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MedChemExpressModel Anatibant -209733-45-9

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

MCE China:Anatibant

Brand:MedChemExpress (MCE)

Cat. No.HY-121156

CAS:209733-45-9

Synonyms:LF 16-0687; XY-2405

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

Shipping:Room temperature in continental US; may vary elsewhere.

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

In Vitro:Anatibant binds to the native bradykinin B2 receptor from human umbilical vein (HUV), rat uterus (RU) and guinea-pig ileum (GPI) giving Ki values of 0.89 nM, 0.28 nM and 0.98 nM, respectively[2]. Anatibant inhibits bradykinin-induced IP1, IP2 and IP3 formation in INT407 cells yielding pKB values of 8.5, 8.6 and 8.7, respectively[2].

In Vivo:Anatibant (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].

IC50 & Target:Bradykinin B2 Receptor (B2R) 0.67 nM (Ki, human recombinant B2 receptor) Bradykinin B2 Receptor (B2R) 1.74 nM (Ki, Rat recombinant B2 receptor) Bradykinin B2 Receptor (B2R) 1.37 nM (Ki, Guinea-pig recombinant B2 receptor)

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References:

[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]

Brand introduction:
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