LF 16-0687_product_DataBase

Bioactivity	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 Ki 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].
Invitro	In isolated organs experiments, LF 16-0687 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].LF 16-0687 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，Ki 值分别为 0.89 nM、0.28 nM 和 0.98 nM[ 2]。LF 16-0687 抑制 INT407 细胞中 bradykinin 诱导的 IP1、IP2 和 IP3 形成，产生的 pKB 值分别为 8.5、8.6 和 8.7[2]。在离体器官实验中，LF 16-0687 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. 0 --> LF 16-0687 相关抗体:
In Vivo	LF 16-0687（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]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	209733-45-9
Formula	C34H36Cl2N6O5S
Molar Mass	711.66
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.

PeptideDB

LF 16-0687

CAS: 209733-45-9 F: C34H36Cl2N6O5S W: 711.66