产品
编 号：F124450
分子式：C10H8BrN7
分子量：306.12
分子式：C10H8BrN7
分子量：306.12
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
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询价
结构图
CAS No: 1337962-47-6
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Sprague-Dawley rats (240-250 g; induced catalepsy by s.c. with 1 mg/kg Haloperidol (HY-14538))
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))
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)
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))
Dosage:0.3 or 3 mg/kg
Administration:p.o.; single dosage
Result:Showed a robust antiparkinsonian activity and displayed antidyskinetic efficacy.
体外研究：
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.
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.
体内研究：
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.Animal Model:Sprague-Dawley rats (240-250 g; induced catalepsy by s.c. with 1 mg/kg Haloperidol (HY-14538))
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))
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)
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))
Dosage:0.3 or 3 mg/kg
Administration:p.o.; single dosage
Result:Showed a robust antiparkinsonian activity and displayed antidyskinetic efficacy.
体外研究：
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.
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