2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. MK-8617

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.

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MK-8617 Chemical Structure

MK-8617 Chemical Structure

CAS No. : 1187990-87-9

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Based on 3 publication(s) in Google Scholar

MK-8617 Related Antibodies

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  • Protocol

  • Purity & Documentation

  • References

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Description

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.

IC50 & Target

IC50: 1 nM (PHD2)[1]
In Vitro

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2. MK-8617 is not a significant inhibitor of the cytochrome p450 enzymes in vitro (IC50), CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6, >60 μM, and is a moderate reversible inhibitor of CYP2C8 at 1.6 μM in vitro. The IC50 of MK-8617 is determined for factor inhibiting HIF (FIH) to be 18 μM[1].

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

MK-8617 Related Antibodies
In Vivo

Tritiated MK-8617 exhibits minimal metabolic turnover in liver microsomes from rat, dog, and monkey (<10% turover) but significant turnover in human liver microsomes (34% turnover) after 60 min (10 μM MK-8617, 1 mg/mL microsomal protein). In terms of its pharmacokinetic profile, MK-8617 shows good oral bioavailability across species (36 to 71%), with low clearance and volume of distribution. After 48 h treatment of MK-8617, postdose recovery of the radioactivity is about 26% bile, 12% urine, and 38% in feces, indicating that ~38% of the MK-8617 is absorbed and eliminated into bile and urine which is consistent with the oral bioavailability (~36%) observed in the rat study. MK-8617 also elicits an increase in erythropoietin (EPO) levels with a mouse MED of 1.5 mpk when dosed iv[1].

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

443.45

Formula

C24H21N5O4
CAS No.
Unlabeled CAS

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C(C2=NN=CC=C2)N=C1O)NC(C3=CC=C(OC)C=C3)C4=CC=C(OC)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (13.53 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 2.2550 mL 11.2752 mL 22.5505 mL
5 mM 0.4510 mL 2.2550 mL 4.5101 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Kinase Assay
[1]

The catalytic activity assays for the HIF-PHD isoforms are performed at subsaturating levels of 2-oxoglutarate. To each well of a 96-well plate are added 1 μL of MK-8617 in DMSO and 20 μL of assay buffer containing 0.15 μg/mL FLAG-tagged full length HIF-PHD isoform expressed in and purified from baculovirus-infected Sf9 cells. After a 30 min preincubation at room temperature, the enzymatic reactions are initiated by the addition of 4 μL of substrates. After 2 h at room temperature, the reactions are terminated and signals are developed by the addition of a 25 μL quench/detection mix to a final concentration of 1 mM ortho-phenanthroline, 0.1 mM EDTA, 0.5 nM anti-(His)6 LANCE reagent, 100 nM AF647-labeled streptavidin, and 2 μg/mL (His)6-VHL complex. The ratio of time-resolved fluorescence signals at 665 and 620 nm is determined, and percent inhibition is calculated relative to an uninhibited control sample run in parallel[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Male Sprague-Dawley rats (approximately 300 g each, n=15/arm) are dosed once daily for 28 days with vehicle (25:75 v/v PEG200/water+1 mol equiv of NaOH) or MK-8617 (1.5 or 15 mg/kg in vehicle). A group of age-matched, untreated controls (n=15) are included in the experiment. On study days 3, 14, and 28, blood samples (~0.25 mL) are obtained via jugular venipuncture and on study day 36 by cardiocentesis for hematological and MK-8617 level analyses[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2550 mL 11.2752 mL 22.5505 mL 56.3761 mL
5 mM 0.4510 mL 2.2550 mL 4.5101 mL 11.2752 mL
10 mM 0.2255 mL 1.1275 mL 2.2550 mL 5.6376 mL
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MK-8617 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:

MK-86171187990-87-9MK8617MK 8617HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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