Abaucin
Based on 28 publication(s) in Google Scholar
RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
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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: 99.59%
- CAS 番号: 300815-41-2
- 分子式: C21H21F3N2O2
- 分子量:390.40
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Abaucin
More- Nat Immunol. 2024 Oct;25(10):1959-1975. [Abstract]
- Adv Funct Mater. 2026 Jun 11.
- J Adv Res. 2025 Mar:69:515-529. [Abstract]
- J Adv Res. 2020 Jul 22:28:231-243. [Abstract]
- Theranostics. 2020 Apr 27;10(13):5687-5703. [Abstract]
- Adv Sci (Weinh). 2026 Jun 22:e22159. [Abstract]
- Adv Sci (Weinh). 2025 Jul 17:e07167. [Abstract]
- Sci Adv. 2026 Jun 26;12(26):eaee8580. [Abstract]
- Sci Adv. 2023 Aug 2;9(31):eadg6856. [Abstract]
- Cell Death Dis. 2022 Feb 17;13(2):158. [Abstract]
- J Neuroinflammation. 2023 Nov 17;20(1):270. [Abstract]
- Acta Pharmacol Sin. 2025 Dec 1. [Abstract]
- J Eur Acad Dermatol Venereol. 2020 Apr;34(4):862-872. [Abstract]
- Stem Cell Res Ther. 2025 Mar 1;16(1):108. [Abstract]
- Stem Cell Res Ther. 2021 Jul 2;12(1):378. [Abstract]
- Hum Reprod. 2019 Apr 1;34(4):646-658. [Abstract]
- Life Sci. 2020 Nov 15:261:118360. [Abstract]
- Liver Int. 2022 Dec;42(12):2696-2712. [Abstract]
- Hepatol Commun. 2026 Apr 24;10(5):e0928.
- Eur J Pharmacol. 2021 Aug 5:904:174165. [Abstract]
- Int Immunopharmacol. 2023 Feb:115:109731. [Abstract]
- Mol Med Rep. 2017 Sep;16(3):3387-3394. [Abstract]
- Sci Rep. 2025 May 15;15(1):16869. [Abstract]
- Exp Cell Res. 2020 Nov 1;396(1):112289. [Abstract]
- Brain Sci. 2025 Feb 27;15(3):255. [Abstract]
- J Interferon Cytokine Res. 2020 May;40(5):245-253. [Abstract]
- J Interferon Cytokine Res. 2019 Apr;39(4):224-232. [Abstract]
- Cell Biomater. 2026 Feb 4.
Customer Validation & Images
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In Vivo Efficacy Study
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Flow Cytometry
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In Vivo Efficacy Study
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Histological Imaging/Staining
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IF
生物活性
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CCR2 360 nM (IC50) |
CCR1 17800 nM (IC50) |
Human α1a receptor 130 nM (IC50) |
Human α1d receptor 320 nM (IC50) |
5HT-1a receptor 470 nM (IC50) |
RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and α1d receptors, rat brain cortex 5HT1a receptor in cells with IC50s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC50, 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC50, 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC50, >100,000 nM)[1]. RS102895 ameliorates the increased extracellular matrix (ECM) protein expression by inhibition of CCR2 at 10 μM, and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 300815-41-2
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性状 Solid
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分子量 390.40
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分子式 C21H21F3N2O2
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Color White to off-white
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SMILES
O=C1NC2=CC=CC=C2C3(CCN(CCC4=CC=C(C(F)(F)F)C=C4)CC3)O1
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別名
RS102895; MLJS-21001
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (28)
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Journal Impact Factor
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Most Recent
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Nat Immunol
2024 Oct;25(10):1959-1975. PMID: 39223350 -
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J Adv Res
Interplay between lipid dysregulation and ferroptosis in chondrocytes and the targeted therapy effect of metformin on osteoarthritis. [Abstract]2025 Mar:69:515-529. PMID: 38621621 -
J Adv Res
2020 Jul 22:28:231-243. PMID: 33364059 -
Theranostics
2020 Apr 27;10(13):5687-5703. PMID: 32483412 -
Adv Sci (Weinh)
RBM10 Deficiency Promotes Anti-PD-1 Resistance in LUAD via STING Alternative Splicing-Driven CCL7 Signaling and Macrophage Polarization. [Abstract]2026 Jun 22:e22159. PMID: 42325102 -
Adv Sci (Weinh)
PLAUR+ Neutrophils Drive Anti-PD-1 Therapy Resistance in Patients with Hepatocellular Carcinoma by Shaping an Immunosuppressive Microenvironment. [Abstract]2025 Jul 17:e07167. PMID: 40673864
Abaucin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 17:e07167. [Abstract]
Abaucin (RS102895) (100 µg per mouse; i.p.; once daily). Representative images of the orthotopic tumors at the study endpoint (5 mice per group). Scale bar: 1 cm. The tumor volume and tumor weight of each group at the study endpoint (n=5 per group).
Abaucin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 17:e07167. [Abstract]
Abaucin (RS102895) (100 µg per mouse; i.p.; once daily). Flow cytometry analysis of CD11b⁺ F4/80⁺ macrophages in each group (n=5 per group).
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Sci Adv
2026 Jun 26;12(26):eaee8580. PMID: 42341114 -
Sci Adv
2023 Aug 2;9(31):eadg6856. PMID: 37531422 -
Cell Death Dis
Targeting CCL2-CCR4 axis suppress cell migration of head and neck squamous cell carcinoma. [Abstract]2022 Feb 17;13(2):158. PMID: 35177591 -
J Neuroinflammation
Ly6C-high monocytes alleviate brain injury in experimental subarachnoid hemorrhage in mice. [Abstract]2023 Nov 17;20(1):270. PMID: 37978532 -
Acta Pharmacol Sin
ATM promotes bone metastatic propensity of breast cancer by inducing osteoclastogenesis via the NFκB-CCL2 pathway. [Abstract]2025 Dec 1. PMID: 41326811 -
J Eur Acad Dermatol Venereol
Recombinant Treponema pallidum protein Tp0136 promotes fibroblast migration by modulating MCP-1/CCR2 through TLR4. [Abstract]2020 Apr;34(4):862-872. PMID: 31856347
Abaucin purchased from MedChemExpress. Usage Cited in: J Eur Acad Dermatol Venereol. 2020 Apr;34(4):862-872. [Abstract]
Inhibition of Tp0136-induced fibroblast migration by both anti-MCP-1 neutralizing antibody (40 μg/mL) and RS102895 (Abaucin) (20 μM; 13 h) (100×).
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Stem Cell Res Ther
Mesenchymal stem cells alleviate idiopathic pneumonia syndrome by facilitating M2 polarization via CCL2/CCR2 axis and further inducing formation of regulatory CCR2 + CD4 + T cells. [Abstract]2025 Mar 1;16(1):108. PMID: 40025564
Abaucin purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Mar 1;16(1):108. [Abstract]
CCL2 and CCR2 antagonists (Abaucin) (2 mg/kg; i.p.; every other day for a total of four injections) reversed the prophylactic effect of MSCs on GVHD.
Abaucin purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Mar 1;16(1):108. [Abstract]
Representative images of HE-stained histological sections of lung tissues showing that the addition of a CCL2 or CCR2 antagonist (Abaucin) (2 mg/kg; i.p.; every other day for a total of four injections) reversed the prophylactic effect of MSCs on lung injury (n = 5). Scale bar = 200 μm.
Abaucin purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Mar 1;16(1):108. [Abstract]
Representative images of immunofluorescence staining for the macrophage marker F4/80 (green) and the M2 marker CD206 (red) in lung tissue. CD206 + macrophages were diminished after treatment with both the CCL2 and CCR2 antagonist (Abaucin) (2 mg/kg; i.p.; every other day for a total of four injections). Scale bar = 200 μm.
Abaucin purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Mar 1;16(1):108. [Abstract]
Immunohistochemical staining with a mouse CD3 monoclonal antibody revealed that T-cell infiltration was more pronounced in lung tissue after treatment with a CCL2 or CCR2 antagonist (Abaucin) (2 mg/kg; i.p.; every other day for a total of four injections). Scale bar = 200 μm.
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Stem Cell Res Ther
Mesenchymal stem cells alleviate idiopathic pneumonia syndrome by modulating T cell function through CCR2-CCL2 axis. [Abstract]2021 Jul 2;12(1):378. PMID: 34215321 -
Hum Reprod
Estrogen receptor β upregulates CCL2 via NF-κB signaling in endometriotic stromal cells and recruits macrophages to promote the pathogenesis of endometriosis. [Abstract]2019 Apr 1;34(4):646-658. PMID: 30838396 -
Life Sci
Enhancement of lens extraction-induced MCP-1 upregulation and microglia response in long-term diabetes via c-jun, stat1 and ERK. [Abstract]2020 Nov 15:261:118360. PMID: 32861799 -
Liver Int
Regulation of the macrophage-hepatic stellate cell interaction by targeting macrophage peroxisome proliferator-activated receptor gamma to prevent non-alcoholic steatohepatitis progression in mice. [Abstract]2022 Dec;42(12):2696-2712. PMID: 36165186 -
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Eur J Pharmacol
IL-6 deficiency promotes colitis by recruiting Ly6Chi monocytes into inflamed colon tissues in a CCL2-CCR2-dependent manner. [Abstract]2021 Aug 5:904:174165. PMID: 33979652 -
Int Immunopharmacol
Salidroside postconditioning attenuates ferroptosis-mediated lung ischemia-reperfusion injury by activating the Nrf2/SLC7A11 signaling axis. [Abstract]2023 Feb:115:109731. PMID: 36907990 -
Mol Med Rep
2017 Sep;16(3):3387-3394. PMID: 28714025
Abaucin purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3387-3394. [Abstract]
Western blot analysis of the protein expression of ERK1/2, p ERK1/2, p38 and p p38 is performed using SDS PAGE.
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Sci Rep
Interleukin-7 enhances recruitment of MDSCs by regulating MCP-1 via JAK1/STAT3 signaling pathway in non-small cell lung cancer. [Abstract]2025 May 15;15(1):16869. PMID: 40374882 -
Exp Cell Res
Tp0136 targets fibronectin (RGD)/Integrin β1 interactions promoting human microvascular endothelial cell migration. [Abstract]2020 Nov 1;396(1):112289. PMID: 32950474 -
Brain Sci
CCR2 Regulates Referred Somatic Hyperalgesia by Mediating T-Type Ca2+ Channel Currents of Small-Diameter DRG Neurons in Gastric Ulcer Mice. [Abstract]2025 Feb 27;15(3):255. PMID: 40149778 -
J Interferon Cytokine Res
Monocyte Chemotactic Protein-1 Regulates Proliferation and Contractility of Human Bladder Smooth Muscle Cells Under Hydrostatic Pressure. [Abstract]2020 May;40(5):245-253. PMID: 32091964 -
J Interferon Cytokine Res
MCP-1/CCL2 Mediated by Autocrine Loop of PDGF-BB Promotes Invasion of Lung Cancer Cell by Recruitment of Macrophages Via CCL2-CCR2 Axis. [Abstract]2019 Apr;39(4):224-232. PMID: 30730243 -
溶剤 & 溶解度
DMSO : 175 mg/mL (448.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 50 mg/mL (128.07 mM; ultrasonic and warming and heat to 60°C)
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 (protect from light). 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 (protect from light). 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 (6.40 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
プロトコル
Transfected mesangial cells (MCs) are serum restricted for 24 h, after which the medium is replaced by serum-free DMEM containing normal glucose (NG; 5.6 mM), NG+Mannitol (NG+M; 24.4 mM), or high glucose (HG; 30 mM). In addition, nontransfected MCs are cultured under NG, NG+M, or HG with or without RS102895 or anti-TGF-1 antibody (25 μg/mL). Nontransfected MCs are also exposed to medium containing recombinant human MCP-1 (10 ng/mL) or recombinant human TGF-1 (2 ng/mL). At 24 h after the media change, cells are harvested and the conditioned culture media are collected[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[3]
CCR2 antagonist RS102895 is dissolved in DMSO. Rats receive daily intrathecal injection of either RS102895 (3 g/L) 10 μL or 10 % DMSO 10 μL between 9 and 20 days after operation. All rats are randomLy divided into five groups (n = 10 per group): Sham group, Sham + RS102895 group, BCP group, BCP + RS102895 group, and BCP + DMSO group. Rats are sacrificed 20 days after operation and the tissue samples from the L4-L5 spinal cord segments are rapidly removed and immediately frozen in liquid nitrogen and stored at −80°C until use for RT-PCR and Western blot[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. [Content Brief]
[2]. Park J, et al. MCP-1/CCR2 system is involved in high glucose-induced fibronectin and type IV collagen expression in cultured mesangial cells. Am J Physiol Renal Physiol. 2008 Sep;295(3):F749-57. [Content Brief]
[3]. Ren F, et al. Analgesic Effect of Intrathecal Administration of Chemokine Receptor CCR2 Antagonist is Related to Change in Spinal NR2B, nNOS, and SIGIRR Expression in Rat with Bone Cancer Pain. Cell Biochem Biophys. 2015 Jun;72(2):611-6. [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 (protect from light). 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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.5615 mL | 12.8074 mL | 25.6148 mL | 64.0369 mL |
| 5 mM | 0.5123 mL | 2.5615 mL | 5.1230 mL | 12.8074 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5615 mL | 6.4037 mL | |
| 15 mM | 0.1708 mL | 0.8538 mL | 1.7077 mL | 4.2691 mL | |
| 20 mM | 0.1281 mL | 0.6404 mL | 1.2807 mL | 3.2018 mL | |
| 25 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5615 mL | |
| 30 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1346 mL | |
| 40 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
| 50 mM | 0.0512 mL | 0.2561 mL | 0.5123 mL | 1.2807 mL | |
| 60 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 1.0673 mL | |
| 80 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL | |
| 100 mM | 0.0256 mL | 0.1281 mL | 0.2561 mL | 0.6404 mL |
Abaucin 関連分類
HY-18611A 関連分類
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