AN-2728
(Synonyms: 克立硼罗; AN-2728; PF-06930164) 目录号 : GC11472
A selective PDE4 inhibitor
Cas No.:906673-24-3
Sample solution is provided at 25 µL, 10mM.
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AN-2728 is an inhibitor of PDE4 with IC50 value of 0.49 μM [1]. PDE4 is a phosphodiesterase and plays an important role in the chronic inflammation associated with psoriasis and atopic dermatitis [2].
AN-2728 is a boron-containing, anti-inflammatory, topically administered compound that inhibits PDE4 activity and suppresses the release of TNF-α, IL-23, IL-12 and other cytokines [2]. In cell based assays, AN-2728 inhibited cytokine release of TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.54, 0.61, 0.83, 2.4 and 5.3 μM, respectively [1].
AN-2728 was well tolerated and had good therapeutic potential. AN-2728 is now in clinical development for the treatment of psoriasis and atopic dermatitis [2].
References:
[1]. Akama T, Baker SJ, Zhang YK, 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, 19(8): 2129-2132.
[2]. Nazarian R, Weinberg JM. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs, 2009, 10(11): 1236-1242.
| Cell experiment [1]: | |
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Cell lines |
Peripheral blood mononuclear cells (PBMCs) |
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Preparation method |
The solubility of this compound in DMSO is >12.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10 μM |
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Applications |
AN-2728 showed a broad range of potent cytokine release inhibition, such as TNF-α, IL-23, IL-12 and other cytokines. |
| Animal experiment [2]: | |
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Animal models |
Phorbol ester-induced mouse ear edema model |
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Dosage form |
1 mg/ear×2 |
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Application |
AN-2728 demonstrated in vivo efficacy in phorbol ester-induced mouse ear edema model by topical application. AN-2728 showed significant inhibition against the ear edema. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Akama T, Baker S J, Zhang Y K, 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[J]. Bioorganic & medicinal chemistry letters, 2009, 19(8): 2129-2132. | |
| Cas No. | 906673-24-3 | SDF | |
| 别名 | 克立硼罗; AN-2728; PF-06930164 | ||
| 化学名 | 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-5-yl)oxy)benzonitrile | ||
| Canonical SMILES | N#CC1=CC=C(OC2=CC=C3C(COB3O)=C2)C=C1 | ||
| 分子式 | C14H10BNO3 | 分子量 | 251.05 |
| 溶解度 | ≥ 12.55 mg/mL in DMSO, ≥ 94.4 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9833 mL | 19.9164 mL | 39.8327 mL |
| 5 mM | 0.7967 mL | 3.9833 mL | 7.9665 mL |
| 10 mM | 0.3983 mL | 1.9916 mL | 3.9833 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet