2. Anti-infection Immunology/Inflammation GPCR/G Protein
  3. CXCR HIV
  4. GSK812397

GSK812397是一种CXCR4拮抗剂，对HIV感染的抑制具有潜力。为了评估GSK812397的临床潜力，需要公斤级别的试剂候选物。本文描述了CXCR4拮抗剂GSK812397的改进型、可扩展的合成路线。这一新路线已在50升固定设备中放大，以在五步反应中以20%的总产率和>99%的化学纯度及对映体纯度获得1.2公斤试剂物质。CXC趋化因子受体4（CXCR4）是一种7跨膜蛋白，部分作为HIV-1多种菌株的宿主共受体发挥作用。人们认为，针对CXCR4将有助于抑制几种细胞病变晚期病毒的复制；因此，CXCR4拮抗剂是实验性抗HIV试剂最有前途的新类之一。GSK812397是一种强效的CXCR4拮抗剂，因此是抑制HIV感染的研究对象。

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GSK812397 Chemical Structure

GSK812397 Chemical Structure

CAS No. : 878197-98-9

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GSK812397 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 1000 nM
Compound: GSK-812397
Cytotoxicity against HEK293 cells after 24 hrs by MTS assay
Cytotoxicity against HEK293 cells after 24 hrs by MTS assay
[PMID: 19949058]
HEK293 IC50
0.56 nM
Compound: GSK-812397
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay
[PMID: 19949058]
HEK293 IC50
0.87 nM
Compound: GSK-812397
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated 30 mins before agonist challenge by FLIPR assay
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated 30 mins before agonist challenge by FLIPR assay
[PMID: 19949058]
HEK293 IC50
1.07 nM
Compound: GSK-812397
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated before agonist challenge measured after 15 mins by FLIPR assay
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated before agonist challenge measured after 15 mins by FLIPR assay
[PMID: 19949058]
HEK293 IC50
1.71 nM
Compound: GSK-812397
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay in presence of 45 mg/ml human serum albumin
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay in presence of 45 mg/ml human serum albumin
[PMID: 19949058]
HEK293 IC50
1.97 nM
Compound: GSK-812397
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay in presence of alpha-acid glycoprotein and human serum albumin
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay in presence of alpha-acid glycoprotein and human serum albumin
[PMID: 19949058]
HEK293 IC50
1.99 nM
Compound: GSK-812397
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay in presence of 1 mg/ml alpha-acid glycoprotein
Inhibition of HIV1 HXB2 gp120-mediated viral infusion into HEK293 cells after 24 hrs by luciferase reporter gene assay in presence of 1 mg/ml alpha-acid glycoprotein
[PMID: 19949058]
HEK293 IC50
2.41 nM
Compound: GSK-812397
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced increase in intracellular calcium level treated 15 mins before agonist challenge measured after 1 hr by FLIPR assay
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced increase in intracellular calcium level treated 15 mins before agonist challenge measured after 1 hr by FLIPR assay
[PMID: 19949058]
HEK293 IC50
26.64 nM
Compound: GSK-812397
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated 30 mins before agonist challenge measured after 45 mins post compound washout by FLIPR assay
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated 30 mins before agonist challenge measured after 45 mins post compound washout by FLIPR assay
[PMID: 19949058]
HEK293 IC50
3.36 nM
Compound: GSK-812397
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated before agonist challenge measured after 5 mins by FLIPR assay
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated before agonist challenge measured after 5 mins by FLIPR assay
[PMID: 19949058]
HOS IC50
> 1000 nM
Compound: GSK-812397
Cytotoxicity against human HOS cells infected with HIV1 3B after 72 hrs by celltiter glow assay
Cytotoxicity against human HOS cells infected with HIV1 3B after 72 hrs by celltiter glow assay
[PMID: 19949058]
HOS IC50
> 1000 nM
Compound: GSK-812397
Antiviral activity against HIV1 Bal infected in human HOS cells after 72 hrs by luminescence assay
Antiviral activity against HIV1 Bal infected in human HOS cells after 72 hrs by luminescence assay
[PMID: 19949058]
HOS IC50
1.23 nM
Compound: GSK-812397
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay
[PMID: 19949058]
HOS IC50
2.01 nM
Compound: GSK-812397
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay in presence of 45 mg/ml human serum albumin
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay in presence of 45 mg/ml human serum albumin
[PMID: 19949058]
HOS IC50
2.87 nM
Compound: GSK-812397
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay in presence of 1 mg/ml alpha-acid glycoprotein
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay in presence of 1 mg/ml alpha-acid glycoprotein
[PMID: 19949058]
HOS IC50
3.14 nM
Compound: GSK-812397
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay in presence of alpha-acid glycoprotein and human serum albumin
Antiviral activity against HIV1 3B infected in human HOS cells after 72 hrs by luminescence assay in presence of alpha-acid glycoprotein and human serum albumin
[PMID: 19949058]
PBMC IC50
> 1000 nM
Compound: GSK-812397
Cytotoxicity against human PBMC infected with HIV1 3B after 7 days by celltiter glow assay
Cytotoxicity against human PBMC infected with HIV1 3B after 7 days by celltiter glow assay
[PMID: 19949058]
U2OS IC50
2.1 nM
Compound: GSK-812397
Antagonist activity at mouse CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at mouse CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
[PMID: 19949058]
U2OS IC50
4.3 nM
Compound: GSK-812397
Antagonist activity at rat CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at rat CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
[PMID: 19949058]
U2OS IC50
6.6 nM
Compound: GSK-812397
Antagonist activity at human CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at human CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
[PMID: 19949058]
U2OS IC50
7.8 nM
Compound: GSK-812397
Antagonist activity at monkey CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at monkey CXCR4 expressed in human U2OS cells assessed as inhibition of SDF1-induced increase in intracellular calcium level by FLIPR assay
[PMID: 19949058]
U-937 IC50
0.34 nM
Compound: GSK-812397
Inhibition of CXCR4-mediated chemotaxis in SDF1-stimulated human U937 cells treated 15 mins before SDF1 challenge measured after 2 hrs by luminescence assay
Inhibition of CXCR4-mediated chemotaxis in SDF1-stimulated human U937 cells treated 15 mins before SDF1 challenge measured after 2 hrs by luminescence assay
[PMID: 19949058]
分子量

420.55

Formula

C24H32N6O
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

GSK812397 相关分类

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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.

Keywords:

GSK812397878197-98-9GSK 812397GSK-812397CXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusInhibitorinhibitorinhibit

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