Home>>Signaling Pathways>> Chromatin/Epigenetics>> HIF>>Adaptaquin

Adaptaquin (Synonyms: HIF prolyl hydroxylase inhibitor)

Catalog No.GC12487

HIF-prolyl hydroxylase-2 (PHD2) inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

Adaptaquin Chemical Structure

Cas No.: 385786-48-1

Size Price Stock Qty
5mg
$61.00
In stock
10mg
$102.00
In stock
50mg
$327.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Background

Adaptaquin is a selective hydroxyquinoline HIF prolyl hydroxylase (HIF-PHD) inhibitor [1][2].

The hypoxia-inducible factor prolyl hydroxylase domain enzymes (HIF-PHDs) are a family of oxygen sensors that has been implicated in neuronal survival. Catalysis by the HIF-PHDs destabilizes the transcriptional activator HIF-1a under normoxia. HIF-PHDs are promising target candidates for mitochondrial protection in paradigms of oxidative stress. The inhibition of HIF-PHDs prevented neuronal cell death induced by mitochondrial toxins [1][2].

Adaptaquin is a hydroxyquinoline HIF-PHD inhibitor. Adaptaquin inhibited purified and recombinant PHD2. Adaptaquin (30 mg/kg) penetrated the blood-brain barrier, resulting in inhibition of the oxygen-sensing HIF-PHDs and activation of HIF-dependent gene expression [1]. In HT-22 cells, Adaptaquin protected against glutamate-induced cell death. Adaptaquin could also restore the mitochondrial ATP production [2].

In intracerebral hemorrhage (ICH) mice model, Adaptaquin decreased edema and significantly improved tape removal task, which were associated with a reduction in the number of degenerating neurons in perihematomal and hematomal areas of the mouse striatum [1].

References:
[1].  Karuppagounder SS, Alim I, Khim SJ, et al. Therapeutic targeting of oxygen-sensing prolyl hydroxylases abrogates ATF4-dependent neuronal death and improves outcomes after brain hemorrhage in several rodent models. Sci Transl Med. 2016 Mar 2;8(328):328ra29.
[2].  Neitemeier S, Dolga AM, Honrath B, et al. Inhibition of HIF-prolyl-4-hydroxylases prevents mitochondrial impairment and cell death in a model of neuronal oxytosis. Cell Death Dis. 2016 May 5;7:e2214.

Chemical Properties

Cas No. 385786-48-1 SDF
Synonyms HIF prolyl hydroxylase inhibitor
Chemical Name 7-[(4-chlorophenyl)[(3-hydroxy-2-pyridinyl)amino]methyl]-8-quinolinol
Canonical SMILES OC1=CC=CN=C1NC(C2=CC=C(Cl)C=C2)C3=C(O)C(N=CC=C4)=C4C=C3
Formula C21H16ClN3O2 M.Wt 377.8
Solubility ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6469 mL 13.2345 mL 26.469 mL
5 mM 0.5294 mL 2.6469 mL 5.2938 mL
10 mM 0.2647 mL 1.3235 mL 2.6469 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg 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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 ddH2O, 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.

Reviews

Review for Adaptaquin

Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Adaptaquin

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.