Taminadenant HCl hydrate (PBF-509; NIR-178)

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Cat #: V3945 CAS #: 2253894-78-7 Purity ≥ 99%

Description: 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.

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Molecular Weight (MW)	N/A
Molecular Formula	N/A
CAS No.	2253894-78-7
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: N/A
	Water: N/A
	Ethanol: N/A
SMILES Code	N/A
Synonyms	PBF509; NIR178; NIR 178; PBF 509; PBF-509; NIR-178

Related Biological Data

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.	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.	Immunoreactivity of A2AR in the striatum of 6-OHDA-lesioned rats. Front Pharmacol. 2018 Oct 19;9:1200.	PBF509-mediated potentiation of l-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 of l-DOPA (4 mg/kg) was monitored during a 2 h period. Front Pharmacol. 2018 Oct 19;9:1200.

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%DMSO + % + %Tween 80 + %ddH₂O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(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.
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