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

Taminadenant  (Synonyms: NIR178; PBF509)

Cat. No.: HY-109139 Purity: 99.84%
COA Handling Instructions

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Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response.

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Taminadenant Chemical Structure

Taminadenant Chemical Structure

CAS No. : 1337962-47-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 66 In-stock
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50 mg USD 220 In-stock
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Based on 1 publication(s) in Google Scholar

Taminadenant Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Taminadenant

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

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  • Purity & Documentation

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  • Customer Review

Description

Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response[1][2].

IC50 & Target

Adenosine receptor[1]
In Vitro

Taminadenant (PBF509) does not show any agonist efficacy in HEK cells permanently expressing the human A2ARSNAP, but completely antagonizes the agonist-mediated cAMP accumulation in A2ARSNAP expressing HEK cells with an IC50 of 72.8 ± 17.4 nM[1].

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

Taminadenant Related Antibodies
In Vivo

Taminadenant (PBF509) (0.3, 3, 7.5, 10, or 30 mg/kg; p.o.; single dosage) attenuates the cataleptic effects of Haloperidol, attenuates pilocarpine-induced tremulous jaw movement, enhances the effects of L-DOPA, shows a robust antiparkinsonian activity and displays antidyskinetic efficacy[1].

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

Animal Model: Sprague-Dawley rats (240-250 g; induced catalepsy by s.c. with 1 mg/kg Haloperidol (HY-14538))[1]
Dosage: 3, 10, or 30 mg/kg
Administration: p.o.; single dosage
Result: Dose-dependently attenuated the cataleptic effects of Haloperidol when administered 1 h after Haloperidol injection.
Animal Model: Sprague-Dawley rats (240-250 g; induced tremulous jaw movement by s.c. with 1 mg/kg Pilocarpine (HY-B0726A))[1]
Dosage: 0.3, 3, or 7.5 mg/kg
Administration: p.o.; single dosage
Result: Dose-dependently attenuated pilocarpine-induced tremulous jaw movement, being effective at the lowest dose tested.
Animal Model: Sprague-Dawley rats (240-250 g; induced hemiparkinsonian by unilateral injection of 6-OHDA (HY-B1081) in the medial forebrain bundle)[1]
Dosage: 0.3 and 3 mg/kg
Administration: p.o.; single dosage
Result: Enhanced the effects of L-DOPA with a minimum efficacious dose (MED) of 3 mg/kg p.o..
Animal Model: Sprague-Dawley rats (240-250 g; induced dyskinesias by i.p. 4 mg/kg L-DOPA (HY-N0304) for 14 days and i.p. 15 mg/kg Benserazide hydrochloride (HY-B0404A))[1]
Dosage: 0.3 or 3 mg/kg
Administration: p.o.; single dosage
Result: Showed a robust antiparkinsonian activity and displayed antidyskinetic efficacy.
Clinical Trial
Molecular Weight

306.12

Formula

C10H8BrN7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

BrC(C(N1C=CC=N1)=NC(N2C=CC=N2)=N3)=C3N
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 : 125 mg/mL (408.34 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 3.2667 mL 16.3335 mL 32.6669 mL
5 mM 0.6533 mL 3.2667 mL 6.5334 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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  • 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 (6.79 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.79 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 99.84%

COA (253 KB) LCMS (93 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 3.2667 mL 16.3335 mL 32.6669 mL 81.6673 mL
5 mM 0.6533 mL 3.2667 mL 6.5334 mL 16.3335 mL
10 mM 0.3267 mL 1.6333 mL 3.2667 mL 8.1667 mL
15 mM 0.2178 mL 1.0889 mL 2.1778 mL 5.4445 mL
20 mM 0.1633 mL 0.8167 mL 1.6333 mL 4.0834 mL
25 mM 0.1307 mL 0.6533 mL 1.3067 mL 3.2667 mL
30 mM 0.1089 mL 0.5444 mL 1.0889 mL 2.7222 mL
40 mM 0.0817 mL 0.4083 mL 0.8167 mL 2.0417 mL
50 mM 0.0653 mL 0.3267 mL 0.6533 mL 1.6333 mL
60 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3611 mL
80 mM 0.0408 mL 0.2042 mL 0.4083 mL 1.0208 mL
100 mM 0.0327 mL 0.1633 mL 0.3267 mL 0.8167 mL
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Taminadenant 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:

Taminadenant1337962-47-6NIR178 PBF509NIR 178NIR-178PBF509PBF 509PBF-509Adenosine ReceptorP1 receptormovement disordersincluding catalepsytremorhemiparkinsonismantitumorInhibitorinhibitorinhibit

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