J-113863
Based on 4 publication(s) in Google Scholar
J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 95.19%
- CAS No.: 353791-85-2
- 화학식: C30H37Cl2IN2O2
- 분자량:655.44
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) J-113863
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Biological Activity
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CCR1 0.9 nM (IC50, Human CCR1) |
CCR1 5.8 nM (IC50, Mouse CCR1) |
CCR3 0.58 nM (IC50, Human CCR3) |
CCR3 460 nM (IC50, Mouse CCR3) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.58 nM
Compound: 3
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Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR3 receptor expressed in CHO cells
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[PMID: 11354381] |
| CHO | IC50 |
0.9 nM
Compound: 3
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Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells
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[PMID: 11354381] |
| HEL | IC50 |
>10000 nM
Compound: 2q-1
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Inhibitory activity of Fractalkine-induced increase in [Ca2+] Conc. in HEL cells at human CX3CR1 receptor
Inhibitory activity of Fractalkine-induced increase in [Ca2+] Conc. in HEL cells at human CX3CR1 receptor
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[PMID: 11311066] |
| U-937 | IC50 |
0.73 nM
Compound: 2q-1
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Inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptor
Inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing human CCR1 receptor
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[PMID: 11311066] |
| U-937 | IC50 |
21 nM
Compound: 2q-1
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inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptor
inhibitory activity against MIP-1 alpha- induced [Ca2+] response in U937 cells expressing mouse CCR1 receptor
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[PMID: 11311066] |
Modified Vaccinia virus Ankara (MVA) but not MVA and vaccinia virus (VACV) infected MH-S cells increase the expression of the CXCR2 acting chemokine CXCL2. MH-S cells constitutively produce CCL2 and CCR1 acting chemokines CCL3, CCL5 and CCL9. Consequently, supernatants of mock treated and virus infected MH-S cells induce chemotaxis of murine promyelocyte MPRO cells and human monocytic THP-1 cells at the same level. However, supernatants of MVA infected MH-S cells significantly increase chemotaxis of the CCR2 deficient human monocytic cell line U-937. Chemotaxis of all above cell types is inhibited by J-113863[1].
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.
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Animal Model:DBA-1 male mice (10-12 weeks) induced with Collagen[2]
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Dosage:3 mg/kg, 10 mg/kg
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Administration:Intraperitoneal injection; once daily; for 11 days
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Result:Improved paw inflammation and joint damage, and dramatically decreased cell infiltration into joints.
Chemical Information
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CAS No. 353791-85-2
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Appearance Solid
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분자량 655.44
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화학식 C30H37Cl2IN2O2
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Color Light yellow to yellow
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SMILES
CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(C3C4=C(OC5=C3C=C(Cl)C=C5)C=CC(Cl)=C4)=O)CC1.[I-]
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Bioact Mater
Phosphorylation inhibition of protein-tyrosine phosphatase 1B tyrosine-152 induces bone regeneration coupled with angiogenesis for bone tissue engineering. [Abstract]2021 Jan 7;6(7):2039-2057. PMID: 33511306 -
Cancer Immunol Res
Targeting CCR1 remodels the tumor microenvironment and relieves immune suppression in pancreatic cancer. [Abstract]2026 May 28. PMID: 42207977 -
Inflamm Regen
JAK inhibition ameliorates bone destruction by simultaneously targeting mature osteoclasts and their precursors. [Abstract]2023 Mar 3;43(1):18. PMID: 36869390 -
J Ethnopharmacol
The analgesic properties of Yu-Xue-Bi tablets in the inflammatory pain mice: By the inhibition of CCL3-mediated macrophage transmigration into the spinal cord. [Abstract]2022 May 10;289:115051. PMID: 35101573
용액&용해도
DMSO : 50 mg/mL (76.28 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (3.81 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.81 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (281 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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Handling Instructions (2659 KB)
References
[1]. Lehmann MH, et al. Modified Vaccinia virus Ankara but not vaccinia virus induces chemokine expression in cells of the monocyte/macrophage lineage. Virol J. 2015 Feb 12;12:21. [Content Brief]
[2]. Amat M, et al. Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo. Br J Pharmacol. 2006 Nov;149(6):666-75. [Content Brief]
[3]. Naya A, et al. Design, synthesis, and discovery of a novel CCR1 antagonist. J Med Chem. 2001 Apr 26;44(9):1429-35. [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 (sealed storage, away from moisture). 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 | 1.5257 mL | 7.6285 mL | 15.2569 mL | 38.1423 mL |
| 5 mM | 0.3051 mL | 1.5257 mL | 3.0514 mL | 7.6285 mL | |
| 10 mM | 0.1526 mL | 0.7628 mL | 1.5257 mL | 3.8142 mL | |
| 15 mM | 0.1017 mL | 0.5086 mL | 1.0171 mL | 2.5428 mL | |
| 20 mM | 0.0763 mL | 0.3814 mL | 0.7628 mL | 1.9071 mL | |
| 25 mM | 0.0610 mL | 0.3051 mL | 0.6103 mL | 1.5257 mL | |
| 30 mM | 0.0509 mL | 0.2543 mL | 0.5086 mL | 1.2714 mL | |
| 40 mM | 0.0381 mL | 0.1907 mL | 0.3814 mL | 0.9536 mL | |
| 50 mM | 0.0305 mL | 0.1526 mL | 0.3051 mL | 0.7628 mL | |
| 60 mM | 0.0254 mL | 0.1271 mL | 0.2543 mL | 0.6357 mL |
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