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]}. In Vitro:Cosalane (10 μg/mL, 1 h) reduces chemotaxis in response to both CCL19 and CCL21 in human H9 cells and mouse T cells^[2].
Cosalane (10-30 μg/mL, 72 h) results in robust growth of T_con cells with supplemental IL-2, and no differences in cell numbers^[1].
Cosaline (0.01-100 μM) exhibits nearly identical activity against the human and murine orthologues of the receptor and is more active in blocking receptor activation by CCL19 (IC₅₀ = 0.207 μM in human and IC₅₀ = 0.193 μM in murine) than CCL21 (IC₅₀ = 2.66 μM in human and IC₅₀ = 1.98 μM in murine)^[2]. In Vivo:Cosalane (15 μg/mL in ex vivo donor T_cons incubation, i.v. with T_cons, 1 h before transplant) reduces TNF and IFN-γ levels in the host colon on day +14 in the cosalane group of (A and B) B6D2 mice^[1].
Cosalane (15 μg/mL in ex vivo donor T_cons incubation, i.v. with T_cons, one single dose) demonstrates substantial suppression of tumor growth and the longest overall survival times in P815 murine mastocytoma (H-2^d) leukemia B6D2 mice model^[1].
Cosalane (1-10 mg/kg, i.v., one single dose) gives a Vd_ss value of 23.1 mL/g at 10 mg/kg and 12.6 mL/g at 5 mg/kg in SD rats^[5].
Cosalane (10 mg/kg, i.v., one single dose) shows the disappearance of Cosalane from the plasma followed a biexponential decline in normal and BC rats^[5].