(R)-VU 6008667

目录号: GC38110纯度: >99.50%
(R)-VU6008667 是 VU6008667 的活性对映异构体,是一种口服活性的乙酰胆碱受体 5 亚型 (M5 NAM) 抑制剂,IC50 值分别为 1.2 μM (human) 和 1.6 μM (rat)。(R)-VU6008667 对 M5 的选择性高于 M1-4,CNS 渗透率高。

(R)-VU 6008667
Cas No.: 2097818-14-7
规格价格库存数量操作
1mg¥540.00现货
1
5mg¥1,620.00现货
1
10mg¥2,970.00现货
1
25mg¥6,750.00现货
1
50mg¥12,150.00现货
1
100mg¥20,250.00现货
1
200mg询价现货
1
500mg询价现货
1

文献被引

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    31, 1291–1307 (2021)

产品描述 Description

(R)-VU 6008667, an active enantiomer of VU6008667, is a orally active acetylcholine receptor subtype 5 (M5 NAM) inhibitor with IC50 values of 1.2 μM (human) and 1.6 μM (rat), respectively. (R)-VU6008667 is selective for M5 over M1-4, high CNS penetration[1].

(R)-VU6008667 (intravenous injection, 1mg/kg; orally administration, 3 mg/kg) displays the desired diminished elimination half-life (t1/2= 2.3 hr) driven by a smaller volume (Vss=7.4 L/kg) and higher clearance (CLp= 82 mL/min/kg), with moderate oral bioavailability (17% F) in rat. (PK study)[1].

[1]. Jung ME, et al.Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.Bioorg Med Chem Lett. 2016 Jun 1;26(11):2719-23

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
2097818-14-7
SMILES
O=C1N2[C@](N(C(C3=CC=C(F)C(F)=C3)=O)CC2)(C4=CC=C(Cl)C(C)=C4)C5=C1C=CC=C5
分子式
C24H17ClF2N2O2
分子量
438.85 g/mol
溶解性
DMSO: 100 mg/mL (227.87 mM)
保存条件
Store at -20°C
General tips
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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol