| Bioactivity | L-771688 is a highly selective α1A-Adrenoceptor antagonist with a Ki of 0.43±0.02 nM. |
| Target | Ki: 0.43±0.02 nM (α1A-Adrenoceptor) |
| Invitro | Specific [3H]L-771688 binding to cloned human α1A-Adrenoceptors is inhibited with high potency by subtype selective compounds, GG818 (Ki=0.026±0.002 nM) and L-771688 (Ki=0.052±0.008 nM) and subtype non-selective α1-adrenoceptor antagonists, prazosin (Ki=0.088±0.0.032 nM) and terazosin (Ki=1.8±0.65 nM). The relative amount of [3H]L-771688 (0.5 nM) binding in various rat tissue membranes is highest in submaxillary gland (9.5 pmol/g tissue), followed by brain (5.8 pmol/g tissue), vas deferens (4.3 pmol/g tissue), kidney (3.4 pmol/g tissue), heart (1.5 pmol/g tissue), urethra (1.1 pmol/g tissue) and prostate (0.88 pmol/g tissue). In contrast, low specific [3H]L-771688 binding is observed in rat urinary bladder (0.55 pmol/g tissue), liver (0.44 pmol/g tissue), aorta (0.11 pmol/g tissue) and spleen (0.11 pmol/g tissue)[1]. |
| Name | L-771688 |
| CAS | 200050-59-5 |
| Formula | C28H33F2N5O5 |
| Molar Mass | 557.59 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Chang RS, et al. In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist. Eur J Pharmacol. 2000 Dec 15;409(3):301-12. |