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Postion:Product Catalog >Biochemical Engineering>Inhibitors>GPCR & G Protein>CXCR antagonist>Plerixafor 8HCl (AMD3100 8HCl)
Plerixafor 8HCl (AMD3100 8HCl)
  • Plerixafor 8HCl (AMD3100 8HCl)
  • Plerixafor 8HCl (AMD3100 8HCl)

Plerixafor 8HCl (AMD3100 8HCl) NEW

Price $3 $2 $1
Package 1kg 100kg 1000kg
Min. Order: 1kg
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-04-16

Product Details

Product Name: Plerixafor 8HCl (AMD3100 8HCl) CAS No.: 155148-31-5
Min. Order: 1kg Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/04/16
Lead time: In stock, ready for shipment Packaging: bag/bottle/drum/IBC
Delivery: By express, by air, by sea Origin: Manufacturer, advantage product
COA, MSDS: Available, contact us for details Contact person: Jessica

 1. Materials information

Names

NamePlerixafor 8HCl (AMD3100 8HCl)
SynonymMore Synonyms

 Plerixafor 8HCl (AMD3100 8HCl) Biological Activity

DescriptionPlerixafor octahydrochloride is a selective CXCR4 antagonist with an IC50 of 44 nM.
Related Catalog
Signaling Pathways >> GPCR/G Protein >> CXCR
Signaling Pathways >> Immunology/Inflammation >> CXCR
Research Areas >> Inflammation/Immunology
Target

125I-CXCL12-CXCR4:44 nM (IC50)

In VitroThe CXCR4 inhibitor Plerixafor (AMD3100) is a potent inhibitor of CXCL12-mediated chemotaxis (IC50, 5.7 nM) with a potency slightly better than its affinity for CXCR4. Treating the cells with CCX771 or CXCL11 has no effect on CXCL12-mediated MOLT-4 or U937 TEM. In contrast, 10 μM Plerixafor inhibits CXCL12-mediated TEM in both cells lines[1]. Plerixafor (10 μM)-treated cells show a moderate reduction in cell proliferation compared to CXCL12-stimulated cells, which do not reach statistical significance[2].
In VivoPlerixafor (2 mg/kg) administration to UUO mice exacerbates renal interstitial T cell infiltration, resulting in increased production of the pro-inflammatory cytokines IL-6 and IFN-γ and decreased expression of the anti-inflammatory cytokine IL-10[3]. Both perivascular and interstitial fibrosis are significantly reduced by the CXCR4 antagonist, Plerixafor (AMD3100) at 8 weeks[4]. LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg.
Cell AssayU87MG cells are seeded in 96-well plates at the density of 6×103 cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R, as described in the previous “Treatments” section. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments[2].
Animal AdminMice[3] Male C57bl/6 mice (6-7 weeks old, weighing 20 g) are used. The animals are acclimated to the housing environment, which is SPF and had a temperature of 22°C and a 12h/12h light/dark cycle for a week. Then, they are randomly divided into following experimental groups, with 8 mice in each group: normal (no specific intervention), UUO+AMD3100 (mice received UUO surgery and 2 mg/kg AMD3100), and UUO+PBS (mice received UUO surgery and the same volume of PBS). AMD3100 and PBS are administered via intraperitoneal injection every day until sacrifice. Rats[4] The CXCR4 antagonist, AMD3100 dissolved in H2O, is delivered in the type 2 diabetic sand rat model at a dose of 6 mg/kg per day for 8 weeks. In complementary studies, the effect of CXCR4 antagonism (AMD3100 6mg/kg/d) on regulatory T cell numbers is examined. For these studies, AMD3100 or vehicle is delivered via minipump for a period of one week.
References

[1]. Zabel BA, et al. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol. 2009 Sep 1;183(5):3204-11.

[2]. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55.

[3]. Yang J, et al. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926.

[4]. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616.

 Chemical & Physical Properties

Density0.962g/cm3
Boiling Point657.5ºC at 760mmHg
Molecular FormulaC28H62Cl8N8
Molecular Weight830.500
Flash Point361.8ºC
Exact Mass826.281677
PSA78.66000
LogP8.68040
Appearance of Characterssolid
Vapour Pressure2.85E-33mmHg at 25°C
Storage condition−20°C
Water SolubilityH2O: ≥10 mg/mL, clear

 Safety Information

Safety Phrases22-24/25
WGK Germany3




2. Packaging of materials

  • For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

  • For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                             Or smaller package 1kg/bottle, 10kgs/bottle as request. 


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3. Shipping & Delivery

  • By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

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  • By Air

Provide airport to airport service

Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

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  • By Sea

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Suitable for goods over 100kg

Delivery: 2-45 days

Cost: low cost

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4. Contact information

For more details, pls contact us freely.

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WhatsApp/Skype/Wechat/LINE: 86  17630971917


Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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