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Cat. No.: HY-112604

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MK-8318

MK-8318 is a potent and selective CRTh2 receptor antagonist with a K_i of 5.0 nM.

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CAS No.: 1416581-40-2
Formule: C₂₇H₂₆F₄N₂O₅
Masse moléculaire:534.50

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

MK-8318 Chemical Structure

CAS No.: 1416581-40-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

MK-8318 is a potent and selective CRTh2 receptor antagonist with a K_i of 5.0 nM.

IC₅₀ & Target^[1]

5.0 nM (Ki)

β-arrestin

3.5 nM (IC₅₀)

cAMP

8.0 nM (IC₅₀)

CYP3A4

50 μM (IC₅₀)

CYP2C9

50 μM (IC₅₀)

CYP2D6

50 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform Prostaglandin Receptor :

In Vitro

MK-8318 also inhibits β-arrestin, cAMP, CYP3A4, CYP2C9, and CYP2D6 with IC₅₀s of 3.5±2.1 nM, 8.0±6.8 nM, 50 µM, 50 µM and 50 µM^[1].

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

In Vivo

In a sheep model, MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mg/kg. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy. MK-8318 also displays good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mg/kg oral dosing^[1].

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

Chemical Information

CAS No. 1416581-40-2
Masse moléculaire 534.50
Formule C₂₇H₂₆F₄N₂O₅
SMILES

FC1=CC=C(N(C(C2=CC=C(OC(F)(F)F)C=C2)=O)[C@@H](CCC3)[C@@H]3[C@H]4N(C(CCC(O)=O)=O)C5CC5)C4=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Huang X, et al. Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684. [Content Brief]

Calculators

Calculateur de molarité

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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MK-8318

Voir tous les produits spécifiques à Isoform Prostaglandin Receptor

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

MK-8318 Related Classifications

HY-112604 Related Classifications