L-765314 is a potent and selective antagonist of α1b adrenergic receptor with Ki of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively. It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure.
In vivo, the results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean Cmax of L-765314 (A322312) is 1.05 μM and the t1/2 is 0.5 h. L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD25>3 mg/kg for each). On the basis of the inhibition of pressor responses to the R1a subtype selective agonist A-61603, L-765314 appears to be selective versus the R1a receptor up to a dose of 0.3 mg/kg. The results of hypotensive potency in rats show that both L-765314 and terazosin tend to decrease heart rate (about 25 bpm at 1 mg/kg iv).
| Molecular Weight | 522.60 |
| Formula | C27H34N6O5 |
| CAS Number | 189349-50-6 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Adrenergic Receptor Products |
|---|
| CRN04894
CRN04894 is an orally nonpeptide, potent and selective antagonist for adrenocorticotropic hormone (ACTH) acting at the melanocortin 2 receptor (MC2R). CRN04894 blocks the action of ACTH at MC2R, providing a potential novel treatment for the diseases of ACTH excess such as Cushing’s disease, congenital adrenal hyperplasia, and ectopic ACTH-secreting tumors. |
| (Des-His6)-ACTH (1-24) (human, bovine, rat)
(Des-His6)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH). |
| ACTH (1-14)
ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production. |
| Mibenratide
Mibenratide, a small cyclic peptide, is an adrenergic β1 receptor antagonist. |
| Conopeptide rho-TIA
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
