Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316 311, and pexacerfont (P<0.001 for all comparisons collapse across time-points); the latter three treatments in turn do not differ from each other. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, P<0.001). Accordingly, detailed Post hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6 h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline)
Biochem Biophys Res Commun. 2020 Apr 30;525(2):326-333.
Spexin as an Anxiety Regulator in Mouse Hippocampus: Mechanisms for Transcriptional Regulation of Spexin Gene Expression by Corticotropin Releasing Factor
Verucerfont purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague-Dawley rats |
| Formulation | |
| Dosages | 5 mL/kg |
| Administration | oral |
| Molecular Weight | 406.48 |
| Formula | C22H26N6O2 |
| CAS Number | 885220-61-1 |
| Solubility (25°C) | 77 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 CRFR Products |
|---|
| K41498 TFA
K41498 TFA is an antisauvagine-30 (aSvg-30) analog and a strongly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM, and 425 nM for human CRF2α, CRF2β, and CRF1 receptors, respectively.K41498 TFA inhibits sauvagine-stimulated cAMP accumulation in hCRF2α/hCRF2β expressing cells. K41498 TFA can be used in hypotension studies. |
| Astressin 2B TFA
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist with IC50 values of 1.3 and > 500 nM for CRF2 and CRF1, respectively. |
| Urocortin, rat
Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively. |
| Urocortin, human
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively. |
| CRF(6-33)(human)
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. |
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