ZK 216348 (Synonyms: (+)-ZK 216348)

Name: ZK 216348
Brand: MedChemExpress
SKU: HY-123352
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製品番号: HY-123352 純度: 99.93%: Data Sheet SDS COA 取扱説明書
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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.

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ZK 216348 構造式

CAS 番号 : 669073-68-1

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 367	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 367	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$350	在庫あり	Estimated Time of Arrival: December 31
10 mg	$560	在庫あり	Estimated Time of Arrival: December 31
25 mg	$1120	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1750	在庫あり	Estimated Time of Arrival: December 31
100 mg	$2800	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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Based on 0 publication(s) in Google Scholar

Other Forms of ZK 216348:

(-)-ZK 216348 在庫あり

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•関連タンパク質:

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製品説明

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
HFF	EC₅₀	91 1 Compound: 2a, ZK-216348	Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay	[PMID: 17181172]
HeLa	EC₅₀	> 2000 1 Compound: 2a, ZK-216348	Activation of MMTV in HeLa cells measured by luciferase activity Activation of MMTV in HeLa cells measured by luciferase activity	[PMID: 17181172]
HeLa	EC₅₀	>2 3 Compound: 2a, ZK-216348	Activation of MMTV in HeLa cells measured by luciferase activity Activation of MMTV in HeLa cells measured by luciferase activity	[PMID: 17181172]
HFF	IC₅₀	59 1 Compound: 2a, ZK-216348	Inhibition of IL1-stimulated IL6 production in HFF cells Inhibition of IL1-stimulated IL6 production in HFF cells	[PMID: 17181172]
HFF	EC₅₀	91 1 Compound: 2a, ZK-216348	Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay	[PMID: 17181172]
HFF	EC₅₀	91 1 Compound: 2a, ZK-216348	Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay	[PMID: 17181172]
HFF	IC₅₀	59 1 Compound: 2a, ZK-216348	Inhibition of IL1-stimulated IL6 production in HFF cells Inhibition of IL1-stimulated IL6 production in HFF cells	[PMID: 17181172]
HeLa	EC₅₀	> 2000 1 Compound: 2a, ZK-216348	Activation of MMTV in HeLa cells measured by luciferase activity Activation of MMTV in HeLa cells measured by luciferase activity	[PMID: 17181172]

体外実験

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.

体内実験

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.

分子量

476.45

分子式

C₂₄H₂₃F₃N₂O₅

CAS 番号

669073-68-1

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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)

溶剤 & 溶解度

体外:

DMSO : ≥ 200 mg/mL (419.77 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	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

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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 7.5 mg/mL (15.74 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.93%

Select Batch:

データシート (277 KB) SDS (252 KB)

COA (253 KB) HNMR (278 KB) RP-HPLC (247 KB) LCMS (137 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Schäcke H, et al. Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Proc Natl Acad Sci U S A. 2004 Jan 6;101(1):227-32. [Content Brief]

[2]. Reuter KC, et al. Selective glucocorticoid receptor agonists for the treatment of inflammatory bowel disease: studies in mice with acute trinitrobenzene sulfonic acid colitis. J Pharmacol Exp Ther. 2012 Apr;341(1):68-80. [Content Brief]

Complete Stock Solution Preparation Table

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

ZK 216348 Related Classifications

Inflammation/Immunology Endocrinology

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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ZK 216348 (Synonyms: (+)-ZK 216348)

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Other Forms of ZK 216348:

ZK 216348 関連抗体

おすすめ

•関連スクリーニングライブラリ:

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純度とドキュメンテーション

参考文献

カスタマーレビュー

ZK 216348 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ZK 216348 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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