Chemicals to which isotopes have been attached in order to label specific atoms. Isotopically labeled compounds are commonly used in synthetic chemistry, characterization techniques such as NMR, and biology.
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An L-type calcium channel blocker induces morphological and growth defects in wild-type C. elegans and those with hypoexpression of egl-19 inhibits L-type calcium channels in chick ciliary neurons increases TRAIL-induced cytotoxicity and synergistically enhances caspase-8 and caspase-3 activation in a concentration-dependent manner in H1299 lung adenocarcinoma cells decreases Survivin expression in A549 cells
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An L- and T-type calcium channel inhibitor inhibits hamster Cav1 2a and human Cav3 2 (IC50s 1 8 and 350 nM respectively) inhibits L- and T-type calcium channels and fetal bovine serum-induced hypertrophy in isolated mouse cardiomyocytes increases survival in a mouse model of acute myocardial infarction induced by ligation of the left coronary artery at 200 mg/kg inhibits SARS-CoV-2 Mpro (IC50 38 5 UM)
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An LTB4 receptor antagonist (Ki 2 UM) inhibits chemotaxis and calcium flux by LTB4 in isolated human neutrophils (IC50s 10 and 7 UM respectively) inhibits bronchoconstriction induced by LTB4 in rats by 46
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An LTB4 receptor antagonist (Ki 2 UM) inhibits chemotaxis and calcium flux by LTB4 in isolated human neutrophils (IC50s 10 and 7 UM respectively) inhibits bronchoconstriction induced by LTB4 in rats by 46
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A TRPA1 antagonist (IC50 0.131 UM in a calcium mobilization assay) selective for human TRPA1 over human TRPV1 and TRPV4 rat TRPV1 TRPV3 and TRPM8 and a panel of 40 additional targets at 10 UM reduces the number of AITC-induced tail flinches in rats at 10 and 30 mg/kg
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A CCR4 receptor antagonist inhibits CCL22-induced calcium flux (IC50 31 6 nM) inhibits CCL22- and CCL17-mediated chemotaxis of Th2 cells (IC50 501 2 nM) reduces alveolitis and leukocyte infiltration in lungs of antigen-challenged ovalbumin sensitized rats in a dose-dependent manner (0 07-2 5 mg/kg p o )
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A diterpene with diverse biological activities a TRPV3 activator (EC50 16 UM for inducing calcium influx in HEK293 cells expressing TRPV3) inhibits IKBa degradation in TNF-a-stimulated HeLa cells at 60-140 UM reduces amyloid-B (25-35) peptide-induced apoptosis increases in MDA levels and the production of ROS reduces paw edema in a mouse model of hind paw inflammation at 50 mg/kg has anxiolytic and antidepressant-like activity in mice
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An agonist of FPR1 and FPR2 induces calcium flux in CHO cells expressing human FPR2 Ga15 and aequorin (EC50 0.044 UM) and in CHO-K1 cells expressing either human FPR1 human FPR2 mouse Fpr1 or mouse Fpr2 Ga16 and aequorin in a concentration-dependent manner inhibits fMLP- or IL-8-induced neutrophil migration (IC50s 0.64 and 0.24 UM respectively) reduces PGE2- and LTB4-induced ear swelling in mice at 50 mg/kg
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A purine nucleotide and an intermediate in the purine nucleotide cycle converted into AMP and fumarate by ADSL in the cytosol inhibits calcium-induced activation of non-selective cation channels in isolated rat brown adipocytes in a patch-clamp assay at 10 UM induces contractions in isolated guinea pig uterus strips at 100 UM increases glucose-induced insulin exocytosis in INS-1 832/13 insulinoma cells at 10 UM decreases muscle damage and pseudohypertrophy in a dystrophin-deficient mdx mouse model of DMD
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An EP4 receptor antagonist (IC50 6 1 nm in a calcium flux assay) selective for EP4 over EP1 EP2 and EP3 receptors (IC50s 10000 nM for all) reverses PGE2-induced ERK phosphorylation in EP4-expressing CHO cells and decreases GM-CSF-induced expression of Il1b Il4ra Il6 Arg1 Cox2 and Il10 in RAW 264 7 cells at 10 UM reduces tumor volume and increases infiltration of CD8 T cells into tumors in a murine colon carcinoma model at 50 and 150 mg/kg once per day
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