2. GPCR/G Protein Immunology/Inflammation Anti-infection
  3. CCR CXCR HIV HSV
  4. 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).

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Cosalane Chemical Structure

Cosalane Chemical Structure

CAS No. : 154212-56-3

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Based on 1 publication(s) in Google Scholar

Cosalane Related Antibodies

Top Publications Citing Use of Products

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

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HIV HIV-1 HIV-2

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HSV-1 HSV-2 HSV

  • Biological Activity

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Description

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].

IC50 & Target[3]

CCR7

2.43 μM (IC50)

CXCR2

0.66 μM (IC50)

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 Tcon 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].

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

Cosalane Related Antibodies
In Vivo

Cosalane (15 μg/mL in ex vivo donor Tcons incubation, i.v. with Tcons, 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 Tcons incubation, i.v. with Tcons, one single dose) demonstrates substantial suppression of tumor growth and the longest overall survival times in P815 murine mastocytoma (H-2d) leukemia B6D2 mice model[1].
Cosalane (1-10 mg/kg, i.v., one single dose) gives a Vdss 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].

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

Animal Model: P815 murine mastocytoma (H-2d) leukemia B6D2 mice model
Dosage: Incubated with donor Tcons at 15μg/mL ex vivo, one single dose
Administration: Intravenous injection (i.v.) on tail with donor Tcons after Cosalane incubation
Result: Demonstrated aggressive tumor growth with 100% malignancy-related mortality in mice given BM cells plus tumor without Tcons.
Rejected the P815 inoculum but developed aggressive aGVHD in BM/tumor plus DMSO-treated Tcons mice.
Demonstrated substantial suppression of tumor growth and the longest overall survival times in P815 murine mastocytoma (H-2d) leukemia B6D2 mice model.
Molecular Weight

767.86

Formula

C45H60Cl2O6
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (130.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3023 mL 6.5116 mL 13.0232 mL
5 mM 0.2605 mL 1.3023 mL 2.6046 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.78%

SDS (251 KB)

COA (249 KB) HNMR (187 KB) LCMS (151 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3023 mL 6.5116 mL 13.0232 mL 32.5580 mL
5 mM 0.2605 mL 1.3023 mL 2.6046 mL 6.5116 mL
10 mM 0.1302 mL 0.6512 mL 1.3023 mL 3.2558 mL
15 mM 0.0868 mL 0.4341 mL 0.8682 mL 2.1705 mL
20 mM 0.0651 mL 0.3256 mL 0.6512 mL 1.6279 mL
25 mM 0.0521 mL 0.2605 mL 0.5209 mL 1.3023 mL
30 mM 0.0434 mL 0.2171 mL 0.4341 mL 1.0853 mL
40 mM 0.0326 mL 0.1628 mL 0.3256 mL 0.8140 mL
50 mM 0.0260 mL 0.1302 mL 0.2605 mL 0.6512 mL
60 mM 0.0217 mL 0.1085 mL 0.2171 mL 0.5426 mL
80 mM 0.0163 mL 0.0814 mL 0.1628 mL 0.4070 mL
100 mM 0.0130 mL 0.0651 mL 0.1302 mL 0.3256 mL
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Cosalane Related Classifications

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:

Cosalane154212-56-3NSC 658586NSC658586NSC-658586CCRCXCRHIVHSVCC chemokine receptorCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusHerpes simplex virusCCR7CXCR2antagonistCCL19CCL21aGVHDHSCTInhibitorinhibitorinhibit

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