FimasartanCAS# 247257-48-3 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 247257-48-3 | SDF | Download SDF |
PubChem ID | 9870652 | Appearance | Powder |
Formula | C27H31N7OS | M.Wt | 501.65 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : ≥ 49 mg/mL (97.68 mM) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | 2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-N,N-dimethylethanethioamide | ||
SMILES | CCCCC1=NC(=C(C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CC(=S)N(C)C)C | ||
Standard InChIKey | AMEROGPZOLAFBN-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C27H31N7OS/c1-5-6-11-24-28-18(2)23(16-25(36)33(3)4)27(35)34(24)17-19-12-14-20(15-13-19)21-9-7-8-10-22(21)26-29-31-32-30-26/h7-10,12-15H,5-6,11,16-17H2,1-4H3,(H,29,30,31,32) | ||
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. |
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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. |
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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. |
Fimasartan Dilution Calculator
Fimasartan Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.9934 mL | 9.9671 mL | 19.9342 mL | 39.8684 mL | 49.8355 mL |
5 mM | 0.3987 mL | 1.9934 mL | 3.9868 mL | 7.9737 mL | 9.9671 mL |
10 mM | 0.1993 mL | 0.9967 mL | 1.9934 mL | 3.9868 mL | 4.9836 mL |
50 mM | 0.0399 mL | 0.1993 mL | 0.3987 mL | 0.7974 mL | 0.9967 mL |
100 mM | 0.0199 mL | 0.0997 mL | 0.1993 mL | 0.3987 mL | 0.4984 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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Safety and efficacy of fimasartan in Mexican patients with grade 1-2 essential hypertension.[Pubmed:28209359]
Arch Cardiol Mex. 2017 Oct - Dec;87(4):316-325.
OBJECTIVE: To evaluate efficacy and safety of 60mg and 120mg Fimasartan (FMS) alone or combined with 12.5mg hydrochlorothiazide (HCTZ) in a Mexican population. METHODS: A six month, treat-to-target, open study was conducted on subjects with grade 1-2 hypertension. The subjects were initially treated with 60mg FMS once daily. In week 8, those with Diastolic Blood Pressure (DBP) <90mmHg continued on the same FMS dose during the rest of the study, while those with DBP >/=90mmHg were randomised to either 120mg FMS or 60mg FMS + 12.5mg HCTZ once daily. In week 12, randomised subjects with DBP >/=90mmHg received 120mg FMS+12.5mg HCTZ, while those achieving target continued with their assigned treatment until the end of the study. RESULTS: FMS 60mg (n=272) decreased both DBP and Systolic Blood Pressure (SBP) by 11.3+/-8.9 (p<.0001) and 16.0+/-14.1 (p<.0001)mmHg, respectively, with 75.4% of subjects reaching the treatment target. Subjects assigned to FMS 120mg, FMS 60mg+HCTZ 12.5mg, or FMS 120mg+HCTZ 12.5mg once daily, showed significant reductions in DBP and SBP with their assigned treatment. At the end of the study, 237/272 subjects (87.1%) achieved a DBP<90mmHg and an SBP<140mmHg. The most frequently reported adverse reactions included headache (3.7%), dry mouth (1.1%), transient liver enzyme increase (1.1%), and dizziness (0.7%). CONCLUSION: Fimasartan is safe and effective in Mexican subjects with grade 1-2 essential hypertension.
Pharmacokinetic drug interaction study using fimasartan and rosuvastatin in healthy volunteers.[Pubmed:27668695]
Int J Clin Pharmacol Ther. 2016 Dec;54(12):992-1003.
OBJECTIVE: This study evaluated the possible pharmacokinetic interactions between rosuvastatin and Fimasartan, an angiotensin II type 1 (AT1) receptor blocker (ARB), approved in Korea for the treatment of mild to moderate hypertension. METHODS: In this open-label, multiple-dose, two-period, single-sequence study, the enrolled subjects were randomized into two separate parts (A and B). In part A, subjects received 120 mg of Fimasartan alone for 7 days during period I, and 120 mg Fimasartan with 20 mg rosuvastatin for 7 days during period II. In Part B, subjects received rosuvastatin alone, followed by concomitant administration of Fimasartan, with the same doses used as in Part A. There was a 7-day washout between periods I and II. Serial blood samples were collected for up to 48 hours for Fimasartan and for up to 72 hours for rosuvastatin after the last dose of each period to determine the steady-state pharmacokinetics of both drugs. RESULTS: The mean Cmax,ss and AUCtau,ss values of Fimasartan were 258.03 +/- 176.75 ng/mL and 746.52 +/- 273.49 ngxh/mL for Fimasartan alone, and 289.40 +/- 231.44 ng/mL and 848.43 +/- 267.45 ngxh/mL for Fimasartan and rosuvastatin coadministration, respectively (p-values for Cmax,ss and AUCtau,ss, 0. 513 and 0.006, respectively). The mean Cmax,ss and AUCtau,ss values of rosuvastatin were 9.94 +/- 4.48 ng/mL and 85.29 +/- 36.25 ngxh/mL for rosuvastatin alone and 11.94 +/- 8.47 ng/mL and 77.33 +/- 38.71 ngxh/mL for Fimasartan and rosuvastatin coadministration, respectively (p-values for Cmax,ss and AUCtau,ss, 0.066 and 0.009, respectively). The geometric mean ratio (GMR) and 90% confidence intervals (CI) for the Cmax,ss and AUCtau,ss of Fimasartan (with/without rosuvastatin) were 1.109 (0.813 - 1.511) and 1.159 (1.061 - 1.265), respectively. The GMR and 90% CI for the Cmax,ss and AUCtau,ss of rosuvastatin (with/without Fimasartan) were 1.090 (0.979 - 1.213) and 0.870 (0.804 - 0.940), respectively. CONCLUSIONS: These results suggest that Fimasartan and rosuvastatin have no relevant pharmacokinetic drug-drug interactions. All treatments were well tolerated during this study, with no serious adverse effects..
A Randomized, Double-blind, Multicenter, Phase III Study to Evaluate the Efficacy and Safety of Fimasartan/Amlodipine Combined Therapy Versus Fimasartan Monotherapy in Patients With Essential Hypertension Unresponsive to Fimasartan Monotherapy.[Pubmed:27502326]
Clin Ther. 2016 Oct;38(10):2159-2170.
PURPOSE: The goal of this study was to evaluate whether the blood pressure-lowering efficacy of Fimasartan/amlodipine combination therapy was superior to that of Fimasartan monotherapy after 8 weeks of treatment in patients with hypertension who had failed to respond adequately to Fimasartan monotherapy. METHODS: This trial was a randomized, double-blind, multicenter, Phase III clinical study. Patients who failed to respond after 4 weeks of treatment with 60 mg daily of Fimasartan (sitting systolic blood pressure [SiSBP]) >/=140 mm Hg) were randomized to receive either daily Fimasartan 60 mg or Fimasartan/amlodipine 60 mg/10 mg. The primary efficacy end point was the change in SiSBP from baseline to week 8. Secondary end points included the change in SiSBP from baseline to week 4, the changes in sitting diastolic blood pressure from baseline to weeks 4 and 8, and the response rate (SiSBP <140 mm Hg or decrease in SiSBP >/=20 mm Hg) or control rate (SiSBP <140 mm Hg) at week 8. Treatment-emergent adverse events were also assessed. FINDINGS: Of 143 patients randomized to treatment, 137 patients who had available efficacy data were analyzed. The mean age of patients was 59.1 (8.9) years, and 100 (73.0%) were male. Baseline SiSBP and sitting diastolic blood pressure were 150.6 (9.2) mm Hg and 91.7 (8.6) mm Hg, respectively. In the Fimasartan/amlodipine combination group, a greater reduction in SiSBP from baseline to week 8 was observed compared with the Fimasartan group (7.8 [13.3] mm Hg in the Fimasartan group vs 20.5 [14.6] mm Hg in the Fimasartan/amlodipine group; P < 0.0001). This reduction was observed after 4 weeks. The mean SiSBP changes from baseline to week 4 were 8.1 (15.8) mm Hg in the Fimasartan group and 20.1 (14.7) mm Hg in the Fimasartan/amlodipine group (P < 0.0001). At week 8, the response rate was significantly higher in the Fimasartan/amlodipine (82.1%) group than in the Fimasartan (32.9%) group (P < 0.0001). The control rate at week 8 was also higher in the Fimasartan/amlodipine (79.1%) group than in the Fimasartan (31.4%) group (P < 0.0001). Adverse drug reactions were observed in 9 patients (6.3%), with no significant differences between treatment groups. There were no serious adverse events associated with the study drugs. IMPLICATIONS: Fimasartan/amlodipine combination therapy exhibited superior efficacy in reducing blood pressure, with no increase in adverse drug reactions, compared with Fimasartan monotherapy. ClinicalTrials.gov identifier: NCT02152306.
The efficacy and safety of co-administration of fimasartan and rosuvastatin to patients with hypertension and dyslipidemia.[Pubmed:28057081]
BMC Pharmacol Toxicol. 2017 Jan 5;18(1):2.
BACKGROUND: Hypertension and dyslipidemia are major risk factors of cardiovascular disease (CVD) events. The objective of this study was to evaluate the efficacy and safety of the co-administration of Fimasartan and rosuvastatin in patients with hypertension and hypercholesterolemia. METHODS: We conducted a randomized double-blind and parallel-group trial. Patients who met eligible criteria after 4 weeks of therapeutic life change were randomly assigned to the following groups. 1) co-administration of Fimasartan 120 mg/rosuvastatin 20 mg (FMS/RSV), 2) Fimasartan 120 mg (FMS) alone 3) rosuvastatin 20 mg (RSV) alone. Drugs were administered once daily for 8 weeks. RESULTS: Of 140 randomized patients, 135 for whom efficacy data were available were analyzed. After 8 weeks of treatment, the FMS/RSV treatment group showed greater reductions in sitting systolic (siSBP) and diastolic (siDBP) blood pressures than those in the group receiving RSV alone (both p < 0.001). Reductions in siSBP and siDBP were not significantly different between the FMS/RSV and FMS alone groups (p = 0.500 and p = 0.734, respectively). After 8 weeks of treatment, FMS/RSV treatment showed greater efficacy in percentage reduction of low-density lipoprotein cholesterol (LDL-C) level from baseline than that shown by FMS alone treatment (p < 0.001). The response rates of siSBP with FMS/RSV, FMS alone, and RSV alone treatments were 65.22, 55.56, and 34.09%, respectively (FMS/RSV vs. RSV, p = 0.006). The LDL-C goal attainment rates with FMS/RSV, RSV alone, and FMS alone treatments were 80.43%, 81.82%, and 15.56%, respectively (FMS/RSV vs. FMS, p < 0.001). Incidence of adverse drug reactions with FMS/RSV treatment was 8.33%, which was similar to those associated with FMS and RSV alone treatments. CONCLUSION: This study demonstrated that the co-administration of Fimasartan and rosuvastatin to patients with both hypertension and hypercholesterolemia was efficacious and safe. TRIAL REGISTRATION: ClinicalTrials.gov Identifier: NCT02166814 . 16 June 2014.