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Art. -Nr.: HY-117876

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S 8308

Name: S 8308
Brand: MedChemExpress
SKU: HY-117876
Availability: PreOrder

(Synonyms: CV 2961)

S 8308 (CV 2961) is a non-peptide angiotensin II (Angiotensin II receptor) receptor antagonist with transient oral activity and short-acting intravenous activity, and exhibits an IC₅₀ of 15 μM in rats. S 8308 competitively blocks the binding of angiotensin II to its receptor, thereby inhibiting vasoconstriction and pressor responses. S 8308 can be used in the research of hypertension and renal hypertension.

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CAS. Nr.: 119256-78-9
Formel: C₁₆H₁₇ClN₃NaO₄
Molecular Weight:373.77

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

S 8308 Chemical Structure

CAS. Nr.: 119256-78-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[3]

AT2 Receptor

15 μM (IC₅₀, rat adrenal cortex microsomes)

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

S 8308 (CV 2961) is a specific competitive angiotensin II receptor antagonist that inhibits the binding of radioligands, with an IC₅₀ of 15 μM in rat adrenal cortex microsomes and an IC₅₀ of 4.5 μM in rat aortic smooth muscle cells ^[3].
S 8308 inhibits the binding of ³H-AII to rat adrenal cortex microsomes with an IC₅₀ of 15 μM, and is a weak angiotensin II receptor antagonist^[6].
S 8308 (60 min) competitively inhibits the binding of angiotensin II to its receptor in rat adrenal cortex microsomes, with an IC₅₀ of 15 μM^[1].
S 8308 (30 min) competitively inhibits the binding of angiotensin II to its receptors on cultured rat aortic smooth muscle cells, with an IC₅₀ of 4.5 μM^[1].
S 8308 (1-30 µM; 15 min) inhibits angiotensin II-induced ⁴⁵Ca²⁺ influx in rat aortic rings in a concentration-dependent manner, with an IC₅₀ of 7 μM, and does not affect norepinephrine- or KCl-induced influx ^[1].
S 8308 (3-100 μM) competitively inhibits angiotensin II-induced contraction of isolated rabbit aortic strips, with a pA₂ value of 5.74, and does not affect the contractions induced by norepinephrine or KCl ^[1].
S 8308 (up to 100 μM) does not inhibit rabbit angiotensin-converting enzyme or rat renin activity^[2].
S 8308 is a non-selective ligand that binds with equal affinity to the AT₁ and AT₂ angiotensin II receptor subtypes in rat adrenal cortical tissue^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

S 8308 (CV 2961) (100 mg/kg; p.o. or i.v.; single administration) reduces blood pressure in rats with renal hypertension, and transient oral activity is observed only at the high dose of 100 mg/kg^[3].
S 8308 (30-100 mg/kg; intravenous administration, oral administration; single-dose administration) produces a rapid and transient hypotensive effect in hypertensive rats with renal artery ligation. Both the 30 mg/kg intravenous dose and the 100 mg/kg oral dose reduce the mean arterial pressure by 20 mmHg, with the durations of action being 30 minutes and less than 30 minutes, respectively^[1].
S 8308 (30 mg/kg; intravenous injection) exhibits antihypertensive activity in renal artery ligation-induced hypertensive rats, with an intravenous ED₃₀ of 30 mg/kg^[4].
S 8308 (100 mg/kg; intravenous injection; single bolus administration) is a selective angiotensin II receptor antagonist in spinalized normotensive rats, which significantly blocks the pressor response induced by angiotensin II and does not attenuate the response to norepinephrine or isoprenaline^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

renal hypertensive strain^[3]
Dosage:

100 mg/kg
Administration:

p.o.; single dose; i.v.; single dose
Result:

Lowered blood pressure in renal hypertensive rats after intravenous administration.
Exhibited transient oral activity only at the 100 mg/kg dose.
Showed short duration of action.

Animal Model:

CD Sprague-Dawley (male, 300-350 g, renal artery-ligated hypertensive model)^[1]
Dosage:

30 mg/kg (i.v.); 100 mg/kg (p.o.)
Administration:

i.v.; single dose; p.o.; single dose
Result:

Reduced mean arterial pressure by 20 mmHg 10 minutes post-administration, with effect lasting 30 minutes.
Produced hypotensive effect within 5 minutes, reaching maximal reduction of 20 mmHg by 15 minutes, with no significant blood pressure reduction observed 30 minutes post-administration.

Animal Model:

normotensive pithed rats^[5]
Dosage:

100 mg/kg
Administration:

i.v.; single bolus
Result:

Markedly inhibited the pressor response to angiotensin II.
Slightly reduced the increase in diastolic pressure to sympathetic nerve stimulation.
Had no significant effect on the responses to norepinephrine and isoproterenol.

Chemical Information

CAS. Nr. 119256-78-9
Molecular Weight 373.77
Formel C₁₆H₁₇ClN₃NaO₄
SMILES

O=C(CC1=C(N=C(CCCC)N1CC2=C([N+]([O-])=O)C=CC=C2)Cl)O[Na]
Synonyms

CV 2961
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Chiu AT, et al. Non-peptide angiotensin II receptor antagonists. II. Pharmacology of S-8308. Eur J Pharmacol. 1988 Nov 15;157(1):13-21.

[2]. Chiu AT, et al. Nonpeptide angiotensin II receptor antagonists. III. Structure-function studies. J Pharmacol Exp Ther. 1989 Sep;250(3):867-74. PMID: 2778716.

[3]. Freidinger RM. Non-peptide ligands for peptide receptors. Trends Pharmacol Sci. 1989 Jul;10(7):270-4.

[4]. Timmermans PB, et al. The discovery of a new class of highly specific nonpeptide angiotensin II receptor antagonists. American journal of hypertension. 1991 Apr;4(4 Pt 2):275S-281S.

[5]. Inada Y, et al. [Nonpeptide angiotensin II-receptor antagonists]. Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 1994 Sep;104(3):217-28.

[6]. Timmermans PB, et al. Nonpeptide angiotensin II receptor antagonists: a novel class of antihypertensive agents. Blood vessels. 1990;27(2-5):295-300.

[7]. Wong PC, et al. Angiotensin II receptor antagonists and receptor subtypes. Trends Endocrinol Metab. 1992 Aug;3(6):211-7.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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S 8308

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