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Taminadenant HCl (PBF509; NIR178) is a novel potent and oral non-xhantine non-furan A2AR (adenosine) antagonist with the potential to be used as a pro-dopaminergic drug for PD management. PBF509 was shown to be a highly potent ligand at the human A2AR, since it antagonized A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 ± 17.4 and 8.2 ± 4.2 nM, respectively. PBF509 (orally) antagonized haloperidol-mediated catalepsy, reduced pilocarpine-induced tremulous jaw movements and potentiated the number of contralateral rotations induced by L-3,4-dihydroxyphenylalanine (L-DOPA) in unilaterally 6-OHDA-lesioned rats. Moreover, PBF509(3 mg/kg) inhibited L-DOPA-induced dyskinesia (LID), showing not only its efficacy on reversing parkinsonian motor impairments but also acting as antidyskinetic agent.
| References |
Front Pharmacol.2018 Oct 19;9:1200;Neoplasia. 2017 Jul; 19(7): 530–536.
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| CAS # |
2253894-78-7
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| Appearance |
Typically exists as solid at room temperature
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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 |
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| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
Inhibition of A2AR-mediated cAMP accumulation. Inhibition of the CGS21680-mediated cAMP accumulation. A SCH442416 and PBF509 concentration-response inhibition curve of CGS21260-mediated cAMP was assessed in HEK-293 cells permanently expressing the A2ARSNAP.Front Pharmacol.2018 Oct 19;9:1200. |
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PBF509 blocks A2AR-mediated whole cell label-free responses.Front Pharmacol.2018 Oct 19;9:1200. |
PBF509 reverses haloperidol-induced catalepsy. Rats were pretreated with haloperidol (1.0 mg/kg, s.c.) and 1 h later the selected cataleptic animals were orally administered with either vehicle or PBF509 (3, 10, and 30 mg/kg, p.o.).Front Pharmacol.2018 Oct 19;9:1200. |
PBF509 attenuates pilocarpine-induced tremulous jaw movements.Effect of different doses of SCH442416 and PBF509 on pilocarpine-induced tremulous jaw movements. The number of jaw movements were recorded during 1 h in rats orally administered with vehicle (Veh), SCH442416 or PBF509 (0.3–7.5 mg/kg) before (20 min) pilocarpine administration (1 mg/kg, i.p.).Front Pharmacol.2018 Oct 19;9:1200. |
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Immunoreactivity of A2AR in the striatum of 6-OHDA-lesioned rats.Front Pharmacol.2018 Oct 19;9:1200. |
PBF509-mediated potentiation ofl-DOPA-induced contralateral rotations in 6-OHDA-lesioned rats. The number of contralateral rotations in 6-OHDA-lesioned rats orally administered with vehicle (Veh) or SCH420814 and PBF509 (0.3 and 3 mg/kg) in the absence or presence ofl-DOPA (4 mg/kg) was monitored during a 2 h period.Front Pharmacol.2018 Oct 19;9:1200. |
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