1. GPCR/G Protein
  2. Leukotriene Receptor
  3. SB-209247

SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity.

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SB-209247 Chemical Structure

SB-209247 Chemical Structure

CAS No. : 154413-61-3

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Description

SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity[1].

IC50 & Target[1]

LTB4

0.78 nM (Ki)

In Vitro

SB-209247 (Compound 3) demonstrates a high degree of selectivity for the LTB4 receptor. SB-209247 competes with [3H]-fMLP and [3H]LTD4 in respective receptor binding assays with IC50 values of 3250 nM and 16800 nM and with another 14 ligands with IC50 values greater than 10000 nM. Functional activity at the cellular level is demonstrated in human polymorphonuclear leukocytes (PMNs) by blocking the LTB4-induced Ca2+ mobilization and LTB4-induced degranulation with IC50 values of 6.6 nM and 53 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SB-209247 (Compound 3) has an ED50 of 14.8 mg/kg for inhibiting neutrophil influx in the murine model, and inhibits the fluid phase (edema) of the inflammatory response with an ED50 of 18.7 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

460.37

Formula

C23H19Cl2NO3S

CAS No.
SMILES

O=C(O)/C=C/C1=NC(CSC2=C(Cl)C=CC=C2Cl)=CC=C1OCCC3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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SB-209247 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SB-209247
Cat. No.:
HY-112741
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