VU0409106

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VU0409106

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1276617-62-9

VU0409106 是一种有效的选择性mGlu₅负变构调节剂 (NAM), 其IC₅₀值为 24 nM。VU0409106 在小鼠模型中具有浓度依赖性的抗焦虑作用。VU0409106 还可穿过血脑屏障。

生物活性

VU0409106 is a potent and selectivemGlu₅negative allosteric modulator (NAM) with anIC₅₀of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB)^[1]^[2].

IC₅₀& Target

mGlu₅

24 nM (IC₅₀)

体内研究
(In Vivo)

VU0409106 (10 mg/kg; i.p.; once) penetrates the blood-brain barrier (BBB) and demonstrates good brain to plasma ratio that near unity^[1].

Animal Model:

CD-1 mice^[1]

Dosage:

10 mg/kg (10% Tween 80 formulation)

Administration:

Intraperitoneal injection.

Result:

1.19Pharmacokinetic Parameters of VU0409106 in CD-1 mice^[1].

	IP (10 mg/kg)
Plasma T_max(h)	0.25
Plasma C_max(ng/mL)	1450
Brain T_max(h)	0.25
Brain C_max(ng/mL)	1350
AUC_plasma(ng/mLoh)	702
AUC_brain(ng/mLoh)	696
B/P ratio	0.99

分子量

330.34

Formula

C₁₅H₁₁FN₄O₂S

CAS 号

1276617-62-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.