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Ripisartan

Ripisartan
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Purity:98.24%
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Ripisartan

Catalog No. T28540Cas No. 148504-51-2
Ripisartan (UP-269-6) is a potent and specific angiotensin II receptor antagonist that inhibits angiotensin II-mediated sympathetic tachycardia responses.
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Pack SizePriceAvailabilityQuantity
1 mg$191In Stock
5 mg$470In Stock
10 mg$689In Stock
25 mg$1,080In Stock
50 mg$1,460In Stock
100 mg$1,960In Stock
500 mg$3,930In Stock
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Product Introduction

Bioactivity
Description
Ripisartan (UP-269-6) is a potent and specific angiotensin II receptor antagonist that inhibits angiotensin II-mediated sympathetic tachycardia responses.
In vitro
UP 269-6 bound selectively to AT1 receptors as evidenced by the inhibition of specific [125I] Sar1, Ile8-AII binding in rat adrenal membranes (IC50 = 35.8 nM) and in cultured vascular smooth muscle cells (IC50 = 23.8 nM). UP 269-6 displayed a very high selectivity for the AT1 compared to the AT2 receptor subtype (IC50 >10,000 nM). UP 269-6 inhibited the AII-induced contraction of isolated rabbit aortic strips.[4]
UP 269-6 at low concentrations (10(-10), 3 x 10(-10), 10(-9) M) of UP 269-6 and insurmountable antagonism at higher concentrations (3 x 10(-9), 10(-8), 3 x 10(-8) M). Based on the calculated pA2 values, UP 269-6 (9.86 +/- 0.25) was an angiotensin II receptor antagonist as potent as L-158,809 (9.82 +/- 0.37) and much more potent than losartan (7.96 +/- 0.38). UP 269-6 was devoid of affinity (IC50 > 10,000 nM) for many other receptors, ion channels and uptake sites, demonstrating its high specificity for AII receptors. Furthermore, this compound did not affect the contractile response to KCl or phenylephrine in rabbit aorta and exhibited no effect on angiotensin-converting enzyme activity. These data demonstrate that UP 269-6 is a highly potent, selective, and specific AT1 receptor antagonist.[4]
In vivo
UP 269-6 (0.03-1 mg/kg; i.v.; rats) shifted dose-dependently to the right of the dose-pressor response curve for angiotensin II and decreased the maximum response. UP 269-6 antagonized the angiotensin II sympathetic-mediated tachycardiac response.[1]
UP 269-6 inhibited dose-dependently the pressor response to angiotensin II with an ID50 of 4.5 micrograms/kg, i.v. in conscious normotensive dogs.[1]
UP 269-6 (0.1 to 30 mg/kg; Oral) resulted in a dose-dependent and long-lasting inhibition of the angiotensin II-induced pressor response in conscious normotensive rats and dogs.[1]
UP 269-6 is a potent and specific angiotensin II receptor antagonist and does not possess agonistic properties.
AliasUP 269-6, UP-2696, UP 2696, UP-269-6, UP269-6
Chemical Properties
Molecular Weight426.47
FormulaC23H22N8O
Cas No.148504-51-2
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 55 mg/mL (128.97 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3448 mL11.7242 mL23.4483 mL117.2415 mL
5 mM0.4690 mL2.3448 mL4.6897 mL23.4483 mL
10 mM0.2345 mL1.1724 mL2.3448 mL11.7242 mL
20 mM0.1172 mL0.5862 mL1.1724 mL5.8621 mL
50 mM0.0469 mL0.2345 mL0.4690 mL2.3448 mL
100 mM0.0234 mL0.1172 mL0.2345 mL1.1724 mL

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