VU6028418|cas:2649803-05-2|西域试剂

VU6028418,99.52%

产品编号：Bellancom-141711| CAS NO：2649803-05-2| 分子式：C₂₃H₂₇F₃N₄O| 分子量：432.48

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-141711		￥5800.00	杭州北京（现货）
Bellancom-141711		￥10500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

VU6028418

产品介绍

VU6028418 是一种有效的、高选择性的、具有口服活性的 M₄ mAChR 拮抗剂，对 hM₄ 的 IC₅₀ 值为 4.1 nM。

生物活性

VU6028418 is a potent, highly selective and orally bioavailable M₄ mAChR antagonist with an IC₅₀ of 4.1 nM against hM₄.

体外研究

体内研究

VU6028418 is orally bioavailable.
In Vivo PK Parameters for VU6028418

parameter	rat (SD)^a	mouse (CD-1)^a	dog (beagle)^a
dose (mg/kg) iv/po	1/10	1/3	1/3
CL_p (mL/min/kg)	6.1	17	43
V_ss (L/kg)	6.7	10.6	8.5
elimination t_1/2 (h)	13	NC	15
C_max (ng/mL) po	17 000	181	70
T_max (h) po	1.5	6.67	17
AUC_0-inf (ng/mL•h) po	30 000	NC	1100
F (%) po	≥100	≥100	86
total brain/total plasma (K_p)	6.4	ND	ND
unbound brain/unbound plasma (K_p,uu)	0.61	ND	ND
CSF/plasma unbound (K_p,u)	0.24	ND	ND

^a Values represent means from two to three animals. ND = not determined. NC = not calculated; there was insufficient data to define the elimination phase (i.e., C_max was one of the last three time points).

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

Animal Model:	SD rat, CD-1 mouse and beagle dog
Dosage:	1, 3 and 10 mg/kg
Administration:	Intravenous injection or oral administration (Pharmacokinetic Analysis)
Result:	Showed good pharmacokinetic results.

体内研究

VU6028418 is orally bioavailable.
In Vivo PK Parameters for VU6028418

parameter	rat (SD)^a	mouse (CD-1)^a	dog (beagle)^a
dose (mg/kg) iv/po	1/10	1/3	1/3
CL_p (mL/min/kg)	6.1	17	43
V_ss (L/kg)	6.7	10.6	8.5
elimination t_1/2 (h)	13	NC	15
C_max (ng/mL) po	17 000	181	70
T_max (h) po	1.5	6.67	17
AUC_0-inf (ng/mL•h) po	30 000	NC	1100
F (%) po	≥100	≥100	86
total brain/total plasma (K_p)	6.4	ND	ND
unbound brain/unbound plasma (K_p,uu)	0.61	ND	ND
CSF/plasma unbound (K_p,u)	0.24	ND	ND

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

Animal Model:	SD rat, CD-1 mouse and beagle dog
Dosage:	1, 3 and 10 mg/kg
Administration:	Intravenous injection or oral administration (Pharmacokinetic Analysis)
Result:	Showed good pharmacokinetic results.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5.56 mg/mL (12.86 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3122 mL	11.5612 mL	23.1225 mL
5 mM	0.4624 mL	2.3122 mL	4.6245 mL
10 mM	0.2312 mL	1.1561 mL	2.3122 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式