Taminadenant NIR178; PBF509|cas:1337962-47-6|西域试剂

Taminadenant NIR178; PBF509,99.84%

产品编号：Bellancom-109139| CAS NO：1337962-47-6| 分子式：C₁₀H₈BrN₇| 分子量：306.12

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-109139	￥1100.00	杭州北京（现货）
Bellancom-109139	￥1600.00	杭州北京（现货）
Bellancom-109139	￥4900.00	杭州北京（现货）
Bellancom-109139	￥7900.00	杭州北京（现货）

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Taminadenant NIR178; PBF509

产品介绍

Taminadenant (NIR178; PBF509) 是一种高效且具有口服活性的腺苷 A_2A 受体 (adenosine A_2A receptor) 拮抗剂。Taminadenant 可拮抗 A2AR 激动剂介导的 cAMP 积累和阻抗反应，K_B 值分别为 72.8 nM 和 8.2 nM。Taminadenant 能逆转运动障碍大鼠模型的运动障碍，包括僵硬、震颤和偏侧震颤麻痹。与 Spartalizumab (HY-P9972) 联合使用时，Taminadenant 还能够抑制肿瘤生长。Taminadenant 能重新激活抗肿瘤免疫反应。

生物活性

Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A_2A receptor (A_2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with K_B 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.

体外研究

Taminadenant (PBF509) does not show any agonist efficacy in HEK cells permanently expressing the human A_2AR^SNAP, but completely antagonizes the agonist-mediated cAMP accumulation in A_2AR^SNAP expressing HEK cells with an IC₅₀ of 72.8 ± 17.4 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (408.34 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2667 mL	16.3335 mL	32.6669 mL
5 mM	0.6533 mL	3.2667 mL	6.5334 mL
10 mM	0.3267 mL	1.6333 mL	3.2667 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。