| Size | Price | Stock | Qty |
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Taminadenant (PBF-509; NIR-178) is a novel, oral and potent adenosine receptor antagonist used as an immunotherapy agent. It functions as a strong and specific antagonist of the human A2A (adenosine 2A) receptor, binding to the receptor with a Ki value of 12 nM. It prevents A2AR from being expressed on T cells, negating the effect of adenosine and A2AR on T cell suppression. Additionally, it triggers an immune response by T cells against tumor cells, which in turn slows the growth of tumor cells that are vulnerable to it. It is also mentioned as a possible pro-dopaminergic medication for the treatment of Parkinson's disease (PD).
| Targets |
Adenosine receptor
|
|---|---|
| ln Vitro |
Taminadenant (PBF509) completely blocks agonist-mediated cAMP accumulation, with an IC50 of 72.8 ± 17.4 nM i HEK cells that express human A2ARSNAP permanently[1]. However, it does not demonstrate any agonist efficacy in these cells.
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| ln Vivo |
Taminadenant (PBF509) (0.3, 3, 7.5, 10, or 30 mg/kg; p.o.; single dosage) increases the effects of L-DOPA, exhibits a strong antiparkinsonian activity, and reduces the cataleptic effects of haloperidol[1]. It also lessens the tremulous jaw movement caused by pilocarpine.
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| Animal Protocol |
Sprague-Dawley rats (240-250 g; induced catalepsy by s.c. with 1 mg/kg Haloperidol (HY-14538))
3, 10, or 30 mg/kg p.o.; single dosage |
| References |
| Molecular Formula |
C10H8BRN7
|
|---|---|
| Molecular Weight |
306.127
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| Exact Mass |
305
|
| Elemental Analysis |
C, 39.24; H, 2.63; Br, 26.10; N, 32.03
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| CAS # |
1337962-47-6
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| Related CAS # |
2253894-78-7 (HCl hydrate); 1337962-47-6; 2253894-81-2 (mesylate); 2253894-80-1 (sulfate); 2253894-79-8 (HCl dihydrate)
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| Appearance |
Solid powder
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| SMILES |
C1=CN(N=C1)C2=NC(=NC(=C2Br)N)N3C=CC=N3
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| InChi Key |
ATFXVNUWQOXRRU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8BrN7/c11-7-8(12)15-10(18-6-2-4-14-18)16-9(7)17-5-1-3-13-17/h1-6H,(H2,12,15,16)
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| Chemical Name |
5-bromo-2,6-di(pyrazol-1-yl)pyrimidin-4-amine
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| Synonyms |
PBF 509; NIR178; PBF509; NIR 178; Taminadenant; PBF-509; NIR-178
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~125 mg/mL (~408.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2666 mL | 16.3329 mL | 32.6659 mL | |
| 5 mM | 0.6533 mL | 3.2666 mL | 6.5332 mL | |
| 10 mM | 0.3267 mL | 1.6333 mL | 3.2666 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04895748 | Active Recruiting |
Drug: DFF332 Drug: RAD001 Drug: PDR001 |
Carcinoma, Renal Cell | Novartis Pharmaceuticals | November 30, 2021 | Phase 1 |
Products are for research use only; We do not sell to patients
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