MK-8318 |
Catalog No.GC31851
One-Click Copy Product Info
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MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1416581-40-2
Sample solution is provided at 25 µL, 10mM.
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MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
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].
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].
[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.
| Cas No. | 1416581-40-2 | SDF | |
| Canonical 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 | ||
| Formula | C27H26F4N2O5 | M.Wt | 534.5 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8709 mL | 9.3545 mL | 18.7091 mL |
| 5 mM | 374.2 μL | 1.8709 mL | 3.7418 mL |
| 10 mM | 187.1 μL | 935.5 μL | 1.8709 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)