SCH 546738
Based on 19 publication(s) in Google Scholar
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.67%
- CAS. Nr.: 906805-42-3
- Formel: C23H31Cl2N7O
- Molecular Weight:492.44
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) SCH 546738
More- J Hepatol. 2016 Jan;64(1):160-70. [Abstract]
- Immunity. 2025 Sep 9;58(9):2320-2335.e9. [Abstract]
- Nat Commun. 2017 Nov 17;8(1):1571. [Abstract]
- Theranostics. 2017 Sep 26;7(17):4192-4203. [Abstract]
- Adv Sci (Weinh). 2025 Jun 20:e01238. [Abstract]
- Sci Adv. 2023 Apr 28;9(17):eadg0654. [Abstract]
- Cell Death Dis. 2025 May 30;16(1):424. [Abstract]
- J Allergy Clin Immunol. 2016 Jul;138(1):114-122.e4. [Abstract]
- Nat Struct Mol Biol. 2024 Apr;31(4):610-620. [Abstract]
- Cancer Immunol Res. 2015 Aug;3(8):864-70. [Abstract]
- Cell Rep. 2025 Apr 24;44(5):115631. [Abstract]
- Int J Mol Sci. 2026 Jan 4;27(1):523. [Abstract]
- Sci Rep. 2025 Jul 1;15(1):21129. [Abstract]
- Sci Rep. 2024 Apr 8;14(1):8196. [Abstract]
- Sci Rep. 2021 Jan 28;11(1):2613. [Abstract]
- Front Biosci (Landmark Ed). 2025 Oct 31;30(10):45931. [Abstract]
- J Orthop Res. 2020 Feb;38(2):336-347. [Abstract]
- Research Square Preprint. 2024 Feb 13.
- University of Calgary. Dec.23. 2015.
Customer Validation & Images
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Cell Proliferation/Viability Assay
Biologische Aktivität
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Human CXCR3 0.4 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.8 nM
Compound: 8a
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Displacement of [125I]CXCL10 from human CXCR3 expressed in mouse BA/F3 cells
Displacement of [125I]CXCL10 from human CXCR3 expressed in mouse BA/F3 cells
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[PMID: 22018463] |
The affinity of SCH 546738 binding to human CXCR3 receptor is determined by competition binding analysis using 35S radiolabeled SCH 535390 (a sulfonamide analog of the CXCR3 compound series with a Kd of 0.6 nM) as a competitive tracer. In addition, SCH 546738 displaces radiolabeled CXCL10 and CXCL11 from human CXCR3 with IC50 ranging from 0.8 to 2.2 nM in a non-competitive manner. SCH 546738 potently and specifically inhibits CXCR3-mediated chemotaxis in human activated T cells with IC90 about 10 nM[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.
Chemical Information
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CAS. Nr. 906805-42-3
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Appearance Solid
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Molecular Weight 492.44
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Formel C23H31Cl2N7O
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Color White to yellow
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SMILES
O=C(N)C1=NC(Cl)=C(N2CCN(C3CCN(CC4=CC=C(Cl)C=C4)CC3)[C@@H](CC)C2)N=C1N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (19)
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Journal Impact Factor
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Most Recent
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J Hepatol
CXC chemokine receptor 3 promotes steatohepatitis in mice through mediating inflammatory cytokines, macrophages and autophagy. [Abstract]2016 Jan;64(1):160-70. PMID: 26394162
SCH 546738 purchased from MedChemExpress. Usage Cited in: J Hepatol. 2016 Jan;64(1):160-70. [Abstract]
CXCR3 antagonists suppress MCD-induced steatohepatitis in vivo. CXCR3 protein levels are decreased after 10 days treatment of CXCR3 antagonists.
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Immunity
Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452 -
Nat Commun
2017 Nov 17;8(1):1571. PMID: 29146996
SCH 546738 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Nov 17;8(1):1571. [Abstract]
Activation of MAPK/ERK pathways after CXCR3 stimulation when cells are pretreated or not with CXCR3 antagonist SCH546738. Total ERK is used as loading control.
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Theranostics
Pro-Inflammatory CXCR3 Impairs Mitochondrial Function in Experimental Non-Alcoholic Steatohepatitis. [Abstract]2017 Sep 26;7(17):4192-4203. PMID: 29158819
SCH 546738 purchased from MedChemExpress. Usage Cited in: Theranostics. 2017 Sep 26;7(17):4192-4203. [Abstract]
Apoptosis related markers, ASK1, p-JNK, cleaved caspase 3 and cleaved PARP are measured by western blot in MCD-fed WT mice treated with vehicle or CXCR3 antagonists SCH546738 and AMG487.
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Adv Sci (Weinh)
NDRG1-Driven Lactate Accumulation Promotes Lung Adenocarcinoma Progression Through the Induction of an Immunosuppressive Microenvironment. [Abstract]2025 Jun 20:e01238. PMID: 40539245 -
Sci Adv
Targeting IRG1 reverses the immunosuppressive function of tumor-associated macrophages and enhances cancer immunotherapy. [Abstract]2023 Apr 28;9(17):eadg0654. PMID: 37115931 -
Cell Death Dis
2025 May 30;16(1):424. PMID: 40447617 -
J Allergy Clin Immunol
Chemokine release from human rhinovirus-infected airway epithelial cells promotes fibroblast migration. [Abstract]2016 Jul;138(1):114-122.e4. PMID: 26883463
SCH 546738 purchased from MedChemExpress. Usage Cited in: J Allergy Clin Immunol. 2016 Jul;138(1):114-122.e4. [Abstract]
A selective CXCR3 receptor antagonist abrogates fibroblast migration to HRV MED (n=6).
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Nat Struct Mol Biol
2024 Apr;31(4):610-620. PMID: 38177682 -
Cancer Immunol Res
STAT3 in CD8+ T Cells Inhibits Their Tumor Accumulation by Downregulating CXCR3/CXCL10 Axis. [Abstract]2015 Aug;3(8):864-70. PMID: 26025380 -
Cell Rep
Myeloid-lineage-specific membrane protein LRRC25 suppresses immunity in solid tumor and is a potential cancer immunotherapy checkpoint target. [Abstract]2025 Apr 24;44(5):115631. PMID: 40279244 -
Int J Mol Sci
CXCL9 and CXCL10 Induce Expression of Nociceptive Ion Channels in Primary Sensory Neurons in Models of HIV-Associated Distal Sensory Polyneuropathy. [Abstract]2026 Jan 4;27(1):523. PMID: 41516395 -
Sci Rep
CXCL10-dependent epithelial-vascular cross-talk for endothelial activation following SARS-CoV-2 infection. [Abstract]2025 Jul 1;15(1):21129. PMID: 40593263 -
Sci Rep
RSAD2 is abundant in atherosclerotic plaques and promotes interferon-induced CXCR3-chemokines in human smooth muscle cells. [Abstract]2024 Apr 8;14(1):8196. PMID: 38589444 -
Sci Rep
Inhibition of the CXCL9-CXCR3 axis suppresses the progression of experimental apical periodontitis by blocking macrophage migration and activation. [Abstract]2021 Jan 28;11(1):2613. PMID: 33510341 -
Front Biosci (Landmark Ed)
A Comparative Study of the Effects of Nine CXCR3 Antagonists on Macrophage Function and the Treatment of Acute Lung Injury. [Abstract]2025 Oct 31;30(10):45931. PMID: 41198562 -
J Orthop Res
2020 Feb;38(2):336-347. PMID: 31424111 -
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Lösungsmittel & Löslichkeit
1 M HCl : 5 mg/mL (10.15 mM; ultrasonic and warming and heat to 60°C)
DMSO : 2.5 mg/mL (5.08 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 1.25 mg/mL (2.54 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.54 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: Corn Oil
Solubility: 1 mg/mL (2.03 mM); Suspended solution; Need ultrasonic and warming
Add each solvent one by one: 0.5% Methylcellulose/saline water
Solubility: 5 mg/mL (10.15 mM); Suspended solution; Need ultrasonic
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.
Protokoll
The preparation of human activated T cells is performed. Human peripheral blood lymphocytes are prepared, depleted of monocytes, and stimulated for 2 days with 1 µg/mL PHA and 100 U/mL IL-2 in RPMI 1640 supplemented with 10% fetal bovine serum (FBS), 2 mM L-Glutamine, 1% non-essential amino acids and 2 mM HEPES. Following stimulation, peripheral blood lymphocytes are cultured in above media containing 5% conditioned media for up to 15 days. uman activated T cell chemotaxis assays ae performed using 96-well ChemoTx microplates with a 3 µm filter. Activated T cells are washed with RPMI medium twice, and then resuspended in the medium containing 20% FBS. 1.25×105 cells/reaction are mixed with indicated concentrations of SCH 546738 (1, 10 or 100 nM) and placed on the filter. SCH 546738 and chemokines are mixed and placed in the bottom well of the ChemoTx system. After 2.5 hours incubation at 37°C/5% CO2, the cells are scraped off and the plate system is centrifuged for 5 minutes at 1000 RPM. The filter screen is then removed and the ChemoTx plate is inverted into a 96 well plate with a funnel plate. The plate system is centrifuged for 5 minutes at 1000 RPM. The volume in the wells is brought to 100 μL with assay buffer and the plates are rested for approximately 15 minutes at room temperature. The number of migrated cells is measured using the Cell Titer Glo Luminescent Assay. Chemotaxis is expressed as a chemotactic index, which is a ratio versus the one without chemokines[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female C57BL/6 mice are used. For immunization, 150 μg MOG35-55 peptide prepared by Princeton Biomolecules and 300 μg killed Mycobacterium tuberculosis are mixed in CFA and injected s.c. in two 50-μL injections over the flanks on day 1. Also, 200 ng of pertussis toxin is injected i.v. on days 0 and 2. SCH 546738 is administered orally 30 mpk in C57BL/6 mice twice daily. Dosing with SCH 546738 started at day 0, 24 h prior to MOG35-55 immunization (day 1). Mice are monitored daily and assessed for clinical signs of disease in a blinded fashion according to the following criteria: 0, no signs of disease; 1, tail paralysis; 2, limp tail and hind limb weakness; 3, hind limb paralysis; 4, hind limb plus forelimb paralysis; and 5, moribund or dead. Cumulative clinical scores are calculated by adding daily scores from the day of immunization until the end of the experiment. Mean clinical scores at separate days and mean maximal scores are calculated by adding the scores of individual mice and dividing with the number of mice in each group, including mice not developing signs of EAE.
Rats[1]
Male Lewis rats challenged by injection of 50 µL (30 mg) of a guinea pig spinal cord homogenate in complete Freund's adjuvant (CFA) into one footpad. SCH 546738 or 0.4% methylcellulose (vehicle) is orally administered at the indicated dose (0.2 mL) twice a day, starting on the day before transplantation until the day of graft rejection. SCH 546738 is administered orally at 10 mg/kg (mpk) in Lewis rats. To test whether SCH 546738 enhances the effect of conventional immunosuppressive reagent, the recipients are received treatment with subtherapeutic dose of CsA for one week combined with treatment with SCH 546738. Graft survival is analyzed using the log-rank test. The parametric data are analyzed by Student t test (2-tailed) using GraphPad InStat version.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Jenh CH, et al. A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection. BMC Immunol. 2012 Jan 10;13:2. [Content Brief]
[2]. Zhang X, et al. CXC chemokine receptor 3 promotes steatohepatitis in mice through mediating inflammatory cytokines, macrophages and autophagy. J Hepatol. 2016 Jan;64(1):160-70. [Content Brief]
[3]. Yue C, et al. STAT3 in CD8+ T Cells Inhibits Their Tumor Accumulation by Downregulating CXCR3/CXCL10 Axis. Cancer Immunol Res. 2015 Aug;3(8):864-870. [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 M HCl | 1 mM | 2.0307 mL | 10.1535 mL | 20.3070 mL | 50.7676 mL |
| 5 mM | 0.4061 mL | 2.0307 mL | 4.0614 mL | 10.1535 mL | |
| 1 M HCl | 10 mM | 0.2031 mL | 1.0154 mL | 2.0307 mL | 5.0768 mL |
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