FR 171113

PAR1 antagonist CAS# 173904-50-2

FR 171113

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Chemical structure

FR 171113

3D structure

Chemical Properties of FR 171113

Cas No. 173904-50-2 SDF Download SDF
PubChem ID 25015749 Appearance Powder
Formula C19H11Cl3N2O4S M.Wt 469.73
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in DMSO
Chemical Name methyl (2E)-2-[3-(4-chlorophenyl)-2-(2,4-dichlorobenzoyl)imino-4-oxo-1,3-thiazolidin-5-ylidene]acetate
SMILES COC(=O)C=C1C(=O)N(C(=NC(=O)C2=C(C=C(C=C2)Cl)Cl)S1)C3=CC=C(C=C3)Cl
Standard InChIKey SDGLYCKTPKZBGI-DALCUZTNSA-N
Standard InChI InChI=1S/C19H11Cl3N2O4S/c1-28-16(25)9-15-18(27)24(12-5-2-10(20)3-6-12)19(29-15)23-17(26)13-7-4-11(21)8-14(13)22/h2-9H,1H3/b15-9+,23-19?
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of FR 171113

DescriptionProtease-activated receptor 1 (PAR1) antagonist. Exhibits potent antiplatelet activity in vitro; inhibits thrombin TRAP-6-induced platelet aggregation (IC50 = 2.5 μM) with no effect on coagulation time.

FR 171113 Dilution Calculator

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FR 171113 Molarity Calculator

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Preparing Stock Solutions of FR 171113

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1289 mL 10.6444 mL 21.2888 mL 42.5777 mL 53.2221 mL
5 mM 0.4258 mL 2.1289 mL 4.2578 mL 8.5155 mL 10.6444 mL
10 mM 0.2129 mL 1.0644 mL 2.1289 mL 4.2578 mL 5.3222 mL
50 mM 0.0426 mL 0.2129 mL 0.4258 mL 0.8516 mL 1.0644 mL
100 mM 0.0213 mL 0.1064 mL 0.2129 mL 0.4258 mL 0.5322 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on FR 171113

TeA is a key virulence factor for Alternaria alternata (Fr.) Keissler infection of its host.[Pubmed:28324684]

Plant Physiol Biochem. 2017 Jun;115:73-82.

A toxin-deficient mutant strain, HP001 mutant of Alternaria alternata, whose mycelium is unable to infect its host, produces little tenuazonic acid (TeA) toxin. How TeA plays a role in initiating host infection by A. alternata remains unclear. In this research we use Imaging-PAM based on chlorophyll fluorescence parameters and transmission electron microscopy to explore the role of TeA toxin during the infection process of A. alternata. Photosystem II damage began even before wild type mycelium infected the leaves of its host, croftonweed (Ageratina adenophora). Compared with the wild type, HP001 mutant produces morphologically different colonies, hyphae with thinner cell walls, has higher reactive oxygen species (ROS) content and lower peroxidase activity, and fails to form appressoria on the host surface. Adding TeA toxin allows the mutant to partially recover these characters and more closely resemble the wild type. Additionally, we found that the mutant is able to elicit disease symptoms when its mycelium is placed on leaves whose epidermis has been manually removed, which indicates that TeA may be determinant in the fungus recognition of its plant host. Lack of TeA toxin appears responsible for the loss of pathogenicity of the HP001 mutant. As a key virulence factor, TeA toxin not only damages the host plant but also is involved in maintaining ROS content, host recognition, inducing appressoria to infect the host and for allowing completion of the infection process.

Vessel Patency at 24 Hours and Its Relationship With Clinical Outcomes and Infarct Volume in REVASCAT Trial (Randomized Trial of Revascularization With Solitaire FR Device Versus Best Medical Therapy in the Treatment of Acute Stroke Due to Anterior Circulation Large Vessel Occlusion Presenting Within Eight Hours of Symptom Onset).[Pubmed:28292867]

Stroke. 2017 Apr;48(4):983-989.

BACKGROUND AND PURPOSE: Higher rates of target vessel patency at 24 hours were noted in the thrombectomy group compared with control group in recent randomized trials. As a prespecified secondary end point, we aimed to assess 24-hour revascularization rates by treatment groups and occlusion site as they related to clinical outcome and 24-hour infarct volume in REVASCAT (Randomized Trial of Revascularization With Solitaire FR Device Versus Best Medical Therapy in the Treatment of Acute Stroke Due to Anterior Circulation Large Vessel Occlusion Presenting Within Eight Hours of Symptom Onset). METHODS: Independent core laboratory adjudicated vessel status according to modified arterial occlusive lesion classification at 24 hours on computed tomographic/magnetic resonance (94.2%/5.8%) angiography and 24-hour infarct volume on computed tomography were studied (95/103 patients in the thrombectomy group versus 94/103 in the control group, respectively). Complete revascularization was defined as modified arterial occlusive lesion grade 3. Its effect on clinical outcome was analyzed by ordinal logistic regression. RESULTS: Complete revascularization was achieved in 70.5% of the solitaire group and in 22.3% of the control group (P<0.001). Significant differences in complete revascularization rates were found for terminus internal carotid artery, M1, and tandem occlusions (all P<0.001) but not for M2 occlusions. In the thrombectomy group, 2 out of 63 patients (3.1%) with modified Thrombolysis in Cerebral Infarction 2b/3 after thrombectomy showed arterial reocclusion (modified arterial occlusive lesion grade 0/1) at 24 hours. Complete revascularization was associated with improved outcome in both thrombectomy (adjusted odds ratio, 4.5; 95% confidence interval, 1.9-10.9) and control groups (adjusted odds ratio, 2.7; 95% confidence interval, 1.0-6.7). Revascularization (modified arterial occlusive lesion grade 2/3) was associated with smaller infarct volumes in either treatment arm. CONCLUSIONS: Complete revascularization at 24 hours is a powerful predictor of favorable clinical outcome, whereas revascularization of any type results in reduced infarct volume in both thrombectomy and control groups. CLINICAL TRIAL REGISTRATION: URL: http://www.clinicaltrials.gov. Unique identifier: NCT01692379.

The CAM-ICU has now a French "official" version. The translation process of the 2014 updated Complete Training Manual of the Confusion Assessment Method for the Intensive Care Unit in French (CAM-ICU.fr).[Pubmed:28365244]

Anaesth Crit Care Pain Med. 2017 Oct;36(5):297-300.

INTRODUCTION: Delirium is common in Intensive-Care-Unit (ICU) patients but under-recognized by bed-side clinicians when not using validated delirium-screening tools. The Confusion-Assessment-Method for the ICU (CAM-ICU) has demonstrated very good psychometric properties, and has been translated into many different languages though not into French. We undertook this opportunity to describe the translation process. MATERIAL AND METHODS: The translation was performed following recommended guidelines. The updated method published in 2014 including introduction letters, worksheet and flowsheet for bed-side use, the method itself, case-scenarios for training and Frequently-Asked-Questions (32 pages) was translated into French language by a neuropsychological researcher who was not familiar with the original method. Then, the whole method was back-translated by a native English-French bilingual speaker. The new English version was compared to the original one by the Vanderbilt University ICU-delirium-team. Discrepancies were discussed between the two teams before final approval of the French version. RESULTS: The entire process took one year. Among the 3692 words of the back-translated version of the method itself, 18 discrepancies occurred. Eight (44%) lead to changes in the final version. Details of the translation process are provided. CONCLUSIONS AND RELEVANCE: The French version of CAM-ICU is now available for French-speaking ICUs. The CAM-ICU is provided with its complete training-manual that was challenging to translate following recommended process. While many such translations have been done for other clinical tools, few have published the details of the process itself. We hope that the availability of such teaching material will now facilitate a large implementation of delirium-screening in French-speaking ICUs.

[Comparing study on the hyoid bone position after treatment of class malocclusion using improved appliance FR ].[Pubmed:28317354]

Hua Xi Kou Qiang Yi Xue Za Zhi. 2016 Aug 1;34(4):369-374.

OBJECTIVE: This study aims to compare the changes of hyoid bone position before and after treatment of Angle class malocclusion using improved appliance FR . METHODS: Forty patients with Angle class malocclusion were chosen and divided into two groups, namely, experimental and control. Each group had 20 patients. The young patients in the experi-mental group were treated using improved appliance FR , whereas those in the control group were treated using classic appliance FR . The hyoid bone position of the two groups were comparatively analyzed using an X-ray film before and after treatment. RESULTS: Compared with the condition before treatment, the condition after treatment showed that the hyoid bone position of young patients with Angle class malocclusion treated using improved appliance FR , H-FH, H-S, H-Ptm, and Ar-H-Me exhibited an increased angle (P<0.01), whereas the hyoid bone position of those treated using H-MP and H-Gn showed a decreased angle (P<0.01). The hyoid bone position of young patients with Angle class malocclusion treated using classic appliance FR , H-FH, H-S, and H-Ptm had an increased angle (P<0.05). Moreover, the hyoid bone position of those treated using Ar-H-Me had an increased angle (P<0.01), and the hyoid bone position of those treated using H-MP and H-RGn had a decreased angle (P<0.05). CONCLUSIONS: Compared with the hyoid bone position before treatment, the hyoid bone position after treatment of the young patients with Angle class malocclusion treated using improved appliance FR may move backward and downward, and the mandibular and hyoid bone position may move through clockwise rotation. The mandibular and hyoid bone position of young patients with Angle class malocclusion treated using classic appliance FR obtained a large angle by moving clockwise. The man-dibular bone moves backward and downward, thereby improving the hyoid bone in backward and upward directions. This condition makes a significant difference in treating the hyoid bone position of young patients with functional Angle class malocclusion..

Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig.[Pubmed:12892834]

Eur J Pharmacol. 2003 Jul 25;473(2-3):163-9.

The antiplatelet and antithrombotic effects of FR171113, 3-(4-chlorophenyl)-2-(2,4-dichlorobenzoylimino)-5-(methoxycarbonyl methylene)-1,3-thiazolidin-4-one, a non-peptide protease-activated receptor 1 (PAR1) antagonist, were evaluated in guinea pigs. FR171113 inhibited Ser-Phe-Leu-Leu-Arg-Asn-NH2 (a synthetic PAR1 agonist peptide)-induced and thrombin-induced aggregation of guinea pig platelets in a concentration-dependent manner in vitro (IC50=1.5 and 0.35 microM, respectively). Subcutaneous administration of FR171113 (0.1-3.2 mg/kg) produced a dose-dependent inhibition of platelet aggregation ex vivo. The ED50 value of FR171113 for platelet aggregation was 0.49 mg/kg s.c. However, FR171113 did not have an inhibitory effect on ADP- or collagen-induced platelet aggregation in vitro and ex vivo. One hour after FR171113 treatment at 1.0 mg/kg s.c., significant inhibition of arterial thrombosis without a prolongation of thrombin time or coagulation time was seen in the FeCl3-induced carotid artery thrombosis model in guinea pigs. Furthermore, FR171113 did not prolong bleeding time even at 32 mg/kg s.c., which is a much higher dose than that required in the thrombosis model. These observations indicate that FR171113 has desirable antiplatelet effects both in vitro and in vivo and that its in vivo antithrombotic activity is efficacious without causing a prolongation of bleeding time.

In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist.[Pubmed:10611442]

Eur J Pharmacol. 1999 Nov 19;384(2-3):197-202.

Synthetic peptides (5 to 14 amino acids), identical in sequence to the new amino-terminus of the thrombin receptor generated following cleavage by thrombin, act as thrombin receptor agonist peptides. Whilst thrombin receptor antagonist peptides are known, non-peptide thrombin receptor antagonists have yet to be described. In the present study, we compared the antiplatelet effects of 3-(4-chlorophenyl)-2-(2,4-dichlorobenzoylimino)-5-(methoxycarbonyl methylene)-1,3-thiazolidin-4-one (FR171113), a novel non-peptide thrombin receptor antagonist, with the known thrombin receptor antagonist 3-mercapto-propionyl-Phe-Cha-Cha-Arg-Asn-Pro-Asn-Asp-Lys-Tyr-OH (C186-65), and argatroban, a specific protease inhibitor of thrombin. FR171113 and C186-65 inhibited thrombin-induced platelet aggregation (IC(50)=0.29 microM and 15 microM, respectively) and Ser-Phe-Leu-Leu-Arg-Asn-NH(2) [a synthetic thrombin receptor agonist peptide (TRAP-6)] induced platelet aggregation (0.15 microM and 20 microM, respectively) in human washed platelets. Argatroban potently inhibited thrombin-induced platelet aggregation (IC(50)=3.5 nM), but did not inhibit TRAP-6-induced aggregation even at 100 microM. In contrast, these compounds did not show inhibitory effects on ADP- and collagen-induced aggregation in human platelet-rich plasma even at 100 microM. FR171113 caused a parallel shift to the right of the concentration-response curve describing aggregation induced by TRAP-6. The Schild plot of the data had a slope of -0.840 (r=0.98) and the pA(2) was 7.29. In protease activity studies using a chromogenic substrate, argatroban inhibited thrombin protease activity in a dose-dependent manner, whereas FR171113 and C186-65 were inactive, even at 100 microM. Additionally, only argatroban displayed dose-dependent prolongation of thrombin time, activated partial thromboplastin time and prothrombin time. FR171113 and C186-65 showed no effects, even at a concentration of 100 microM. These results suggest that FR171113 has a similar mode of action to C186-65, but with more potent antiplatelet activity. In conclusion, FR171113 is suggested to be the first example of a non-peptide thrombin receptor antagonist.

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