CAS:442908-10-3Vipadenant

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Vipadenant 3-(4-氨基-3-甲基苄基)-7-(呋喃-2-基)-3H-[1,2,3]三唑并[4,5-d]嘧啶-5-胺 Cat No. FB05121Cas No. 442908-10-3

Synonyms: BIIB-014;V2006

Vipadenant is an adenosine antagonist with Ki of 1.3 nM and 68 nM for A2A and A1, respectively. Vipadenant is a selective A2A receptor antagonist with Ki values of 1.3, 68, 63, and 1,005 nM for A2A, A1, A2B, and A3 receptors, respectively, used in development for for Parkinson's disease.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1120 mL
- 15.5598 mL
- 31.1197 mL
- 5 mM
- 0.6224 mL
- 3.1120 mL
- 6.2239 mL
- 10 mM
- 0.3112 mL
- 1.5560 mL
- 3.1120 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

442908-10-3

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C16H15N7O

运输

蓝冰

分子量

321.34

别名

BIIB-014;V2006

溶解度

DMSO	31.0 mg/mL (96.5 mM)

动物实验配方

靶点数据

生物活性

靶点 Adenosine Receptor A2A

Ki:1.3nM Adenosine Receptor A1

Ki:68nM
描述Vipadenant is a selective Adenosine A2A receptor with Ki value of 1.3nM. It exhibits much lower affinity to A1 and A2B with Ki value of 63nM, and Ki value of 1005nM for A3. Vipadenant had a minimum effective dose of 0.1 and 1 mg/kg in the mouse and rat haloperidol-induced hypolocomotion models in vivo, respectively. Vipadenant was able to increase contralateral rotations in 6-OHDA lesioned rats when dosed orally in combination with apomorphine at 3 and 10 mg/kg. Vipadenant also showed reversal of motor disability in MPTP-treated marmosets without dyskinesias at a minimum effective dose of <5 mg/kg, p.o.^[1].

动物研究

剂量

Rat: 2 mg/kg, 5 mg/kg^[2] (p.o.); 1 mg/kg, 2 mg/kg^[2] (i.v.); 0.3 mg/kg - 30 mg/kg^[3] (i.p.)

给药途径

p.o., i.v., i.p.

动物药代数据

Animal	Rats^[2]
Dose	2 mg/kg
Administration	p.o. or i.v.
F	30.4 ± 8.9%
T_1/2	65.2 ± 20.2 min (p.o.) 71.2 ± 8.5 min (i.v.)
T_max	7.5 ± 5.0 min (p.o.) 2.0 ± 0.0 min (i.v.)
AUC_last	16716.4 ± 7245.0 min·ng/ml (p.o.) 90694.2 ± 18814.6 min·ng/ml (i.v.)
CL	22.5 ± 4.3 ml/min/kg (i.v.)
C_max	229.7 ± 88.0 min (p.o.) 3091.0 ± 221.6 min (i.v.)
Vss	1209.3 ± 174.4 ml/kg (i.v.)

靶点	Description	IC50
Adenosine Receptor A2A		Ki:1.3nM
Adenosine Receptor A1		Ki:68nM