1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor
  2. Glucocorticoid Receptor
  3. (-)-ZK 216348

(-)-ZK 216348 是 (+)-ZK 216348 (HY-123352) 的对映异构体。(+)-ZK 216348 是一种非甾体选择性糖皮质激素受体 (glucocorticoid receptor) 激动剂,其 IC50 为 20.3 nM。ZK 216348 还与孕激素 (Prednisolone) 和盐皮质激素 (mineralocorticoid receptor) 受体结合,IC50 分别为 20.4 nM 和 79.9 nM。ZK 216348 具有与 Prednisolone 相似的抗炎活性,并且其副作用更少。

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(-)-ZK 216348 Chemical Structure

(-)-ZK 216348 Chemical Structure

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规格 价格 是否有货 数量
1 mg ¥1454
In-stock
5 mg ¥3200
In-stock
10 mg ¥5200
In-stock
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100 mg   询价  

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Customer Review

Other Forms of (-)-ZK 216348:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(-)-ZK 216348 is the enantiomer of (+)-ZK 216348 (HY-123352). (+)-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]

体外研究
(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].

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

体内研究
(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].

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

分子量

476.45

Formula

C24H23F3N2O5

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 230 mg/mL (482.74 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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.

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Inquiry Information

产品名称:
(-)-ZK 216348
目录号:
HY-123352A
需求量: