
- SB525334
- SB 431542
- LY2157299
- LY2109761
- SB-505124 hydrochloride
- SD-208
A 83-01ALK-5 inhibitor |
Sample solution is provided at 25 µL, 10mM.
































Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure

Description | A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 nM, 45 nM and 7.5 nM, respectively. | |||||
Targets | ALK5 | ALK4 | ALK7 | |||
IC50 | 12 nM | 45 nM | 7.5 nM |
Cell experiment [1]: | |
Cell lines | Mv1Lu and C2C12 cells |
Preparation method | The solubility of this compound in DMSO is > 21.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition | 0.01 ~ 10 μM; 1 hr |
Applications | In Mv1Lu cells, A-83-01 reduced the level of TGF-β-induced transcription in a concentration-dependent manner, with the IC50 value of 25 nM. On the other hand, for BMP-induced transcriptional activity in C2C12 cells, A-83-01 showed no effect at the dose of 1 μM. However, at the concentrations over 3 μM, A-83-01 slightly suppressed the transcriptional activity induced by BMP4. |
References: [1]. Tojo M, Hamashima Y, Hanyu A, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer science, 2005, 96(11): 791-800. |

A 83-01 Dilution Calculator
calculate

A 83-01 Molarity Calculator
calculate
Cas No. | 909910-43-6 | SDF | Download SDF |
Synonyms | A83-01;A-83-01 | ||
Chemical Name | 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide | ||
Canonical SMILES | CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5 | ||
Formula | C25H19N5S | M.Wt | 421.52 |
Solubility | ≥21.1 mg/mL in DMSO, ≥9.82 mg/mL in EtOH with ultrasonic and warming, <2.29 mg/ml="" in="" h2o="">2.29> | 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. |
A 83-01 is a small-molecule inhibitor of activin receptorlike kinase (ALK)-5 with IC50 value of 12 nM [1].
A 83-01 inhibited 68% of the transcriptional activation induced by ALK-5 at concentration of 1 μM in Mv1LuR4-2 cells that transfected with luciferase reporter gene and constitutively active ALK-5. In cells transfected with luciferase reporter gene only, A 83-01 treatment inhibited the activity of ALK-5 induced by TGF-β (IC50 value was 12 nM) but not BMP. A 83-01 also showed inhibition on the activity of ALK-4 and ALK-7 in R4-2 cells with IC50 values of 45 and 7.5 nM, respectively. For other ALK receptors such as ALK-1, 2, 3 and 6, A 83-01 showed weak inhibition. Besides that, A 83-01 was proved to reduce the cell growth inhibition [1].
References:1.Tojo M, Hamashima Y, Hanyu A, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer science, 2005, 96(11): 791-800.
ebiomall.com






>
>
>
>
>
>
>
>
>
>
>
>
深夜,保姆觉得无聊就想去楼下看电视。但是她看不了,因为楼下没有电视(因为孩子的父母不希望他们的孩子看太多垃圾)。她就打电话给孩子的父母,问是否可以在他们的卧室看电视,当然孩子的父母同意了。
但保姆又想要最后一个请求。
她问是否可以用毯子或者衣服盖住那小丑雕像,因为那使她感到很害怕。
电话沉默了一会。
(此时爸爸在和保姆通话)
他说:带孩子离开房间……
我们将会叫警察……我们从来没有什么小丑雕像。
那小丑很可能是一个从监狱逃出来的杀人犯。
电话里沉默了一会儿。
(正在跟保姆通话的孩子的父亲)说:带上孩子们,离开房子……我们会通知警察……我们没有一个小丑雕像……
孩子们和保姆被小丑谋杀了。
结果是,小丑是一个从监狱里逃出来的杀人犯。
如果你不在5分钟内转发这个贴子,这个小丑在凌晨3点时将会拿着刀站在你的床前。
我在这里发了,这就是恶魔般的小丑没有杀我的原因
慢性心功能不全的病因的防治
风湿性心瓣膜病在我国仍属慢性心力衰竭的常见病因。应用青霉素治疗链球菌感染,已使风湿热和风湿性心瓣膜病在发达国家基本绝迹。择期手术治疗风湿性心瓣膜病,有效地控制高血压以及积极防治冠脉病变与心肌缺血等病因治疗;消除心力衰竭的诱因如控制感染、避免体力过劳和精神应激等。可预防心力衰竭的发生。
收缩性心力衰竭的治疗
1、减轻心脏负荷包括减少体力活动和精神应激。严重者宜绝对卧床休息,在心功能逐步改善过程中,适当下床活动,以免卧床休息过久并发静脉血栓形成或肺炎。此外,应注意解除精神负担,必要时给予小量镇静剂。
2、限制钠盐摄入适当限制日常饮食中的钠盐摄入量,食盐量2~5g,忌盐腌制食物。应用利尿剂引起大量利尿时,钠盐限制不宜过严,以免发生低钠血症。
3、利尿剂的应用利尿剂通过抑制肾小管不同部位Na+重吸收,或增加肾小球Na+滤过,增进水、Na+排出,从而降低心室充盈压,减轻肺循环和(或)体循环瘀血所致临床症状,其疗效肯定,但对心力衰竭整体过程的影响(如生存率等)不明,长期应用利尿剂理论上可能产生下列不良作用:①降低心排血量,从而激活RAS,血浆肾素和醛固酮增高。②导致低钾血症。③降低糖耐量。④导致高尿酸血症。⑤导致高脂血症。⑥导致室性心律失常。目前利尿剂属治疗心力衰竭伴水、钠潴留患者的一线药物,大多与其他心力衰竭治疗药物(如地高辛、ACE抑制剂)联合应用,单纯舒张性心力衰竭者利尿剂宜慎用。
4、正性肌力药物的应用由于慢性心力衰竭患者心肌收缩性减弱,改善心肌收缩功能曾被认为是心力衰竭的首要治疗。正性肌力药物能使心室功能曲线左上移,增加每搏作功,降低心室充盈压,从而使扩大的心脏缩小。虽然在增加心肌收缩的同时也增加心肌能量消耗,但扩大的心脏缩小后,其心肌氧耗和冠脉血供分别较心脏扩大时降低和改善,心肌能量供需的不平衡因而并不加重,甚至有所减轻。正性肌力药减轻症状、改善运动耐量和心功分级的效果明显,但多中心随机对照慢性心力衰竭患者长期临床治疗试验结果表明除洋地黄外,大多具有增高病死率与室性心律失常发生率的倾向。ACEI则不仅减轻症状、改善运动耐量和心功分级的效果更显著,且能降低病死率和病残率。因而大多数临床医师选用ACEI作为与利尿剂联用,以治疗窦性心律的慢性心力衰竭患者。
西安医专附属医院 内科心血管专家杜志桢,1976年毕业于西安医科大学医疗系。2002年晋升为主任医师,从事内科心血管疾病临床工作30余年。对冠心病、心肌缺血、心绞痛及高血压病等治疗,积累了丰富的临床经验。对心脑血管相关疾病如高脂血症、心肾功能不全的治疗亦有较成熟经验。曾担任西安医学会心血管病学会委员。前列腺素E1治疗急性肾衰获市新技术项目奖(94年)。有关心血管病近10余篇论文公开发表。为东南大学《现代医学》杂志编委。
职称:主任医师
医院科室:西安医学专科学校附属医院心内科
擅长:冠心病、高血压病、心肌病、心肌炎、心力衰竭、心律失常、心肌梗塞、心肌缺血、心绞痛治疗。
治疗病名:冠心病、心梗、顽固心律失常、高血压心脏病、心衰、心绞痛、肺心病、风心病高脂血症、动脉硬化等。展开

