2. GPCR/G Protein Neuronal Signaling
  3. CGRP Receptor
  4. Atogepant

Atogepant  (Synonyms: MK-8031; AGN-241689)

Cat. No.: HY-109022 Purity: 99.90%
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Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.

For research use only. We do not sell to patients.

Atogepant Chemical Structure

Atogepant Chemical Structure

CAS No. : 1374248-81-3

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1 mg USD 560 In-stock
5 mg USD 1590 In-stock
10 mg USD 2540 In-stock
25 mg USD 5000 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Atogepant:

Atogepant Related Antibodies

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Description

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Atogepant Related Antibodies
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]

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

603.52

Formula

C29H23F6N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1[C@]2(CC3=CC(C(N[C@H]4C[C@](C5=C(C(F)=CC=C5F)F)([H])[C@H](N(C4=O)CC(F)(F)F)C)=O)=CN=C3C2)C6=CC=CN=C6N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (165.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6569 mL 8.2847 mL 16.5695 mL
5 mM 0.3314 mL 1.6569 mL 3.3139 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.90%

COA (259 KB) HNMR (304 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6569 mL 8.2847 mL 16.5695 mL 41.4236 mL
5 mM 0.3314 mL 1.6569 mL 3.3139 mL 8.2847 mL
10 mM 0.1657 mL 0.8285 mL 1.6569 mL 4.1424 mL
15 mM 0.1105 mL 0.5523 mL 1.1046 mL 2.7616 mL
20 mM 0.0828 mL 0.4142 mL 0.8285 mL 2.0712 mL
25 mM 0.0663 mL 0.3314 mL 0.6628 mL 1.6569 mL
30 mM 0.0552 mL 0.2762 mL 0.5523 mL 1.3808 mL
40 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0356 mL
50 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8285 mL
60 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6904 mL
80 mM 0.0207 mL 0.1036 mL 0.2071 mL 0.5178 mL
100 mM 0.0166 mL 0.0828 mL 0.1657 mL 0.4142 mL
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Atogepant Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Atogepant1374248-81-3MK-8031 AGN-241689MK8031MK 8031AGN241689AGN 241689AGN-241689CGRP ReceptorCalcitonin gene-related peptide receptororally activemigraineHEK293 cells.Inhibitorinhibitorinhibit

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