Art. -Nr.: HY-19732

BIBS 39

Name: BIBS 39
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SKU: HY-19732
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BIBS 39 is a non-peptide angiotensin II receptor antagonist with antihypertensive activity, with higher affinity for the AT1 receptor than for the AT2 receptor. BIBS 39 competitively blocks AT1-mediated vasoconstriction and pressor responses, and effectively inhibits the activity of the renin-angiotensin-aldosterone system. BIBS 39 reduces diastolic blood pressure and induces mild, transient reflex tachycardia, with no off-target functional activity on the norepinephrine, K⁺/Cl⁻ or vasopressin pathways. BIBS 39 can be used in research related to hypertension and renal hypertension^[1][2^][3].

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Reinheit : 99.70%
CAS. Nr.: 133085-33-3
Formel: C₃₂H₃₆N₄O₃
Molecular Weight:524.65

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BIBS 39 Chemical Structure

CAS. Nr.: 133085-33-3

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

AT2 Receptor

AT1 Receptor

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

BIBS 39 (60 min) shows high affinity for AT₁ receptors in rat lung membranes (K_i=29 nM) and 17-fold selectivity for AT₁ over AT₂ receptors in rat adrenal medulla membranes^[1].
BIBS 39 (10^-8-10^-6 M; 30 min) acts as a competitive AII receptor antagonist in isolated rabbit aortic rings, with a pA₂ value of 8.14, and does not affect contractions induced by noradrenaline or KCl at 10^-5 M^[1].

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

In Vivo

BIBS 39 (0.3-10 mg/kg; i.v.; single dose) acts as a competitive, selective angiotensin II receptor antagonist in pithed normotensive rats, producing dose-dependent diastolic blood pressure reduction and parallel rightward shifts of AII dose-pressor response curves with a maximum shift factor of 228.3 at 10 mg/kg i.v^[1].
BIBS 39 (0.03-30 mg/kg; i.v.; cumulative doses at 15-minute intervals, single dose) is an effective antihypertensive agent in conscious renal hypertensive rats, with an ED₃₀ of 2.0 mg/kg i.v. and a 25-minute duration of action at a 1 mg/kg i.v. dose^[2].
BIBS 39 (1-10 mg/kg; i.v.; single dose) dose-dependently antagonizes AII-induced cardiovascular effects in propranolol-treated pithed rabbits, with a 10 mg/kg i.v. dose significantly reducing basal diastolic blood pressure and heart rate^[3].

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

Animal Model:

Wistar rats (male, 220-260 g, pithed)^[1]
Dosage:

0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

i.v.; single dose
Result:

Lowered diastolic blood pressure by 7.7 mmHg at 0.3 mg/kg, 10.0 mmHg at 1 mg/kg, 11.8 mmHg at 3 mg/kg, and 11.8 mmHg at 10 mg/kg.
Caused parallel rightward shifts of the AII log dose-pressor response curve with shift factors of 4.5 (0.3 mg/kg), 11.8 (1 mg/kg), 55.8 (3 mg/kg), and 228.3 (10 mg/kg).
Did not affect heart rate at any dose.
Did not alter log dose-pressor response curves for noradrenaline or vasopressin at 3 mg/kg.
Showed no agonistic activity (no increase in diastolic blood pressure).

Animal Model:

Wistar (male, 135-145 g, two-kidney, one-clip renal hypertension model)^[2]
Dosage:

0.03 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

i.v.; cumulative doses at 15-minute intervals (dose-response study); single dose (duration study)
Result:

Caused a significant, dose-dependent decrease in diastolic blood pressure (DBP).
Reduced DBP by 5-6 mmHg at 0.03 mg/kg i.v.
Achieved maximal DBP reduction of ~46 mmHg at 10 mg/kg i.v.
Had an ED₃₀ (dose lowering DBP by 30 mmHg) of 2.0 mg/kg i.v.
Showed no significant additional DBP reduction when captopril was administered after its maximal hypotensive dose.
Caused a significant, dose-dependent increase in heart rate (HR); increased HR by 40 beats/min at 10 mg/kg i.v.
Reduced DBP by 15.8 mmHg at 1 minute post-injection of 1 mg/kg i.v. dose.
Reached maximal DBP reduction of 25.5 mmHg at 3 minutes post-injection of 1 mg/kg i.v. dose.
Maintained antihypertensive effect for 25 minutes after 1 mg/kg i.v. dose.
Induced a small, transient HR increase of 30 beats/min at 3 minutes post-injection of 1 mg/kg i.v. dose.

Animal Model:

New Zealand White (male, 1.4-1.8 kg, pithed, propranolol pretreated)^[3]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

i.v.; single dose
Result:

Produced basal diastolic blood pressure (DBP) of 30 mmHg, left ventricular pressure (LVP) of 50 mmHg, left ventricular end-diastolic pressure (LVEDP) of -2.6 mmHg, dP/dtmax of 1,700 mmHg/s, and heart rate (HR) of 210 beats/min at 1 mg/kg i.v.
Produced basal DBP of 21 mmHg, LVP of 48 mmHg, LVEDP of -1.5 mmHg, dP/dtmax of 1,500 mmHg/s, and HR of 214 beats/min at 3 mg/kg i.v.
Caused statistically significant reduction in basal DBP (16 mmHg, p < 0.05 vs. propranolol-only group) and statistically significant reduction in basal HR (204 beats/min, p < 0.05 vs. propranolol-only group), alongside LVP of 46 mmHg, LVEDP of -1.8 mmHg, and dP/dtmax of 1,460 mmHg/s at 10 mg/kg i.v.
Caused parallel, rightward shifts of angiotensin II-induced dose-response curves for DBP and LVEDP without altering maximal angiotensin II-induced responses across all doses.

Related Protocols :

Research Protocol for Cardiovascular Diseases

Chemical Information

CAS. Nr. 133085-33-3
Appearance Solid
Molecular Weight 524.65
Formel C₃₂H₃₆N₄O₃
Color White to off-white
SMILES

O=C(C1=CC=CC=C1C2=CC=C(CN3C4=CC(NC(NC5CCCCC5)=O)=CC=C4N=C3CCCC)C=C2)O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 32 mg/mL (60.99 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9060 mL

9.5302 mL

19.0603 mL

5 mM

0.3812 mL

1.9060 mL

3.8121 mL

10 mM

0.1906 mL

0.9530 mL

1.9060 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 1.25 mg/mL (2.38 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1.25 mg/mL (2.38 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.38 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang J, et al. Characterization of BIBS 39 and BIBS 222: two new nonpeptide angiotensin II receptor antagonists[J]. European journal of pharmacology, 1992, 218(1): 35-41.

[2]. Zhang J, et al. Antihypertensive activity of the novel, nonpeptide angiotensin II receptor antagonists BIBS 39 and BIBS 222 in conscious renal hypertensive rats. Pharmacology. 1993;46(5):241-247. [Content Brief]

[3]. Zhang J, et al. Hemodynamic effects of angiotensin II and the influence of angiotensin receptor antagonists in pithed rabbits. J Cardiovasc Pharmacol. 1995;25(5):724-731. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9060 mL	9.5302 mL	19.0603 mL	47.6508 mL
	5 mM	0.3812 mL	1.9060 mL	3.8121 mL	9.5302 mL
	10 mM	0.1906 mL	0.9530 mL	1.9060 mL	4.7651 mL
	15 mM	0.1271 mL	0.6353 mL	1.2707 mL	3.1767 mL
	20 mM	0.0953 mL	0.4765 mL	0.9530 mL	2.3825 mL
	25 mM	0.0762 mL	0.3812 mL	0.7624 mL	1.9060 mL
	30 mM	0.0635 mL	0.3177 mL	0.6353 mL	1.5884 mL
	40 mM	0.0477 mL	0.2383 mL	0.4765 mL	1.1913 mL
	50 mM	0.0381 mL	0.1906 mL	0.3812 mL	0.9530 mL
	60 mM	0.0318 mL	0.1588 mL	0.3177 mL	0.7942 mL

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BIBS 39

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen