Cenicriviroc Mesylate
Based on 7 publication(s) in Google Scholar
Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 497223-28-6
- Formula: C42H56N4O7S2
- Molecular Weight:793.05
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Storage:
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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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Cenicriviroc Mesylate
More- Biomaterials. 2021 Jan;265:120392. [Abstract]
- Cells. 2020 Apr 14;9(4):964. [Abstract]
- Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504. [Abstract]
- Sci Rep. 2024 Jul 23;14(1):16897. [Abstract]
- Antiviral Res. 2020 Oct;182:104902. [Abstract]
- Eur J Immunol. 2024 Jul;54(7):e2350847. [Abstract]
- bioRxiv. 2026 Mar 19:2026.03.17.712383. [Abstract]
Customer Validation & Images
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ELISA
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Bio/Physico-chemical Assay
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WB
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IF
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In Vivo Imaging
Biological Activity
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CCR5 0.29 nM (IC50) |
CCR2 5.9 nM (IC50) |
R5 HIV-1 0.024-0.08 nM (IC50, in PBMCs) |
R5 HIV-2 0.03-0.98 nM (IC50, in PBMCs) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
>10000 nM
Compound: (S)-(-)-5b
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Displacement of [125I]RANTES from CCR1 expressed in CHO cells
Displacement of [125I]RANTES from CCR1 expressed in CHO cells
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[PMID: 16539392] |
| CHO | IC50 |
1100 nM
Compound: (S)-(-)-5b
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Displacement of [125I]TARC from CCR4 expressed in CHO cells
Displacement of [125I]TARC from CCR4 expressed in CHO cells
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[PMID: 16539392] |
| CHO | IC50 |
2400 nM
Compound: (S)-(-)-5b
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Displacement of [125I]eotaxin from CCR3 expressed in CHO cells
Displacement of [125I]eotaxin from CCR3 expressed in CHO cells
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[PMID: 16539392] |
| CHO | IC50 |
3.1 nM
Compound: (S)-(-)-5b
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Displacement of [125I]RANTES from CCR5 expressed in CHO cells
Displacement of [125I]RANTES from CCR5 expressed in CHO cells
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[PMID: 16539392] |
| CHO | IC50 |
5.9 nM
Compound: (S)-(-)-5b
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Displacement of [125I]MCP-1 from CCR2b expressed in CHO cells
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cells
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[PMID: 16539392] |
| CHO | IC50 |
>10000 nM
Compound: (S)-(-)-5b
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Displacement of [125I]MIP-3beta from CCR7 expressed in CHO cells
Displacement of [125I]MIP-3beta from CCR7 expressed in CHO cells
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[PMID: 16539392] |
| COS-7 | IC50 |
0.1 nM
Compound: (S)-(-)-5b
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Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
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[PMID: 16539392] |
| MOLT-4 | IC50 |
0.2 nM
Compound: (S)-(-)-5b
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Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
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[PMID: 16539392] |
Migration of mouse monocytes in response to carbon tetrachloride (CCL2) is reduced following pre-treatment with Cenicriviroc Mesylate (CVC) at a concentration of 1 μM. Compare to untreated and unstimulated cells, the average fold change in migrating cells (±SD) is 0.8±0.2 (p>0.05) and 0.7±0.4 (p>0.05) for CCL2-stimulated cells treated with Cenicriviroc Mesylate and unstimulated cells treated with Cenicriviroc Mesylate, respectively[1]. Phenotypic susceptibility testing shows, for the four R5-tropic HIV-2 isolates, a median EC50 for Cenicriviroc Mesylate of 0.39 nM (0.03, 0.33, 0.45 and 0.98 nM). The dual-tropic and the X4-tropic HIV-2 strains are resistant to Cenicriviroc Mesylate with EC50 at >1000 nM, and Maximum percentages of inhibition (MPI) at 33% and 4%, respectively[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.
Chemical Information
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CAS No. 497223-28-6
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Appearance Solid
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Molecular Weight 793.05
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Formula C42H56N4O7S2
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Color Light yellow to yellow
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SMILES
O=C(/C1=C/C2=CC(C3=CC=C(OCCOCCCC)C=C3)=CC=C2N(CC(C)C)CCC1)NC4=CC=C([S@](CC5=CN=CN5CCC)=O)C=C4.OS(=O)(C)=O
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Synonyms
TAK-652 Mesylate; TBR-652 Mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (7)
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Journal Impact Factor
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Most Recent
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Biomaterials
Nanoparticles retard immune cells recruitment in vivo by inhibiting chemokine expression. [Abstract]2021 Jan;265:120392. PMID: 32992116
Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Jan;265:120392. [Abstract]
The toxicity experiment of CCR5 inhibitor (Cenicriviroc) in zebrafish. Represent imaging of Tg (mpx:EGFP) larvae were treated with control buffer and 5 µM, 10 µM, 20 µM CCR5 inhibitor (Cenicriviroc) (24 h). Scale bar: 500 µm. The MPX+ cells number of whole body in Tg (mpx:EGFP) larvae.
Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 Jan;265:120392. [Abstract]
Represented imaging of macrophages recruitment to wounds in 72 hpf Tg (mpx:EGFP) larvae treated with control buffer and CCR5 inhibitor (Cenicriviroc) (5-20 µM; 24 h) with Imaris analysis. Scale bar: 200 μm.
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Cells
2020 Apr 14;9(4):964. PMID: 32295224
Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Cells. 2020 Apr 14;9(4):964. [Abstract]
These spheroids were repeatedly exposed to different anti-NASH drugs, from day 7 to 14, with renewed drug exposure every alternate day. Expression of COL1A1 protein was reduced for Cenicriviroc (3 μM; continuous supplementation in culture medium; medium was refreshed every other day during day 7–14), elafibranor, and lanifibranor.
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Am J Physiol Cell Physiol
Cenicriviroc prevents dysregulation of astrocyte/endothelial cross talk induced by ischemia and HIV-1 via inhibiting the NLRP3 inflammasome and pyroptosis. [Abstract]2024 Feb 1;326(2):C487-C504. PMID: 38145295
Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504. [Abstract]
Evaluation of CVC (Cenicriviroc) (24 h) antiviral activity against different HIV-1 strains in primary human astrocytes. Cells were infected with HIV-1 NL4-3, YU-2, and JR-CSF in the presence of CVC (1 μM) or vehicle (0.1% DMSO). Cell cultures were washed after 12 h of infection and resuspended in 1 mL of fresh medium containing CVC or vehicle to maintain constant drug/vehicle levels for the duration of the experiment. HIV-1 p24 levels in the supernatants were determined at the indicated time points. Note that CVC effectively protected against astrocyte infection by the JR-CSF strain.
Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504. [Abstract]
Effect of CVC (Cenicriviroc) (1 μM; 24 h) on endothelial permeability after OGD/R exposure and HIV-1 infection of astrocytes. Permeability was assessed by adding 10 kDa fluorescein isothiocyanate (FITC)-dextran (0.1 mg/mL) to the upper compartment of the Transwell system, followed by spectrophotometric measurement of its passage through human brain microvascular endothelial cell (HBMEC) monolayers into the lower compartment for 1 h.
Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504. [Abstract]
Cenicriviroc (CVC) (1 μM; 24 h). Representative images of Western blots for the tight junction (TJ) proteins zona occludens 1 (ZO-1), occludin, and claudin-5.
Cenicriviroc Mesylate purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2024 Feb 1;326(2):C487-C504. [Abstract]
Representative confocal immunofluorescence staining images of NLRP3 (green), ASC (red), and nuclei (blue). Scale bar: 50 μm.The results showed that the colocalization of NLRP3 with ASC was increased in OGD/R-treated infected astrocytes compared with the control, and this effect was partially alleviated by CVC (Cenicriviroc) (1 μM; 24 h) treatment, which suggests reduced inflammasome formation and activation.
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Sci Rep
Inhibition of intrahepatic monocyte recruitment by Cenicriviroc and extracellular matrix degradation by MMP1 synergistically attenuate liver inflammation and fibrogenesis in vivo. [Abstract]2024 Jul 23;14(1):16897. PMID: 39043893 -
Antiviral Res
The chemokine receptor antagonist cenicriviroc inhibits the replication of SARS-CoV-2 in vitro. [Abstract]2020 Oct;182:104902. PMID: 32739404 -
Eur J Immunol
Cenicriviroc, a CCR2/CCR5 antagonist, promotes the generation of type 1 regulatory T cells. [Abstract]2024 Jul;54(7):e2350847. PMID: 38643381 -
bioRxiv
MAIT cell responses to S. aureus and sensitivity to HlgAB are modulated by activation and tissue-dependent virulence effects. [Abstract]2026 Mar 19:2026.03.17.712383. PMID: 41890076
Solvent & Solubility
DMSO : 100 mg/mL (126.10 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: ≥ 2.08 mg/mL (2.62 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 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 (2.62 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.
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.
Protocol
Mouse monocyte migration in response to Cenicriviroc Mesylate (CVC) treatment is assessed ex vivo in triplicate. Thioglycollate (TG) is injected intraperitoneally into male C57BL/6 mice (n=3; 8 to 10 weeks of age) and activated macrophages are collected 48 hours later by peritoneal lavage. Cells are incubated for 2 hours in the presence of 1 μM Cenicriviroc Mesylate. Cells are harvested from the lower compartment and analyzed by flow cytometry to enumerate F4/80+CD11b+ macrophages. Results are analyzed using FlowJo software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male C57BL/6 mice (n=44; 8 to 10 weeks of age) are allocated to receive treatments via oral gavage (PO) on Days 1 to 5 in the following groups: non-disease control, vehicle control twice daily (BID), Cenicriviroc Mesylate 5 mg/kg/day (CVC5) BID, Cenicriviroc Mesylate 20 mg/kg/day (CVC20) BID, Cenicriviroc Mesylate 100 mg/kg/day (CVC100) BID, Cenicriviroc Mesylate 20 mg/kg once-daily (QD). On Day 4, peritonitis is induced via IP injection of thioglycollate (TG) 3.85% (1 mL/animal) 2 hours post-dose in all groups except non-disease controls[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 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]. Lefebvre E, et al. Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis. PLoS One. 2016 Jun 27;11(6):e0158156. [Content Brief]
[2]. Visseaux B, et al. Cenicriviroc, a Novel CCR5 (R5) and CCR2 Antagonist, Shows In Vitro Activity against R5 Tropic HIV-2 Clinical Isolates. PLoS One. 2015 Aug 6;10(8):e0134904. [Content Brief]
[3]. Lalezari J, et al. Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects. J Acquir Immune Defic Syndr. 2011 Jun 1;57(2):118-25. [Content Brief]
[4]. Baba M, et al. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans. Antimicrob Agents Chemother. 2005 Nov;49(11):4584-91. [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 |
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| DMSO | 1 mM | 1.2610 mL | 6.3048 mL | 12.6095 mL | 31.5239 mL |
| 5 mM | 0.2522 mL | 1.2610 mL | 2.5219 mL | 6.3048 mL | |
| 10 mM | 0.1261 mL | 0.6305 mL | 1.2610 mL | 3.1524 mL | |
| 15 mM | 0.0841 mL | 0.4203 mL | 0.8406 mL | 2.1016 mL | |
| 20 mM | 0.0630 mL | 0.3152 mL | 0.6305 mL | 1.5762 mL | |
| 25 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2610 mL | |
| 30 mM | 0.0420 mL | 0.2102 mL | 0.4203 mL | 1.0508 mL | |
| 40 mM | 0.0315 mL | 0.1576 mL | 0.3152 mL | 0.7881 mL | |
| 50 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL | |
| 60 mM | 0.0210 mL | 0.1051 mL | 0.2102 mL | 0.5254 mL | |
| 80 mM | 0.0158 mL | 0.0788 mL | 0.1576 mL | 0.3940 mL | |
| 100 mM | 0.0126 mL | 0.0630 mL | 0.1261 mL | 0.3152 mL |
Cenicriviroc Mesylate Related Classifications
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