Anatibant | B2R antagonist | Probechem Biochemicals

Chemical Structure : Anatibant

Anatibant (LF 16-0687, XY-2405)

Catalog No.: PC-26632Not For Human Use, Lab Use Only.

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Biological Activity

Anatibant (LF 16-0687, XY-2405) is a potent, selective non-peptide bradykinin B2 receptor (B2R) antagonist with 0.67 nM, 1.74 nM and 1.37 nM for human, rat and guinea-pig recombinant B2 receptor respectively.
Anatibant (LF 16-0687, XY-2405) binds to the native BK B2 receptor from human umbilical vein (HUV), rat uterus (RU) and guinea-pig ileum (GPI) giving K(i) values of 0.89 nM, 0.28 nM and 0.98 nM, respectively.
Anatibant (LF 16-0687, XY-2405) inhibits BK-induced IP1, IP2 and IP3 formation in INT407 cells yielding pK(B) values of 8.5, 8.6 and 8.7, respectively.
Anatibant (LF 16-0687, XY-2405) is a competitive antagonist of BK-mediated contractions giving pA2 values of 9.1 in HUV, 7.7 in RU and 9.1 in GPI.
Anatibant (LF 16-0687, XY-2405) markedly reduced BK-induced edema of the stomach, duodenum and pancreas in rates.

Physicochemical Properties

M.Wt	784.58
Formula	C34H38Cl4N6O5S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-N-(3-(4-Carbamimidoylbenzamido)propyl)-1-((2,4-dichloro-3-(((2,4-dimethylquinolin-8-yl)oxy)methyl)phenyl)sulfonyl)pyrrolidine-2-carboxamide dihydrochloride

References

1. Pruneau D, et al. Immunopharmacology. 1999 Sep;43(2-3):187-94.

Anatibant (LF 16-0687, XY-2405)

Biological Activity

Physicochemical Properties

References

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