Anatibant  (Synonyms: LF 16-0687; XY-2405)

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 K_i 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].

In isolated organs experiments, Anatibant behaved as a competitive antagonist of bradykinin-mediated contractions giving pA₂ values of 9.1 in HUV, 7.7 in RU and 9.1 in GPI^[2].
Anatibant 与来自人脐静脉 (HUV)、大鼠子宫 (RU) 和豚鼠回肠 (GPI) 的天然 bradykinin B2 受体结合，K_i 值分别为 0.89 nM、0.28 nM 和 0.98 nM^{[ 2]}。
Anatibant 抑制 INT407 细胞中 bradykinin 诱导的 IP1、IP2 和 IP3 形成，产生的 pK_B 值分别为 8.5、8.6 和 8.7^[2]。
在离体器官实验中，Anatibant 充当 bradykinin 介导的收缩的竞争性拮抗剂，使 HUV 中的 pA2 值为 9.1，RU 中的 pA₂ 值为 7.7，GPI 中的 pA2 值为 9.1^[2]。

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

Anatibant（3 mg/kg；皮下推注；分别在创伤后 15 分钟和 8 小时注射）可显着降低治疗小鼠创伤后 24 小时的颅内压 (ICP) 和挫伤体积^[1]。

711.66

C₃₄H₃₆Cl₂N₆O₅S

209733-45-9

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]