BX471
Based on 28 publication(s) in Google Scholar
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.98%
- No. CAS: 217645-70-0
- Fòrmula: C21H24ClFN4O3
- Peso molecular:434.89
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) BX471
More- Signal Transduct Target Ther. 2021 Feb 28;6(1):91. [Abstract]
- Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
- Cell Res. 2018 Mar;28(3):323-335. [Abstract]
- Immunity. 2026 Mar 10;59(3):598-617.e11. [Abstract]
- Cancer Discov. 2026 May 19. [Abstract]
- Neuron. 2025 Nov 18:S0896-6273(25)00803-7. [Abstract]
- J Biomed Sci. 2026 Jan 9;33(1):10. [Abstract]
- J Exp Clin Cancer Res. 2022 Mar 3;41(1):81. [Abstract]
- Sci Adv. 2021 May 26;7(22):eabb5943. [Abstract]
- Cell Death Dis. 2025 Dec 22;16(1):918. [Abstract]
- Cancer Lett. 2025 Dec 1:634:218064. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Aug 26;122(34):e2503779122. [Abstract]
- Mol Med. 2024 Dec 20;30(1):253. [Abstract]
- Mol Med. 2024 Jun 3;30(1):74. [Abstract]
- J Invest Dermatol. 2025 Nov 28:S0022-202X(25)03613-9. [Abstract]
- J Agric Food Chem. 2024 Apr 15. [Abstract]
- Commun Biol. 2026 May 15;9(1):661. [Abstract]
- Commun Biol. 2026 May 9. [Abstract]
- Int Immunopharmacol. 2026 May 1:176:116478. [Abstract]
- Int Immunopharmacol. 2025 Feb 6:147:114027. [Abstract]
- Int J Mol Sci. 2024 Apr 14;25(8):4337. [Abstract]
- Sci Rep. 2020 Nov 25;10(1):20508. [Abstract]
- Neuropharmacology. 2025 Feb 15:264:110239. [Abstract]
- J Inflamm Res. 2020 Jul 21:13:343-356. [Abstract]
- Lab Invest. 2020 Apr;100(4):619-629. [Abstract]
- Immunol Lett. 2018 Dec:204:29-37. [Abstract]
- bioRxiv. 2024 November 03.
- Research Square Preprint. 2021 Oct.
Customer Validation & Images
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In Vivo Efficacy Study
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WB
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Cell Migration/Invasion Assay
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
Actividad biológica
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MIP-1α-CCR1 1 nM (Ki) |
RANTES-CCR1 2.8 nM (Ki) |
MCP-3-CCR1 5.5 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
5.5 nM
Compound: 2, BX-471
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Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
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[PMID: 19183043] |
| THP-1 | IC50 |
1.5 nM
Compound: 2, BX-471
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Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
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[PMID: 19183043] |
| THP-1 | IC50 |
18 nM
Compound: BX-741
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Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
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[PMID: 17446072] |
| THP-1 | IC50 |
18 nM
Compound: BX-741
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Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
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[PMID: 17446072] |
BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca2+ mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX471 demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors[1].
BX471 is also able to displace 125I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner with a Ki of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC50 of 5.8±1 nM and 198±7 nM, respectively[2].
BX471 (0.1-10 μM) shows a dose-dependent inhibition of RANTES-mediated and shear-resistant adhesion on IL-1β-activated microvascular endothelium in shear flow in isolated blood monocytes. BX471 also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μM by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug plasma levels drops to 0.1 μM or lower. Mice treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45 positive leukocytes of approximately 55%. BX471 has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1-positive cells by 65% in UUO kidneys as compared with vehicle control[2]. Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 217645-70-0
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Appearance Solid
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Peso molecular 434.89
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Fòrmula C21H24ClFN4O3
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Color White to off-white
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SMILES
O=C(N)NC1=CC(Cl)=CC=C1OCC(N2[C@H](C)CN(CC3=CC=C(F)C=C3)CC2)=O
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Synonyms
ZK-811752
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (28)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Eosinophil-derived chemokine (hCCL15/23, mCCL6) interacts with CCR1 to promote eosinophilic airway inflammation. [Abstract]2021 Feb 28;6(1):91. PMID: 33640900 -
Cancer Cell
Cathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation. [Abstract]2021 Mar 8;39(3):423-437.e7. PMID: 33450198 -
Cell Res
2018 Mar;28(3):323-335. PMID: 29327730
BX471 purchased from MedChemExpress. Usage Cited in: Cell Res. 2018 Mar;28(3):323-335. [Abstract]
Percentage of large, intermediate and small colonies in the single-colony forming assay of sorted LT-HSCs co-cultured with Eos and intervened with the CCL-6 antibody and BX471 (200 μM).
BX471 purchased from MedChemExpress. Usage Cited in: Cell Res. 2018 Mar;28(3):323-335. [Abstract]
ROS MFI analysis in HSCs co-cultured for 2 h with Eos following treatment with BX471 (200 μM).
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Immunity
2026 Mar 10;59(3):598-617.e11. PMID: 41722568 -
Cancer Discov
Senescent-like neutrophils shape angiogenic immunosuppressive niches in colorectal cancer liver metastasis. [Abstract]2026 May 19. PMID: 42154581 -
Neuron
2025 Nov 18:S0896-6273(25)00803-7. PMID: 41260217 -
J Biomed Sci
2026 Jan 9;33(1):10. PMID: 41508046 -
J Exp Clin Cancer Res
Tumor bud-derived CCL5 recruits fibroblasts and promotes colorectal cancer progression via CCR5-SLC25A24 signaling. [Abstract]2022 Mar 3;41(1):81. PMID: 35241150 -
Sci Adv
2021 May 26;7(22):eabb5943. PMID: 34039594
BX471 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2021 May 26;7(22):eabb5943. [Abstract]
Representative crystal violet staining and quantification of migrated B16-F10 cells in the Oris cell migration assay. B16-F10 cells were cultured in control medium or eosinophil culture supernatant after migration for 36 hours treated with or without 20 μM BX471.
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Cell Death Dis
2025 Dec 22;16(1):918. PMID: 41430036
BX471 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Dec 22;16(1):918. [Abstract]
BX471 (50 mg/kg, i.p.) treatment significantly reduced tumor volume in WT mice, whereas recombinant CCL7 supplementation markedly increased tumors in Zbp1−/− mice.
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Cancer Lett
Tumor-derived CCL5 recruits CCR1+ macrophages to suppress apoptosis and drive proliferation in duodenal adenocarcinoma. [Abstract]2025 Dec 1:634:218064. PMID: 41015267 -
Proc Natl Acad Sci U S A
Unraveling the neuroimmune mechanisms in cancer-induced bone pain: New horizons for therapeutic intervention of the two-phase paradigm. [Abstract]2025 Aug 26;122(34):e2503779122. PMID: 40828016 -
Mol Med
CXCL4 deficiency limits M4 macrophage infiltration and attenuates hyperoxia-induced lung injury. [Abstract]2024 Dec 20;30(1):253. PMID: 39707183 -
Mol Med
Inhibition of CC chemokine receptor 1 ameliorates osteoarthritis in mouse by activating PPAR-γ. [Abstract]2024 Jun 3;30(1):74. PMID: 38831316
BX471 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Jun 3;30(1):74. [Abstract]
Western blot was employed to determine the expression of P16INK4a and P21CIP1 treated with BX471 (5, 10 μM).
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J Invest Dermatol
Multiomics reveals CCL3-driving neuronal sensitization in chronic pruritus of unknown origin. [Abstract]2025 Nov 28:S0022-202X(25)03613-9. PMID: 41320115 -
J Agric Food Chem
Palmatine Attenuated Lipopolysaccharide-Induced Acute Lung Injury by Inhibiting M1 Phenotype Macrophage Polarization via NAMPT/TLR2/CCR1 Signaling. [Abstract]2024 Apr 15. PMID: 38619332 -
Commun Biol
2026 May 15;9(1):661. PMID: 42141167 -
Commun Biol
Targeting CCR1-mediated macrophage phenotypic switching to alleviate bladder pain and urinary dysfunction in interstitial cystitis. [Abstract]2026 May 9. PMID: 42103951 -
Int Immunopharmacol
2026 May 1:176:116478. PMID: 41825208 -
Int Immunopharmacol
Blocking the CCL5/CCL7-CCR1 axis regulates macrophage polarization through NF-κB pathway to alleviate the progression of osteoarthritis. [Abstract]2025 Feb 6:147:114027. PMID: 39805173 -
Int J Mol Sci
Novel Findings on CCR1 Receptor in CNS Disorders: A Pathogenic Marker Useful in Controlling Neuroimmune and Neuroinflammatory Mechanisms in Parkinson's Disease. [Abstract]2024 Apr 14;25(8):4337. PMID: 38673922 -
Sci Rep
Multiple myeloma hinders erythropoiesis and causes anaemia owing to high levels of CCL3 in the bone marrow microenvironment. [Abstract]2020 Nov 25;10(1):20508. PMID: 33239656 -
Neuropharmacology
CCR1 antagonist as a potential modulator of inflammatory, autophagic, and apoptotic markers in spinal cord injury. [Abstract]2025 Feb 15:264:110239. PMID: 39608704 -
J Inflamm Res
Therapeutic Effect of C-C Chemokine Receptor Type 1 (CCR1) Antagonist BX471 on Allergic Rhinitis. [Abstract]2020 Jul 21:13:343-356. PMID: 32801828 -
Lab Invest
CCL8 secreted by tumor-associated macrophages promotes invasion and stemness of glioblastoma cells via ERK1/2 signaling. [Abstract]2020 Apr;100(4):619-629. PMID: 31748682 -
Immunol Lett
2018 Dec:204:29-37. PMID: 30321562 -
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Solvente y solubilidad
DMSO : ≥ 100 mg/mL (229.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.75 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: ≥ 2.08 mg/mL (4.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 50% PEG300 50% Saline
Solubility: 5 mg/mL (11.50 mM); Clear 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.
Protocolo
Fasted male beagle dogs (n=3 per treatment group) are given BX471 either by oral gavage or by intravenous injection via the cephalic vein at a dose of 4 mg/kg. The compound is dissolved in a vehicle of 40% aqueous cyclodextrin. Serial blood samples are collected utilizing an in-dwelling catheter in the jugular vein at the indicated time points up to 6 h post-dosing. EDTA is used as an anticoagulant. The samples are centrifuged (1000× g for 10 min at 4°C), and plasma is stored frozen until analyzed for drug levels by HPLC-MS (electrospray mode operated under a positive ion mode). Plasma samples are thawed and denatured by the addition of four parts of ice-cold methanol containing a fixed amount of an internal standard to one part of plasma. The resulting protein precipitate is removed by centrifugation at 5000× g, and the supernatants are analyzed directly. Concurrently plasma calibration standards of BX471 are prepared over the range of quantification, processed, and analyzed under identical conditions. A FISONS, VG Platform single quadrupole instrument is used in these analyses with an electrospray inlet operated at 3.57 kV. Chromatographic separation is accomplished using a YMC AQ octadecyl silane reversed phase column (4.6×250 mm) following a short isocratic elution method (35% methanol, 65% water containing 0.1% trifluoroacetic acid). The total column flow (1 mL/min) is split post-column to infuse 50 μL/min into the mass spectrometer. The chromatograms are collected over a total run time of 7.5 min/sample following a 50-μL injection on the column. The ions are collected in a single ion positive ionization mode. A calibration curve for quantification is generated by plotting ion current ratios between the internal standard peak and the analyte in the plasma standards over the quantification range. Calculations of percent oral availability is deduced from the area under curve measurements. Pharmacokinetic parameters are calculated using WinNonLin version 3.0.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liang M, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8. [Content Brief]
[2]. Anders HJ, et al. A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J Clin Invest. 2002 Jan;109(2):251-9. [Content Brief]
[3]. Furuichi K, et al. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury. J Immunol. 2008 Dec 15;181(12):8670-6. [Content Brief]
[4]. Horuk R, et al. A non-peptide functional antagonist of the CCR1 chemokine receptor is effective in rat heart transplant rejection. J Biol Chem. 2001 Feb 9;276(6):4199-204. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2994 mL | 11.4972 mL | 22.9943 mL | 57.4858 mL |
| 5 mM | 0.4599 mL | 2.2994 mL | 4.5989 mL | 11.4972 mL | |
| 10 mM | 0.2299 mL | 1.1497 mL | 2.2994 mL | 5.7486 mL | |
| 15 mM | 0.1533 mL | 0.7665 mL | 1.5330 mL | 3.8324 mL | |
| 20 mM | 0.1150 mL | 0.5749 mL | 1.1497 mL | 2.8743 mL | |
| 25 mM | 0.0920 mL | 0.4599 mL | 0.9198 mL | 2.2994 mL | |
| 30 mM | 0.0766 mL | 0.3832 mL | 0.7665 mL | 1.9162 mL | |
| 40 mM | 0.0575 mL | 0.2874 mL | 0.5749 mL | 1.4371 mL | |
| 50 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
| 60 mM | 0.0383 mL | 0.1916 mL | 0.3832 mL | 0.9581 mL | |
| 80 mM | 0.0287 mL | 0.1437 mL | 0.2874 mL | 0.7186 mL | |
| 100 mM | 0.0230 mL | 0.1150 mL | 0.2299 mL | 0.5749 mL |
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