Icatibant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

缓激肽 B2 受体 (B2R) 的选择性和特异性拮抗剂，IC50 和 Ki 分别为 1.07 nM 和 0.798 nM。

A selective and specific antagonist of bradykinin B2 receptor (B2R) with IC50 and Ki of 1.07 nM and 0.798 nM respectively; protects against memory impairment in mLFPI mice (10 nmol/kg); attenuates the brain edema, interleukin-1β, tumor necrosis factor-α, and nitric oxide metabolites content elicited by mLFPI.Other Indication Approved.

Icatibant (10-30 μM) potentiates angiotensin III, but not angiotensin II (contraction mediated by angiotensin AT1 receptors), and Lys-des-Arg9-bradykinin, but not des-Arg9-bradykinin (effects mediated by the bradykinin B1 receptors).

Icatibant (0.3, or 1.5 mg/kg, subcutaneous administration twice daily in mice) shows a significant preventive effect on ulcerative Colitis. Animal Model:Female mice of the CBA/J (H-2k) strain.Dosage:0.06, 0.3, or 1.5 mg/kg.Administration:Subcutaneous administration twice daily.Result:The length of the large intestine was 93.6±6.8 mm with the 1.5 mg/kg dosage and 94.0±4.1 mm with the 0.3 mg/kg dosage , showing a significant preventive effect on shortening.

HOE-140 | JE-049

GPCR/G Protein

Bradykinin Receptor

Bradykinin Receptor

Other Indications

Other Disease

130308-48-4

1304.522

C59H89N19O13S

>98% (HPLC)

10 mM in DMSO

N=C(N)NC(C(C1NCC2=C(C=CC=C2)C1)=O)CC[C@@H](C(O)=O)N(C([C@H](CO)N(C(CN(C([C@H]3N(C([C@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)N)=O)=O)CCC3)=O)C(C4NC[C@H](O)C4)=O)=O)C([C@H](CC5=CC=CS5)N)=O)=O)C(C6N[C@@]7([H])CCCC[C@@]7([H])C6)=O

L-Arginine, D-arginyl-L-arginyl-L-prolyl-(4R)-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-(3R)-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-(2S,3aS,7aS)-octahydro-1H-indole-2-carbonyl-

(-20℃)

With Ice Pack

≥ 2 years