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首页 / 抑制剂/激动剂 / 代谢酶 / PDE / Crisaborole/克立硼罗

Crisaborole/克立硼罗 {[allProObj[0].p_purity_real_show]}

货号：A203325 同义名： AN-2728; PF-06930164

AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity with an IC50 of 0.49 μM and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.

Crisaborole/克立硼罗 化学结构 CAS号：906673-24-3
Crisaborole/克立硼罗 化学结构
CAS号：906673-24-3
Crisaborole/克立硼罗 3D分子结构
CAS号：906673-24-3
Crisaborole/克立硼罗 化学结构 CAS号：906673-24-3
Crisaborole/克立硼罗 3D分子结构 CAS号：906673-24-3
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Crisaborole/克立硼罗 纯度/质量文件 产品仅供科研

货号：A203325 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

更多 >
产品名称 PDE ↓ PDE1 ↓ PDE10A ↓ PDE2 ↓ PDE3 ↓ PDE4 ↓ PDE5 ↓ PDE6 ↓ 其他靶点 纯度
Doxofylline ✔ 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

 		96%
7-(2,3-Dihydroxypropyl)theophylline ✔ 98%
Aminophylline +

PDE, IC50: 0.12 mM

 		98+%
Anagrelide HCl ✔ 99%+
Irsogladine ✔ mAChR,AChR 99%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

 		99%+
Dipyridamole ✔ 98%
Luteolin +

PDE1, Ki: 15.0 μM

 		++

PDE2, Ki: 6.4 μM

 		+

PDE3, Ki: 13.9 μM

 		+

PDE4, Ki: 11.1 μM

 		+

PDE5, Ki: 9.5 μM

 		98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

 		99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

 		97%
Milrinone ++

PDE2, IC50: 5.2 μM

 		++

PDE3, IC50: 2.1 μM

 		ATPase 99%
Pimobendan ++

PDE3, IC50: 0.32 μM

 		98%
Cilostazol ++

PDE3, IC50: 0.2 μM

 		98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

 		99% (HPLC)
Apremilast +++

PDE4, IC50: 74 nM

 		98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

 		98+%
Roflumilast ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

 		99%
Rolipram +++

PDE4B, IC50: 130 nM

 		99%+
Cilomilast +++

HPDE4, IC50: 120 nM

LPDE4, IC50: 100 nM

 		99%
Fenspiride HCl +

PDE3, pIC50: 3.44

 		+

PDE4, pIC50: 4.16

 		99% (HPLC)
Avanafil ++++

PDE5, IC50: 1 nM

 		98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

 		98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

 		98%
Icariin ++

PDE5, IC50: 0.432 μM

 		98%
Sildenafil ✔ +++

PDE6, IC50: 33 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Crisaborole/克立硼罗 生物活性

描述 Cyclic nucleotide phosphodiesterases(PDEs) are enzymes that regulate the cellular levels of the second messengers, cAMP and cGMP, by controlling their rates of degradation. The single known mechanism for removing cellular 3′, 5′-cyclic adenosine monophosphate (cAMP), a critical intracellular messenger for regulation of immune responses, is through degradation to AMP via the PDE family of enzymes. The four phosphodiesterase 4 (PDE4) enzymes (A/B/C/D) play a critical role in degrading cAMP in lymphocytes, endothelial cell, keratinocytes and smooth muscle cells. The long forms of each PDE4 subtype can be phosphorylated by PKA and ERK phosphorylation. AN-2728 is a topically administered, boron-containing, anti-inflammatory compound, with an IC50 of 0.49 μM that inhibits PDE4 activity and thereby suppresses the release of TNF-alpha (IC50 0.54 μM), IL-2 (IC50 0.61 μM), IFN-γ (IC50 0.83 μM) and other cytokines. In a vivo study, ear edema mice were dosed 1 mg/ear × 2 and 78% inhabitation rate of AN-2728 was achieved, which suggested that these compounds have good anti-inflammatory activity. In a vitro study, AN-2728 at 10 nM reacted with ATP substrate (40 nM) and result showed AN2728 inhibit the major isoforms of PDE4 in vitro, suggesting that AN-2728 is an efficient PDE4 inhibitor.
作用机制 AN2728 competes with cAMP to inhibit the PDE4B1-catalytic domain.

Crisaborole/克立硼罗 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03645057 Atopic Dermatitis Phase 3 Not yet recruiting August 31, 2020 -
NCT03250663 Mild to Moderate Atopic Dermat... 展开 >>itis 收起 << Phase 1 Recruiting August 1, 2019 United States, North Carolina ... 展开 >> Wake Forest University Heath Sciences Recruiting Winston-Salem, North Carolina, United States, 27157 收起 <<
NCT03770858 - Not yet recruiting December 2019 United States, Illinois ... 展开 >> Northwestern University Not yet recruiting Chicago, Illinois, United States, 60611 Contact: Dermatology CTU    312-503-5944    NUdermatologyCTU@northwestern.edu 收起 <<

Crisaborole/克立硼罗 参考文献

[1]Nazarian R, Weinberg JM. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs. 2009 Nov;10(11):1236-42.

[2]Akama T, Baker SJ, et al. Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2129-32.

Crisaborole/克立硼罗 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.98mL

0.80mL

0.40mL

19.92mL

3.98mL

1.99mL

39.83mL

7.97mL

3.98mL

Crisaborole/克立硼罗 技术信息

CAS号906673-24-3
分子式C14H10BNO3
分子量 251.05
SMILES Code OB1OCC2=C1C=CC(OC1=CC=C(C=C1)C#N)=C2
MDL No. MFCD17169940
别名 AN-2728; PF-06930164; Crisaborole, Eucrisa
运输蓝冰
InChI Key USZAGAREISWJDP-UHFFFAOYSA-N
Pubchem ID 44591583
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Crisaborole | 906673-24-3 | AN-2728 | PF-06930164 | AN2728 | AN 2728 | PF06930164 | PF 06930164 | PF-06930164 | PDE Inhibitor | Metabolic Enzyme/Protease | Phosphodiesterase (PDE) | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Crisaborole/克立硼罗 纯度/质量文件 | Crisaborole/克立硼罗 亚型比较 | Crisaborole/克立硼罗 生物活性 | Crisaborole/克立硼罗 临床数据 | Crisaborole/克立硼罗 参考文献 | Crisaborole/克立硼罗 实验方案 | Crisaborole/克立硼罗 技术信息

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