2. GPCR/G Protein
  3. Adenosine Receptor
  4. Imaradenant

Imaradenant  (Synonyms: HTL1071; AZD4635)

Cat. No.: HY-101980 Purity: 99.55%
SDS COA Handling Instructions

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AZD4635 (HTL1071) est un récepteur de l'adénosine A2A (A2AR) qui est puissant, sélectif et oralement actif. AZD4635 se lie à l'A2AR humain avec un Ki de 1,7 nM et présente une sélectivité >30 fois supérieure à celle des autres récepteurs de l'adénosine.

AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.

For research use only. We do not sell to patients.

Imaradenant Chemical Structure

Imaradenant Chemical Structure

CAS No. : 1321514-06-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
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Based on 3 publication(s) in Google Scholar

Imaradenant Related Antibodies

Top Publications Citing Use of Products

View All Adenosine Receptor Isoform Specific Products:

View All Isoforms
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors[1].

IC50 & Target

Ki: 1.7 nM (A2AR)[1]
Cellular Effect
Cell Line Type Value Description References
T-cell EC50
725.1 nM
Compound: AZD4635
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
Antagonist activity at A2AAR in human T -cells assessed as increase in IL-2 production preincubated for 1 hr followed by CD3/CD28 monoclonal antibody addition and measured after 24 hrs in presence of NECA by ELISA
[PMID: 35714367]
In Vitro

In the presence of 0.1, 1 and 10 μM adenosine, the IC50s of AZD4635 for inhibition of cAMP production are 0.79, 10.0 and 142.9 nM, respectively[1].

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

Imaradenant Related Antibodies
Clinical Trial
Molecular Weight

315.73

Formula

C15H11ClFN5
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

NC1=NC(C2=CC=C(F)C=C2)=C(C3=CC(Cl)=NC(C)=C3)N=N1
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 : ≥ 83.3 mg/mL (263.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1673 mL 15.8363 mL 31.6726 mL
5 mM 0.6335 mL 3.1673 mL 6.3345 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.68%

SDS (393 KB)

COA (252 KB) HNMR (212 KB) LCMS (137 KB)

Handling Instructions (2659 KB)
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 3.1673 mL 15.8363 mL 31.6726 mL 79.1816 mL
5 mM 0.6335 mL 3.1673 mL 6.3345 mL 15.8363 mL
10 mM 0.3167 mL 1.5836 mL 3.1673 mL 7.9182 mL
15 mM 0.2112 mL 1.0558 mL 2.1115 mL 5.2788 mL
20 mM 0.1584 mL 0.7918 mL 1.5836 mL 3.9591 mL
25 mM 0.1267 mL 0.6335 mL 1.2669 mL 3.1673 mL
30 mM 0.1056 mL 0.5279 mL 1.0558 mL 2.6394 mL
40 mM 0.0792 mL 0.3959 mL 0.7918 mL 1.9795 mL
50 mM 0.0633 mL 0.3167 mL 0.6335 mL 1.5836 mL
60 mM 0.0528 mL 0.2639 mL 0.5279 mL 1.3197 mL
80 mM 0.0396 mL 0.1980 mL 0.3959 mL 0.9898 mL
100 mM 0.0317 mL 0.1584 mL 0.3167 mL 0.7918 mL
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Imaradenant 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:

Imaradenant1321514-06-0HTL1071 AZD4635HTL 1071HTL-1071AZD4635AZD 4635AZD-4635Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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