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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
화학식: C₂₇H₂₆F₄N₂O₅
분자량:534.50

보관:

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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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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)

All Prostaglandin Receptor Isoforms :

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
분자량 534.50
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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MK-8318

All Prostaglandin Receptor Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

MK-8318 Related Classifications

HY-112604 Related Classifications