Home > TGF-beta/Smad & > Type II TGFβ receptor inhibitor

Type II TGFβ receptor inhibitor

ITD 1,ITD-1,ITD1

ITD1 is a selective inhibitor of TGF-β signaling (IC50 = 0.85 μM) which acts by clearing the type II TGFβ receptor from the cell surface.

目录号
EY2031
EY2031
EY2031
EY2031
纯度
99.24%
99.24%
99.24%
99.24%
规格
1 mg
5 mg
10 mg
50 mg
原价
360
890
1180
4300
售价
360
890
1180
4300
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
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  • 生物活性

    ITD1 displays little or no inhibition of activin, Wnt or BMP signaling pathways. Induces proteasomal degradation of the TGF-β type II receptor. Inhibits TGF-β-induced mesoderm formation from mouse embryonic stem cells (ESCs) during early differentiation. ITD1 stimulates the differentiation of cardiomyocytes and promote cardiogenesis in murine embryonic stem cell (mESCs) in vitro between days 3-5. Does not induce differentiation of vascular smooth muscle cells or endothelial cells. TGFβ inhibition by the (+)-eneatiomer is approximately 15-fold more effective than by its (−)-enantiomer.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Kinney et al (2013) Emerging strategies for spatiotemporal control of stem cell fate and morphogenesis. Trends Biotechnol. 31 78. PMID: 23219200.
    [2] Willems et al (2012) Small molecule-mediated TGF-ß type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell 11 242. PMID: 22862949.

    分子式
    C27H29NO3    		 分子量
    415.52    		 CAS号
    1099644-42-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    20 mM    		 Water
    <1 mg/mL    		 Ethanol
    10 mM

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02688712 Rectal Adenocarcinoma Drug: LY2157299|Drug: Capecitabine|Drug: Fluorouracil|Procedure: Tumor specific mesorectal excision Providence Health & Services|Eli Lilly and Company Phase 2 2016-06-01 2016-06-23
    NCT00949351 Type 2 Diabetes With Nephropathy Drug: Aliskiren 300mg/d Lerdsin General Hospital Phase 4 2009-09-01 2009-07-29
    NCT00656825 Healthy Drug: P144 cream|Drug: P144 cream|Drug: P144 cream|Drug: Placebo ISDIN|Digna Biotech S.L. Phase 1 2007-03-01 2008-11-04
    NCT00574613 Skin Fibrosis Drug: P144|Drug: placebo ISDIN|Digna Biotech S.L. Phase 2 2007-09-01 2013-02-08
    NCT02488252 Diabetic Nephropathies Drug: Semi-individualised Chinese Medicine treatment|Drug: Routine medical care (active comparator) The University of Hong Kong|School of Chinese Medicine, The University of Hong Kong Phase 2|Phase 3 2015-07-01 2016-10-25
    NCT02689778 Diabetic Nephropathy|Albuminuria Drug: Pirfenidone|Drug: Placebo Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|Grupo Medifarma, S. A. de C. V. Phase 3 2016-03-01 2016-08-29
    NCT00320970 Diabetic Nephropathy|Hypertension Drug: Candesartan Providence Health & Services|AstraZeneca 2002-08-01 2007-08-01
    NCT01015937 Diabetic Nephropathy|Proteinuria Drug: Turmeric extract|Drug: Angiotensin-converting enzyme (ACE) inhibitor + Angiotensin-II type 1 receptor (ATI) blocker Shaheed Faghihi Hospital|Shiraz University of Medical Sciences 2008-03-01 2009-11-17
    NCT00990639 Alcoholic Liver Disease Drug: candesartan for hepatic fibrosis Yonsei University Phase 1|Phase 2 2005-09-01 2009-10-06
    NCT01541267 Chronic Kidney Disease|Proteinuria Drug: aliskiren, eplerenon, telmisartan Medical University of Gdansk Phase 4 2009-12-01 2012-02-28
    NCT02446548 Albuminuria Drug: aliskiren|Drug: losartan|Other: Placebo Medical University of Gdansk 2013-03-01 2015-05-13

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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