Cosalane

Cosalane (NSC 658586) is a CCR7 (IC50 = 2.43 μM) and CXCR2 antagonist (IC50 = 0.66 μM) . Cosalane is an inhibitor of HIV replication with a wide range of activity against HIV-1 isolates, HIV-2, Rauscher murine leukemia virus, HSV-1, HSV-2 and human cytomegalovirus. Cosalane inhibits both attachment of gp120 to CD4. Cosalane inhibits human and murine CCR7 in response to both CCL19 and CCL21 agonists. Cosalane can be studied in research for HIV or attenuating acute graft-versus-host disease (aGVHD) in allogeneic hematopoietic stem cell transplantation (HSCT) [1][2][3][4][5].

Product Specifications

CAS Number

[154212-56-3]

Product Name Alternative

NSC 658586

UNSPSC

12352005

Target

CCR; CXCR; HIV; HSV

Type

Reference compound

Related Pathways

Anti-infection; GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-anti-virus

Field of Research

Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/cosalane.html

Purity

99.78

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC(CCC[C@H]([C@H]1CC[C@]2([C@@]3(CC[C@]4(C[C@H](CC[C@@]4([C@]3(CC[C@]12C)[H])C)CC/C=C(C5=CC(C(O)=O)=C(C(Cl)=C5)O)/C6=CC(C(O)=O)=C(C(Cl)=C6)O)[H])[H])[H])C)C

Molecular Formula

C45H60Cl2O6

Molecular Weight

767.86

References & Citations

[1]Fowler KA, et al., The Ex Vivo Treatment of Donor T Cells with Cosalane, an HIV Therapeutic and Small-Molecule Antagonist of CC-Chemokine Receptor 7, Separates Acute Graft-versus-Host Disease from Graft-versus-Leukemia Responses in Murine Hematopoietic Stem Cell Transplantation Models. Biol Blood Marrow Transplant. 2019 Jun;25 (6) :1062-1074.|[2]Hull-Ryde EA, et al., Identification of Cosalane as an Inhibitor of Human and Murine CC-Chemokine Receptor 7 Signaling via a High-Throughput Screen. SLAS Discov. 2018 Dec;23 (10) :1083-1091.|[3]Max Van Hoof, et al., Optimization of triazolo[4,5-d]pyrimidines towards human CC chemokine receptor 7 (CCR7) antagonists, European Journal of Medicinal Chemistry, Volume 251, 2023, 115240, ISSN 0223-5234.|[4]Santhosh KC, et al., Correlation of anti-HIV activity with anion spacing in a series of cosalane analogues with extended polycarboxylate pharmacophores. J Med Chem. 2001 Mar 1;44 (5) :703-14.|[5]5. Udata C, et al., Enhanced transport of a novel anti-HIV agent--cosalane and its congeners across human intestinal epithelial (Caco-2) cell monolayers. Int J Pharm. 2003 Jan 2;250 (1) :157-68.