2. GPCR/G Protein
  3. Angiotensin Receptor
  4. BIBS 39

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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BIBS 39

BIBS 39 Chemical Structure

CAS No. : 133085-33-3

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BIBS 39 Related Antibodies

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Description

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].

IC50 & Target[1]

AT2 Receptor

 

AT1 Receptor

 

In Vitro

BIBS 39 (60 min) shows high affinity for AT1 receptors in rat lung membranes (Ki=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.

BIBS 39 Related Antibodies
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.
Molecular Weight

524.65

Formula

C32H36N4O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9060 mL 9.5302 mL 19.0603 mL
5 mM 0.3812 mL 1.9060 mL 3.8121 mL
View the Complete Stock Solution Preparation Table

* 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.

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  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BIBS 39133085-33-3BIBS39BIBS-39Angiotensin Receptorangiotensin IIrabbit aortic ringsrenin-angiotensin-aldosterone systemrat lung membraneshypertensionrat adrenal medulla membranespithed normotensive ratsAT 2 receptorsAT 1 receptorsrenal hypertensive rats
Inhibitorinhibitorinhibit

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