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Purity: ≥98%
FT011 is a novel potent anti-inflammatory and anti-fibrotic agent that has been reported to attenuate organ damage in diabetic rats with cardiomyopathy and nephropathy. n diabetic rats, FT011 reduced retinal leukostasis, microglial density and mRNA levels of intercellular adhesion molecule-1 (ICAM-1). In Müller cells, FT011 reduced diabetes-induced gliosis and vascular endothelial growth factor (VEGF) immunolabeling and the hyperglycaemic-induced increase in ICAM-1, monocyte chemoattractant protein-1, CCL20, cytokine-induced neutrophil chemoattractant-1, VEGF and IL-6. Late intervention with FT011 reduced acellular capillaries and the elevated mRNA levels of collagen IV and fibronectin in diabetic rats. In conclusion, the protective effects of FT011 in cardiorenal disease extend to key elements of diabetic retinopathy and highlight its potential as a treatment approach.
| Targets |
Anti-fibrotic; ICAM-1
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| ln Vitro |
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| ln Vivo |
In rats with myocardial infarction, FT011 (100 mg/kg bid, po) improves cardiac function and myocardial remodeling[1].
Collagen synthesis in NCF was determined by (3)H-proline incorporation following stimulation with TGF-β or angiotensin II (Ang II). FT011 inhibited collagen synthesis to both agents in a dose dependent manner. In vivo, Sprague Dawley rats underwent left anterior descending coronary artery ligation or sham surgery and were randomized one week later to receive either FT011 (200mg/kg/day) or vehicle for a further 4 weeks. Echocardiography and cardiac catheterization were performed, and tissues were collected for histological analysis of collagen, myocyte hypertrophy, interstitial macrophage accumulation and Smad2 phosphorylation. mRNA expression of collagens I and III and TGF-β was measured using in situ hybridization and RT-PCR, respectively. FT011 treatment was associated with improved cardiac function (increased ejection fraction, fraction shortening and preload recruitable stroke work) and myocardial remodeling (reduced left ventricular diameter and volume at both end diastolic and systolic) compared with vehicle treatment. FT011 significantly reduced collagen matrix deposition, myocyte hypertrophy and interstitial macrophage infiltration, and mRNA expression of collagens I and III in NIZ compared with vehicle treatment. Conclusion: Anti-fibrotic therapy with FT011 in MI rats attenuated fibrosis and preserved systolic function.[1] |
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| Cell Assay |
Measurement of collagen synthesis in rat neonatal cardiac fibroblasts (NCF)[1]
NCF were isolated from one to two day old pups with enzymatic digestion as described previously, and used at passage two. NCF collagen synthesis assays were performed as described previously. Briefly, NCF were pre-incubated for 2 h in the presence of FT011 (10–200 μM) or 0.1% DMSO (control group) in fresh DMEM/F12 before stimulation with 5 ng/ml of TGF-β or 100 nM of AngII in the presence of 1 μCi of 3H-proline/well and incubated for further 48 h before harvest. 3H-proline level was counted with 3 ml scintillation fluid on a β-counter to determine the level of 3H-proline incorporation. Experiments were performed in triplicate. |
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| Animal Protocol |
Animal/Disease Models: Seventy male Sprague Dawley (SD) rats (weighing 200-250 g)[1]
Doses: 100 mg/kg Route of Administration: BID, po on day 7 after surgery, for 4 weeks Experimental Results: Increased ejection fraction, fraction shortening and preload recruitable stroke work. Myocardial infarction and study design[1] Seventy male Sprague Dawley (SD) rats in total weighing 200–250 g were randomized to undergo left anterior descending coronary artery (LAD) ligation or sham surgery as described previously [18]. Briefly, animals were anesthetized with isoflurane, intubated and the thoracic cavity opened. The pericardial sac was torn open and a 6-0 prolene suture was used to ligate the LAD. Visible blanching and hypokinesis of the anterior wall of the left ventricle and swelling of the left atrium are indicative of successful ligation. Sham operations consisted of the same procedure except that the suture was passed through the myocardium beneath the LAD without ligation. Echocardiography was performed on all animal groups 2 days post-MI surgery (base-line). On day 7 after surgery, sham and MI groups were randomized to receive either treatment with FT011 (100 mg/kg b.i.d. gavage) or vehicle (0.1% carboxy-methyl cellulose) for 4 weeks. We have previously examined the safety profile of FT011 within the dose range used in the present study. Cardiac function was assessed by echocardiography and cardiac catheterization prior to sacrificing at day 35 after surgery. |
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| References | ||
| Additional Infomation |
Pathological deposition of extracellular matrix in the non-infarct zone (NIZ) of the ventricle post myocardial infarction (MI) is a key contributor to cardiac remodeling and heart failure. FT011, a novel antifibrotic compound, was evaluated for its efficacy in neonatal cardiac fibroblasts (NCF) and in an experimental MI model.
In summary, our findings indicate that FT011 reduces collagen matrix accumulation and myocyte hypertrophy in the heart following MI, which is associated with a significant improvement in systolic function. While the precise mode of action for FT011 is not certain, these data confirm the therapeutic potential of FT011, specifically targeting fibrosis in the setting of MI and heart failure.[1] |
| Molecular Formula |
C₂₀H₁₇NO₅
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| Molecular Weight |
351.35
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| Exact Mass |
351.11
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| Elemental Analysis |
C, 68.37; H, 4.88; N, 3.99; O, 22.77
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| CAS # |
1001288-58-9
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| Related CAS # |
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| PubChem CID |
23648966
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
618.9±55.0 °C at 760 mmHg
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| Flash Point |
328.1±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
4.39
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
564
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CC#C)C1=CC=C(/C=C/C(NC2C=CC=CC=2C(=O)O)=O)C=C1OC
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| InChi Key |
UIWZIDIJCUEOMT-PKNBQFBNSA-N
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| InChi Code |
InChI=1S/C20H17NO5/c1-3-12-26-17-10-8-14(13-18(17)25-2)9-11-19(22)21-16-7-5-4-6-15(16)20(23)24/h1,4-11,13H,12H2,2H3,(H,21,22)(H,23,24)/b11-9+
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| Chemical Name |
2-[[(E)-3-(3-methoxy-4-prop-2-ynoxyphenyl)prop-2-enoyl]amino]benzoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.12 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8462 mL | 14.2308 mL | 28.4616 mL | |
| 5 mM | 0.5692 mL | 2.8462 mL | 5.6923 mL | |
| 10 mM | 0.2846 mL | 1.4231 mL | 2.8462 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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