规格

价格

库存

数量

1 mg

¥ 35,900

10-14周

5 mg

¥ 71,900

5日内发货

生物活性

产品描述	BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains.
靶点活性	HIV-1:（EC50）15 nM
体外活性	BI 224436 has cellular cytotoxicity of more than 90 μM. BI 224436 has a low, 2.1-fold decrease in antiviral potency in the presence of 50% human serum. BI 224436 has drug-like in vitro absorption, distribution, metabolism, and excretion (ADME) properties, including Caco-2 cell permeability, solubility, and low cytochrome P450 inhibition[1]. BI 224436 retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q. BI 224436 displays an additive effect in combination with most approved antiretrovirals, including INSTIs.
体内活性	BI 224436 exhibits excellent pharmacokinetic profiles in rat (clearance as a percentage of hepatic flow [CL], 0.7%; bioavailability [F], 54%), monkey (CL, 23%; F, 82%), and dog (CL, 8%; F, 81%)[1].

化学信息

分子量	442.51
分子式	C₂₇H₂₆N₂O₄
CAS No.	1155419-89-8
Smiles	Cc1nc2ccccc2c(-c2ccc3OCCc4ccnc2c34)c1[C@H](OC(C)(C)C)C(O)=O
密度	1.277 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 50 mg/mL (112.99 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (5.65 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO