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编 号:F005439
分子式:C12H10ClN
分子量:203.67
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生物活性:
3-Chlorodiphenylamine is a high affinity Ca2+?sensitizer of cardiac muscle. 3-Chlorodiphenylamine is based on diphenylamine and binds to the isolated N-domain of cardiac troponin C (cTnC) (Kd=6 μM). 3-Chlorodiphenylamine is an excellent starting scaffold for the development of more potent Ca2+-sensitizing compounds due to its small size, and can be used for systolic heart failure research.

体外研究:
3-Chlorodiphenylamine is able to bind highly (Kd=10 μM) to a chimeric protein consisting of the regulatory N-domain of cTnC (cNTnC) and the switch region of cTnI (cNTnC–cSp chimera).3-Chlorodiphenylamine (100 μM) results in a 1.5-fold increase in the Ca2+?sensitivity of force development without altering the maximal or resting forces in skinned ventricular trabeculae.3-Chlorodiphenylamine (25-100 μM) increases Ca2+?sensitivity of the N-domain of intact cTnC after reconstitution into the cTn complex (cTnC complexed with cTnI and cTnT) in a concentration-dependent manner. It exhibits pCa50s with 6.39±0.01, 6.65±0.01, and 6.73±0.02 in the presence of 25, 50, and 100 μM 3-Chlorodiphenylamine, respectively.
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