Atogepant
CAS No. : 1374248-81-3
(Synonyms: MK-8031; AGN-241689)
Price and Availability of
CAS No. : 1374248-81-3
| Size | Price | Stock |
|---|---|---|
| 1mg | $195 | In-stock |
| 5mg | $340 | In-stock |
| 10mg | $420 | In-stock |
| 25mg | $850 | In-stock |
| 50mg | $1500 | In-stock |
| 100mg | $2650 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-109022 |
| M.Wt: | 603.52 |
| Formula: | C29H23F6N5O3 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
Introduction of
1374248-81-3
:
Functional potency of atogepant for human cloned CGRP and related receptors[2]
In Vivo:Atogepant (3, 10, 30 mg/kg; Oral gavage (p.o.); Once a day; 9 days) improvement is observed in abnormal facial pain induced by nitroglycerin in rats, and in capsaicin-induced dermal vasodilation in primates[2].
Atogepant concentrations and concentration ratios in plasma, cerebrospinal fluid and brain tissue (Sprague-Dawley rats)[2]
Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine[1][2].
IC50 & Target:CGRP[1]
In Vitro:
Binding affinities (Ki, nM)a of atogepant for human and non-human CGRP receptors[2]
| Species | Human (cloned) | Human (native) | Rhesus | Rat | Mouse | Rabbit | Dog |
| K i (nM) | 0.015 | 0.026 | 0.009 | 0.7 | 0.13 | 2.1 | 1.2 |
Functional potency of atogepant for human cloned CGRP and related receptors[2]
| Receptor | CGRP | AM1 | AM2 | CRT | AMY1 | AMY3 |
| IC50 (nM) | 0.026 | >18000 | 400 | 6274 | 2.4 | 1418 |
Atogepant concentrations and concentration ratios in plasma, cerebrospinal fluid and brain tissue (Sprague-Dawley rats)[2]
| Parameter | Plasma Cmax (ng/mL) | CSF Cmax (ng/mL) | Brain Cmax (ng/g) | CSF/plasma Cmax ratios (ng/ml) | Brain/plasma Cmax ratios (ng/ml) | Brain/CSF Cmax ratios (ng/ml) | Plasma AUC0-last (ng h/ml) | CSF AUC0-last (ng h/ml) | Brain AUC0-last (ng h/g) | CSF/plasma AUC0-last ratios (ng h/ml) | Brain/plasma AUC0-last ratios (ng h/ml) | Brain/CSF AUC0-last ratios (ng h/ml) |
| Atogepant 5 mg/kg | 180.7 | 0.9 | 2.4 | 0.005 | 0.0133 | 2.6667 | 1110.9 | 4.2 | 17.9 | 0.0038 | 0.0161 | 4.2619 |
| Atogepant 20 mg/kg | 853.7 | 3.7 | 17.3 | 0.0043 | 0.0203 | 4.6757 | 6511.7 | 20.0 | 102.3 | 0.0031 | 0.0157 | 5.1150 |
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