Taminadenant
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.84%
- CAS. Nr.: 1337962-47-6
- Formel: C10H8BrN7
- Molecular Weight:306.12
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Taminadenant
MoreAlle Adenosine Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Adenosine receptor[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (240-250 g; induced catalepsy by s.c. with 1 mg/kg Haloperidol (HY-14538))[1]
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Dosage:3, 10, or 30 mg/kg
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Administration:p.o.; single dosage
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Result:Dose-dependently attenuated the cataleptic effects of Haloperidol when administered 1 h after Haloperidol injection.
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Animal Model:Sprague-Dawley rats (240-250 g; induced tremulous jaw movement by s.c. with 1 mg/kg Pilocarpine (HY-B0726A))[1]
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Dosage:0.3, 3, or 7.5 mg/kg
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Administration:p.o.; single dosage
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Result:Dose-dependently attenuated pilocarpine-induced tremulous jaw movement, being effective at the lowest dose tested.
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Animal Model:
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Dosage:0.3 and 3 mg/kg
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Administration:p.o.; single dosage
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Result:Enhanced the effects of L-DOPA with a minimum efficacious dose (MED) of 3 mg/kg p.o..
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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]
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Dosage:0.3 or 3 mg/kg
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Administration:p.o.; single dosage
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Result:Showed a robust antiparkinsonian activity and displayed antidyskinetic efficacy.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1337962-47-6
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Appearance Solid
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Molecular Weight 306.12
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Formel C10H8BrN7
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Color White to off-white
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SMILES
BrC(C(N1C=CC=N1)=NC(N2C=CC=N2)=N3)=C3N
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Synonyms
NIR178; PBF509
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Adenosine A2A receptor is a tumor suppressor of NASH-associated hepatocellular carcinoma. [Abstract]2023 Sep 19;4(9):101188. PMID: 37729873
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Núñez F, et al. PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders. Front Pharmacol. 2018 Oct 19;9:1200. [Content Brief]
[2]. Chiappori AA, et al. Phase I Study of Taminadenant (PBF509/NIR178), an Adenosine 2A Receptor Antagonist, with or without Spartalizumab (PDR001), in Patients with Advanced Non-Small Cell Lung Cancer. Clin Cancer Res. 2022 Jun 1;28(11):2313-2320. [Content Brief]
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 |
Taminadenant Related Classifications
HY-109139 Related Classifications
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