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

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

Cat. No.: HY-109022 Purity: 99.93%
Handling Instructions Technical Support

Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.

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Atogepant

Atogepant 화학구조

CAS No. : 1374248-81-3

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

Other Forms of Atogepant:

Top Publications Citing Use of Products
  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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.

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
분자량

603.52

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
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.

  • 몰농도 계산기

  • 농도 희석 계산기

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
순도&문서

Purity: 99.93%

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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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.

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Inquiry Information

상품명:
Atogepant
Cat. No.:
HY-109022
수량:
MCE Japan Authorized Agent: