- Nortadalafil
| AN-2728PDE4 inhibitor,anti-inflammatory compound |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.33%
- COA (Certificate Of Analysis)
- HPLC(Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | Peripheral blood mononuclear cells (PBMCs) |
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. |
Reacting condition | 10 μM |
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]: | |
Animal models | Phorbol ester-induced mouse ear edema model |
Dosage form | 1 mg/ear×2 |
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. |
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. |
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. | |
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| Cas No. | 906673-24-3 | SDF | Download SDF |
| Synonyms | AN2728;AN 2728 | ||
| Chemical Name | 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 | ||
| Formula | C14H10BNO3 | M.Wt | 251.05 |
| Solubility | ≥12.55 mg/mL in DMSO, ≥94.4 mg/mL in EtOH, <2.62 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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（第1张图和第2张图是经旋转后方向恰好相反的两张图，上矢状窦等静脉也显示了）
女患，70岁，大专毕业，我院退休药师。7-8年前患脑梗（具体不详）。记忆力差5-6年，近记忆为著，几次做饭后忘记关火，将炉具的台板（玻璃的）烧裂。近5-6年来，病人每年住院彻底检查治疗1次（主要是使用活血化瘀及营养脑细胞药）。平素，病人双耳听力略差，睡眠欠佳、便秘、尿频，偶从卧位坐起时视蒙。既往有时血压略高，未降压治疗。本次为“通血管”再来住院。查体：血压：140/80mmHg,双耳听力略差，近记忆力差，但智力（MMSE：26分)正常，颅神经未见异常，四肢肌力、感觉未见异常，植物神经未查，双掌颌反射（+），双下肢病理反射均阴性。血常规：淋巴细胞比率略高，余均正常；尿常规、心电图、癌胚抗原均正常；凝血四项：除凝血酶时间略长外均正常；生化全项：除总胆固醇略高外均正常；超声心动图：老年瓣退行性改变，左室舒张功能减退，房膜瘤可能。彩超：双侧颈动脉粥样硬化形成。头MRA:右大脑中动脉及其分支未显示。
问题：1MRI怎么会这样逍遥？病人无肢体瘫，生活自理如常人。
2为明确头MRA:右大脑中动脉及其分支未显示的病因和程度，除做DSA外，还需做什么？
3如不做DSA，给他订类药、阿斯匹林及活血化瘀的中药可不可以？
教。
版主laocao留言:
患者的年龄，病史，症状，辅助检查传上来，便于进一步讨论，谢谢！
