计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A 2A receptor (A 2A R) 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 . Taminadenant reactivate the antitumor immune response
In Vitro
Taminadenant (PBF509) does not show any agonist efficacy in HEK cells permanently expressing the human A 2A R SNAP , but completely antagonizes the agonist-mediated cAMP accumulation in A 2A R SNAP expressing HEK cells with an IC 50 of 72.8 ± 17.4 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE 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 ) 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 ) 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 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 for 14 days and i.p. 15 mg/kg Benserazide hydrochloride ) Dosage: 0.3 or 3 mg/kg Administration: p.o.; single dosage Result: Showed a robust antiparkinsonian activity and displayed antidyskinetic efficacy.
IC50& Target:Adenosine receptor
规格
别名
塔米纳登特
规格或纯度
10mM in DMSO
英文名称
Taminadenant
生化机理
Taminadenant（NIR178；PBF509）是一种高效口服活性腺苷 A 2A 受体（A 2A R）拮抗剂。Taminadenant 可拮抗 A2AR 激动剂介导的 cAMP 积累和阻抗反应，其 K B 值分别为 72.8 nM 和 8.2 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
技术文档
高级数据
产品属性
| ALogP | 1.2 |
|---|
关联靶点（人）
ADORA2A
Tclin
腺苷受体A2a(Adenosine receptor A2a)
(0 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1337962-47-6，分子式为 C10H8BrN7，分子量为 306.13 g/mol。
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每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
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