In vitro: BAR 501 is a selective GPBAR1 agonist devoid of FXR agonistic activity. It effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1, with an EC50 of 1 μM. Exposure of GLUTAg cells to BAR501 (10 μM) increases the expression of GLP-1 mRNA by 2.5 folds.
In vivo: Pretreating rats for 6 days with BAR501, 15 mg/kg, reduces basal portal pressure and blunts the vasoconstriction activity of norepinephrine. Pretreatment with BAR501 attenuates the hepatic vasomotor activity induced by shear stress and methoxamine. Administration of BAR501 exerts a direct vasodilatory activity in the CCl4 model. Treating mice with BAR501 at the dose of 15 mg/Kg reduces portal pressure and AST plasma levels. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity.
Cell Experiment | |
---|---|
Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
---|---|
Animal models | Mice bearing GM-CSF-secreting B16 tumors |
Formulation | 5% DMA, 47.5% propylene glycol |
Dosages | 75 mg/kg b.i.d |
Administration | s.c. |
Molecular Weight | 406.64 |
Formula | C26H46O3 |
CAS Number | 1632118-69-4 |
Solubility (25°C) | 10mM in DMSO |
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 CGRP Receptor Products |
---|
Adrenomedullin (16-31), human
Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). |
α-CGRP(human)
α-CGRP(human) is a regulatory neuropeptide of 37 amino acids. |
Adrenomedullin (AM) (22-52), human
Adrenomedullin (AM) (22-52), human is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat. |
Calcitonin Gene Related Peptide (CGRP) II, rat
Calcitonin Gene Related Peptide (CGRP) II, rat, a CGRP receptor activator, is a potent and long-lasting vasodilator. |
Adrenomedullin (11-50), rat
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.