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Ripisartan

Catalog No. T28540 CAS 148504-51-2

Synonyms: UP 269-6, UP-2696, UP 2696, UP-269-6, UP269-6

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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Ripisartan, CAS 148504-51-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 191.00
5 mg	In stock	$ 470.00
10 mg	In stock	$ 689.00
25 mg	In stock	$ 1,080.00
50 mg	In stock	$ 1,460.00
100 mg	In stock	$ 1,960.00
500 mg	In stock	$ 3,930.00

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Purity: 98.24%

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Description	Ripisartan (UP-269-6) is a potent and specific angiotensin II receptor antagonist that inhibits angiotensin II-mediated sympathetic tachycardia responses.
Targets&IC50	Adrenal membranes:35.8 nM, Smooth muscle cells (SMCs):23.8 nM
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.

Synonyms	UP 269-6, UP-2696, UP 2696, UP-269-6, UP269-6
Molecular Weight	426.47
Formula	C23H22N8O
CAS No.	148504-51-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Cazes M, et al. In vivo pharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist. Eur J Pharmacol. 1995;284(1-2):157-170. 2. Virone-Oddos A, et al. In vitro and in vivo effects of UP 269-6, a new potent orally active nonpeptide angiotensin II receptor antagonist, on vascular smooth muscle cell proliferation. Br J Pharmacol. 1997;120(3):488-494. 3. McIntyre M, et al. Comparison of the oral angiotensin II receptor antagonist UP 269-6 or enalapril 20 mg on blood pressure and neurohormonal effects in salt-deplete man. J Cardiovasc Pharmacol. 1995;25(6):994-1000. 4. Caussade F, et al. In vitro pharmacological characterization of UP 269-6, a novel nonpeptide angiotensin II receptor antagonist. Fundam Clin Pharmacol. 1995;9(2):119-128.

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Related Products

Related compounds with same targets

TRV-120027 TFA L162389 CGP48369 Aviptadil Acetate Losartan Carboxylic Acid Olmesartan [Sar1, Ile8]-Angiotensin II acetate Lisinopril dihydrate

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Keywords

Ripisartan 148504-51-2 Endocrinology/Hormones RAAS UP 269-6 UP-2696 UP 2696 UP2696 UP-269-6 UP269-6 inhibitor inhibit

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