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SCH527123

Cat. No. M2161
SCH527123 Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 280 In stock
50mg USD 620 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively. SCH-527123 bound with high affinity to the CXCR2 receptors of mouse (K(d) = 0.20 nM), rat (K(d) = 0.20 nM), and cynomolgus monkey (K(d) = 0.08 nM) and was a potent antagonist of CXCR2-mediated chemotaxis (IC(50) approximately 3-6 nM). In contrast, SCH527123 bound to cynomolgus CXCR1 with lesser affinity (K(d) = 41 nM) and weakly inhibited cynomolgus CXCR1-mediated chemotaxis (IC(50) approximately 1000 nM). Oral treatment with SCH527123 blocked pulmonary neutrophilia (ED(50) = 1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. SCH-527123 also suppressed the pulmonary neutrophilia (ED(50) = 1.3 mg/kg), goblet cell hyperplasia (ED(50) = 0.7 mg/kg), and increase in BAL mucin content (ED(50) = <1 mg/kg) in rats after i.t. administration of vanadium pentoxide. In vivo, SCH-527123 treatment decreased tumor growth and microvessel density when compared with vehicle-treated tumors.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 397.42
Formula C21H23N3O5
CAS Number 473727-83-2
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source The University of Birmingham (2015).SCH527123, Figure 5.5. (AbMole Bioscience, Kowloon, Hong Kong)
Method
Cell Lines CXCR2 and CXCR1
Concentrations 3nM (specific to CXCR2) and 42nM (required for concurrent CXCR1 inhibition).
Incubation Time
Results Pre-incubation with the dual CXCR1/2 inhibitor (SCH527123) at both concentrations (3 nM and 42 nM) caused a significant reduction in chemokinesis in gradients of both IL-8 and GROα, but only 3 nM caused a significant reduction of chemokinesis in Sol (Figure 5.5).
Rating
References

Safety and efficacy of a CXCR2 antagonist in patients with severe asthma and sputum neutrophils: a randomized, placebo-controlled clinical trial.
Nair P, et al. Clin Exp Allergy. 2012 Jul;42(7):1097-103. PMID: 22702508.

The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models.
Ning Y, et al. Mol Cancer Ther. 2012 Jun;11(6):1353-64. PMID: 22391039.

A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation.
Chapman RW, et al. J Pharmacol Exp Ther. 2007 Aug;322(2):486-93. PMID: 17496165.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SCH527123 supplier, CXCR, inhibitors

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