LF 16-0687  (Synonyms: XY-2405)

LF 16-0687 (XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. LF 16-0687 binds to the human, rat and guinea-pig recombinant B2 receptor with K_i values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. LF 16-0687 crosses the blood-brain barrier (BBB). LF 16-0687 can be used in research on brain damage diseases^[1][2].

LF 16-0687 binds to the native bradykinin 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^[2].
LF 16-0687 inhibits bradykinin-induced IP1, IP2 and IP3 formation in INT407 cells yielding pK_B values of 8.5, 8.6 and 8.7, respectively^[2].

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

LF 16-0687 (3 mg/kg; subcutaneous bolus; injection 15 min and 8 h after trauma, respectively) significantly reduces intracranial pressure (ICP) and of contusion volume 24 h after trauma in treated mice^[1].

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

711.66

C₃₄H₃₆Cl₂N₆O₅S

209733-45-9

O=C(NCCCNC(C1=CC=C(C=C1)C(N)=N)=O)[C@H]2N(CCC2)S(=O)(C3=CC=C(C(COC4=C5N=C(C=C(C5=CC=C4)C)C)=C3Cl)Cl)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Klaus Zweckberger, et al. Anatibant, a selective non-peptide bradykinin B2 receptor antagonist, reduces intracranial hypertension and histopathological damage after experimental traumatic brain injury. Neurosci Lett. 2009 Apr 24;454(2):115-7.  [Content Brief]

  [2]. D Pruneau, et al. Pharmacological profile of LF 16-0687, a new potent non-peptide bradykinin B2 receptor antagonist. Immunopharmacology. 1999 Sep;43(2-3):187-94.  [Content Brief]