1. Anti-infection
  2. HIV
  3. BMS-585248

BMS-585248 是一种有效的第三代 HIV-1 附着抑制剂,具有良好的体外和体内药代动力学特征。

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BMS-585248 Chemical Structure

BMS-585248 Chemical Structure

CAS No. : 619331-12-3

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查看 HIV 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile[1].

IC50 & Target

HIV-1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MT2 EC50
0.8 nM
Compound: 12m, BMS-585428
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in absence of human serum
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in absence of human serum
[PMID: 23360431]
MT2 EC50
2.3 nM
Compound: 12m, BMS-585428
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in presence of human serum
Antiviral activity against HIV1 BRU infected in MT2 cells after 4 to 5 days by reverse transcriptase assay in presence of human serum
[PMID: 23360431]
U-87MG ATCC IC50
< 5 nM
Compound: 29
Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay
Antiviral activity against HIV1 pseudovirus in U87 cells expressing CD4 and CCR5 after 72 hrs by M33 pseudotyped assay
[PMID: 18052117]
U-87MG ATCC CC50
> 40000 nM
Compound: 3
Cytotoxicity against human U87 cells coexpressing CD4, CxCR4 receptors after 72 hrs
Cytotoxicity against human U87 cells coexpressing CD4, CxCR4 receptors after 72 hrs
[PMID: 19534463]
体内研究
(In Vivo)

BMS-585248 (静脉注射 (1 mg/kg) 和口服 (5-200 mg/kg); 一次)具有良好的药代动力学特征,雄性大鼠静脉注射 (1mg /kg) 和口服 (5mg /kg) 后,AUC 值分别为 3220 nM·h 和 8064 nM·h。

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

Animal Model: Male rats[1]
Dosage: 5, 15, and 200 mg/kg
Administration: Orally, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of BMS-585248 in male rats[1].
PO
Dose (mg/kg) 15 75 200
Cmax (μM) 6.6 8.4 11
AUCtot (μM·h) 42 115 145
分子量

447.42

Formula

C22H18FN7O3

CAS 号
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.

纯度 & 产品资料
参考文献

BMS-585248 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BMS-585248
目录号:
HY-13829
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