BIBS-39 is a novel, nonpeptide angiotensin II receptor antagonist, showing antihypertensive activity. In contrast to the angiotensin II receptor subtype 1 (AT1) selective drug DuP 753, BIBS-39 also displays affinity for the angiotensin II receptor subtype 2. BIBS 39 displaced [125I] AII from its specific binding sites with a K(i) value of 29 +/- 7 nM for the AII subtype I (AT1) receptor and a K(i) value of 480 +/- 110 nM for the AII subtype 2 (AT2) receptor. BIBS 39 appears to be effective antihypertensives in the model of the renal hypertensive rat.
MedKoo Cat#: 522996
Name: BIBS-39
CAS#: 133085-33-3
Chemical Formula: C32H36N4O3
Exact Mass: 524.2787
Molecular Weight: 524.67
Elemental Analysis: C, 73.26; H, 6.92; N, 10.68; O, 9.15
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 30.0 | 57.18 | |
| DMSO | 30.0 | 57.18 | |
| DMSO:PBS (pH 7.2) (1:3) | 0.3 | 0.48 |
The following data is based on the product molecular weight 524.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
