am-12

AM12 inhibits Lanthanide-evoked TRPC5 activity (IC50: 0.28 μM).

AM-1235 是一种有效的选择性大麻素受体 CB1 激动剂。

Bam 12P is a Pro-Met-enkephalin precursor that is isolated from the bovine adrenal medulla.

Bam 12P acetate 是牛肾上腺、垂体和下丘脑中推定的脑啡肽前体。

TMI-1 (WAY-171318) 是一种有效的抑制剂，用于抑制去整合素金属酶17 (ADAM17) 和其他基质金属蛋白酶MMPs。TMI-1 能够有效地抑制LPS 诱导的人原代单核细胞和人全血中TNF-α的分泌。TMI-1 在三阴性 (TN) 和过度表达ERBB2的乳腺肿瘤细胞系中选择性地诱导Caspase 依赖的细胞凋亡。

(R)-AM1241 binds to cannabinoid (CB) receptors and has greater than 100-fold selectivity for the CB2 over the CB1 receptor (Kis = 15 and 5,000 nM, respectively, in a membrane assay using human receptors). (R)-AM1241 acts as an agonist at human CB2 receptors (EC50 = 118 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 315 and 341 nM, respectively). Similar to the racemate AM1241 , (R)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (R)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone .

(S)-AM1241 binds to cannabinoid (CB) receptors and is selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively, in a membrane assay using human receptors). (S)-1241 acts as an agonist at human, rat, and mouse CB2 receptors but shows greater activity at human CB2 (EC50 = 131 nM) than at rat and mouse CB2 receptors (EC50 = 785 and 2,000 nM, respectively). Similar to the racemate AM1241 , (S)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (S)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone .

AM1241 是一种选择性大麻素 CB2 受体激动剂，Ki 为 3.4 nM，比 CB1 受体选择性高 82 倍。

PAMP-12 (human, porcine) acetate (PAMP-12 (human, porcine) acetate (196305-05-2 free base)) 是 ir-PAMP 的主要成分，由 AM 前体加工而成，PAMP-20 也是如此，并且可能参与心血管控制。

AM-6826 is a Pan-Pim inhibitor. In a mouse xenograft tumor model, AM-6826 can inhibit the growth of KMS-12-BM melanoma by 93%.

Paclitaxel octadecanedioate is a prodrug form of paclitaxel that is comprised of paclitaxel conjugated to 1,18-octadecanedioic acid.1 Unlike paclitaxel, it does not promote tubulin polymerization in vitro when used at a concentration of 10 μM. A 5:1 mixture of paclitaxel octadecanedioate:human serum albumin (HSA) is cytotoxic to HT-1080, PANC-1, and HT-29 cells (IC50s = 12, 2.48, and 8.62 nM, respectively). This mixture reduces tumor growth and increases survival in an HT-1080 mouse xenograft model in a dose-dependent manner. |1. Callmann, C.E., Leguyader, C.L.M., Burton, S.T., et al. Antitumor activity of 1,18-octadecanedioic acid-paclitaxel complexed with human serum albumin. J. Am. Chem. Soc. 141(30), 11765-11769 (2019).

Adrenomedullin (AM) (1-12), human, is a peptide with the sequence Tyr-Arg-Gln-Ser-Met-Asn-Asn-Phe-Gln-Gly-Leu-Arg. Adrenomedullin (AM) (1-12), human, was initially identified as a vasodilator, and as such, it has the ability to relax vascular tone. Other