Cosalane
Based on 1 publication(s) in Google Scholar
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.50%
- CAS 番号: 154212-56-3
- 分子式: C45H60Cl2O6
- 分子量:767.86
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Cosalane
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生物活性
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CCR7 2.43 μM (IC50) |
CXCR2 0.66 μM (IC50) |
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 (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.
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Animal Model:P815 murine mastocytoma (H-2d) leukemia B6D2 mice model
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Dosage:Incubated with donor Tcons at 15μg/mL ex vivo, one single dose
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Administration:Intravenous injection (i.v.) on tail with donor Tcons after Cosalane incubation
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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.
化学情報
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CAS 番号 154212-56-3
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性状 Solid
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分子量 767.86
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分子式 C45H60Cl2O6
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Color White to off-white
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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
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別名
NSC 658586
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Immunother Cancer
FMO2+ cancer-associated fibroblasts sensitize anti-PD-1 therapy in patients with hepatocellular carcinoma. [Abstract]2025 May 2;13(5):e011648. PMID: 40316306
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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 |
Cosalane 関連分類
HY-120427 関連分類
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