC(=O)C2=C1C=C(C=C2)NC(=O)[C@](CC(C)(C)C3=CC=CC4=C3OCC4)(C(F)(F)F)O
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| InChi Key |
VRZVKIJRJRBQJT-HSZRJFAPSA-N
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| InChi Code |
InChI=1S/C24H23F3N2O5/c1-13-17-11-15(7-8-16(17)20(30)34-29-13)28-21(31)23(32,24(25,26)27)12-22(2,3)18-6-4-5-14-9-10-33-19(14)18/h4-8,11,32H,9-10,12H2,1-3H3,(H,28,31)/t23-/m1/s1
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| Chemical Name |
(2R)-4-(2,3-dihydro-1-benzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamide
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| Synonyms |
ZK-216348; ZK 216348; ZK216348
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~419.77 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2099 mL | 1.0494 mL | 2.0989 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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