enterocytes

DMT1 blocker 2 是一种二价金属转运蛋白 1 的直接抑制剂(IC50:0.83 μM)。它可以阻断体内肠细胞的铁摄取。

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

TLR4-IN-C34-C2-COO is a linker compound that incorporates TLR4 inhibitor TLR4-IN-C34. It effectively inhibits TLR4 activity in enterocytes and macrophages. Moreover, it demonstrates a notable ability to mitigate systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis.

TLR4-IN-C34-C2-amide-C6-OH 是一种含有 TLR4抑制剂 TLR4-IN-C34 的连接子。TLR4-IN-C34 抑制肠细胞和巨噬细胞中的 TLR4，减少内毒素血症和坏死性小肠结肠炎小鼠模型的全身炎症。

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH为包括TLR4抑制剂TLR4-IN-C34的连接子。该化合物通过抑制肠细胞与巨噬细胞内TLR4活性，能够减轻内毒素血症及坏死性小肠结肠炎小鼠模型中的全身性炎症。

Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH 是一种含有 TLR4抑制剂 TLR4-IN-C34 的连接子。TLR4-IN-C34 抑制肠细胞和巨噬细胞中的TLR4，减少内毒素血症和坏死性小肠结肠炎小鼠模型的全身炎症。

Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH 是一种融合了TLR4-IN-C34抑制剂的连接子。这种抑制剂在阻断肠细胞与巨噬细胞内的TLR4上发挥作用，有效减轻了内毒素血症及坏死性小肠结肠炎小鼠模型中的全身性炎症现象。