| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Tasosartan (ANA-756, AC1Q6LAA, DB01349, WAY-ANA-756, Verdia) is a pyrido-pyrimidin-based and long-acting antagonist of angiotensin II (AngII) receptor with anti-hypertensive effects. Its active metabolite, enoltasosartan, has been credited for its prolonged duration of action. In an investigation aimed at determining the respective roles played by enoltasosartan and tasosartan in the overall pharmacological effect of tasosartan. In a randomized, double blind, three-period crossover study, the AngII receptor blockade effect of single doses of tasosartan (100 mg p.o. and 50 mg i.v.) and enoltasosartan (2.5 mg i.v.) was compared in 12 healthy subjects using two approaches: the ex vivo AngII radioreceptor assay and the in vivo blood pressure response to exogenous AngII. Tasosartan caused AngII subtype-1 (AT1) receptors to be blocked quickly and persistently. In vivo, 1 to 2 hours after drug administration, tasosartan (p.o. or i.v.) blocked 80% of AT1 receptors, and it still had a 40% effect at 32 hours. The blockade in vitro was estimated to be 20% at 32 hours and 90% at 2 hours. On the other hand, despite the intravenous administration and elevated plasma levels, the blockade caused by enoltasosartan was significantly delayed and barely reached 60 to 70%. The presence of plasma proteins significantly affected the AT1 antagonistic effect of enoltasosartan in vitro, causing a decrease in its affinity for the receptor and a slower rate of receptor association. Tasosartan alone is mostly responsible for the early effects, with enoltasosartan having little to no effect. Oltasosartan's antagonistic effect manifests itself later. Oltasosartan's delayed in vivo blockade effect seems to be caused by a strong and slow protein binding followed by a slow process of dissociation from the carrier.
| Targets |
Angiotensin II (AngII) receptor
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|---|---|
| ln Vitro |
Tasosartan is an oral active nonpeptide AngII antagonist, exhibited specific and selective antagonistic activity against AT1 receptors in vitro. In the absence of proteins in the binding buffer, the IC50 value for inhibiting the specific binding of 125I-AngII to the rat adrenal membrane is 1.2±0.6 nM [1].
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| ln Vivo |
Tasosartan administration significantly (p<0.05) reduces the pressor response in rats to angiotensin-II at doses of 1.0 and 3.0 mg/kg (iv)[2].
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| Animal Protocol |
Rats: Four groups of rats, each weighing 343±8 g, were studied to determine the pressor response to angiotensin-II administration. After the introduction of either the vehicle or graded doses of Tasosartan (0.3, 1.0, or 3.0 mg/kg, iv), each rat receives four separate bolus injections of angiotensin-II.
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| References |
| Molecular Formula |
C23H21N7O
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|---|---|
| Molecular Weight |
411.4591
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| Exact Mass |
411.18
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| Elemental Analysis |
C, 67.14; H, 5.14; N, 23.83; O, 3.89
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| CAS # |
145733-36-4
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| Related CAS # |
145733-36-4
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| Appearance |
Solid powder
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| SMILES |
CC1=C2CCC(=O)N(C2=NC(=N1)C)CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5
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| InChi Key |
ADXGNEYLLLSOAR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29)
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| Chemical Name |
2,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one
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| Synonyms |
ANA-756; AC1Q6LAA; DB01349; WAY-ANA-756; Verdia; AC1L1U5X; WAY-ANA 756; WAYANA-756; WAY ANA 756; Tasosartan
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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 |
| 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) |
DMSO: ~125 mg/mL (~303.8 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 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: ≥ 2.08 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4304 mL | 12.1518 mL | 24.3037 mL | |
| 5 mM | 0.4861 mL | 2.4304 mL | 4.8607 mL | |
| 10 mM | 0.2430 mL | 1.2152 mL | 2.4304 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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