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Synonyms: NSC-658586, NSC 658586, NSC 640067

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $372 | In Stock | In Stock | |
| 5 mg | $868 | In Stock | In Stock | |
| 10 mg | $1,070 | In Stock | In Stock | |
| 25 mg | $1,590 | In Stock | In Stock |
| Description | Cosalane (NSC 658586) is a small-molecule inhibitor and a CCR7 and CXCR2 antagonist (IC50 = 2.43 μM and 0.66 μM, respectively), with broad-spectrum antiviral activity that blocks HIV-1, HIV-2, and other viral replication, used for HIV treatment and mitigation of acute graft-versus-host disease in allogeneic hematopoietic stem cell transplantation. |
| Targets & IC50 | HSA:1.24 ± 0.24 nM (Ki) |
| In vitro | Methods: Tcon cells were treated with Cosalane (10-30 μg/mL) for 72 hours in the presence of IL-2 supplementation to observe cell growth. Results: Cosalane promoted robust growth of Tcon cells with no difference in cell numbers.[1] Methods: Human or murine cells were treated with Cosalane to detect its blocking effect on CCL19- and CCL21-induced chemotaxis and receptor activation. Results: Cosalane (10 μg/mL, 1 hour) reduced chemotaxis of human H9 cells and mouse T cells toward CCL19 and CCL21; Cosalane showed similar activity against human and murine receptor orthologs, being more effective at blocking CCL19-induced receptor activation (IC50: human 0.207 μM, murine 0.193 μM) than CCL21 (IC50: human 2.66 μM, murine 1.98 μM).[2] |
| In vivo | Methods: In the B6D2 mouse model, Cosalane (15 μg/mL) was administered via intravenous injection 1 hour before transplantation after in vitro cell culture, and TNF and IFN-γ levels in host colon were measured on day 14 post-transplantation; additionally, in the P815 mouse mastocytoma leukemia model, a single intravenous injection of Cosalane (15 μg/mL, after in vitro culture) was given to observe tumor growth and survival. Results: Cosalane treatment reduced TNF and IFN-γ levels in mouse colon, significantly inhibited tumor growth, and prolonged overall survival.[1] Methods: In SD rats, single intravenous injections of different doses of Cosalane (1-10 mg/kg) were administered to determine its pharmacokinetic parameters; and in normal and BC rats, single intravenous injection of Cosalane (10 mg/kg) was given to analyze plasma drug elimination. Results: The steady-state volume of distribution (Vdss) of Cosalane in rats was dose-dependent, being 23.1 mL/g at 10 mg/kg and 12.6 mL/g at 5 mg/kg; and the drug was eliminated from plasma in a bi-exponential manner.[3] |
| Synonyms | NSC-658586, NSC 658586, NSC 640067 |
| Molecular Weight | 767.86 |
| Formula | C45H60Cl2O6 |
| Cas No. | 154212-56-3 |
| Smiles | C[C@@]12[C@@]3([C@]([C@]4([C@](C)(CC3)[C@@]([C@@H](CCCC(C)C)C)(CC4)[H])[H])(CC[C@]1(C[C@@H](CCC=C(C5=CC(C(O)=O)=C(O)C(Cl)=C5)C6=CC(C(O)=O)=C(O)C(Cl)=C6)CC2)[H])[H])[H] |
| Relative Density. | 1.191g/cm3 |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (130.23 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (4.3 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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