DC49633 |
BMS-193884 |
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor. |
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DC49634 |
GLP-1R agonist 8 |
GLP-1R agonist 8 is a potent GLP-1R agonist with an EC50 of < 2 nM (WO2021219019A1, compound 129a). |
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DC49635 |
GLP-1R agonist 7 |
GLP-1R agonist 7 is a potent GLP-1R agonist with an EC50 of 0.67 µM (WO2021244645A1, compound WXA001). |
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DC49636 |
GLP-1R agonist 5 |
GLP-1R agonist 5 is a potent GLP-1R agonist with an EC50 of <10 nM (WO2021259309A1, compound 35). |
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DC49637 |
GLP-1R agonist 6 |
GLP-1R agonist 6 is a potent GLP-1R agonist with an EC50 of 0.15 nM for human GLP-1R (WO2021249492A1, compound 005A or 005B). |
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DC49638 |
BAY 1214784 |
BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids. |
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DC49639 |
Roxatidine |
Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is a histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect. |
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DC49640 |
REV 5901 |
REV 5901 is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 is also a 5-lipoxygenase inhibitor. REV 5901 can be used for the research of asthma in which leukotriene release be involved. |
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DC49641 |
BAY-u 9773 |
BAY-u 9773 is a non-selective antagonist of the CysLT receptors (cysteinyl leukotrienes receptors) with about the same IC50 for CysLT1 and CysLT2. BAY-u9773 is used for the inhibition of LT responses. |
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DC49642 |
VU0455691 |
VU0455691 is a potent, selective orthosteric M1 mAChR antagonist (pIC50=6.64; IC50=0.23 µM for hM1). |
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DC49643 |
Heliosupine N-oxide |
Heliosupine N-oxide, Heliosupin metabolite, inhibits muscarinic acetylcholine receptor (mAChR) with the IC50 of 350 μM. Heliosupine N-oxide is a pyrrolizidine alkaloid (PA). |
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DC49644 |
McN-A-343 |
McN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 reduces inflammation and oxidative stress in an experimental model of ulcerative colitis. |
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DC49645 |
hMC1R agonist 1 |
(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family. |
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DC49646 |
N-Acetyltryptamine |
N-Acetyltryptamine is a partial agonist for melatonin receptors in the retina. N-Acetyltryptamine is also used for determination of serotonin N-acetyl transferase activity. |
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DC49647 |
MNI137
Featured
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MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization. |
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DC49648 |
Imnopitant dihydrochloride |
Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist. |
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DC49649 |
BIBP3226 |
BIBP3226 is a potent and selective neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist, with Kis of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 displays anxiogenic-like effect. |
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DC49650 |
Y1R probe-1
Featured
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Y1R probe-1 (Compound 39) is a high-affinity fluorescence probe for the Neuropeptide Y Y1 Receptor. Y1R probe-1 has the potential for the research of cancer disease. |
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DC49651 |
Acetyl tetrapeptide-15 |
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. |
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DC49652 |
MRS2395 |
MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6. |
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DC49653 |
BW A868C |
BW A868C, a hydantoin compound, is a BW245C structural analogue. BW A868C is a selective and potent competitive prostaglandin D2 (PGD2) antagonist. BW A868C has no effect on other prostaglandin receptors (IP, EP1, EP2, TP and FP). |
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DC49654 |
SC-51322 |
SC-51322 is a potent and selective antagonist of prostaglandin E2 (PGE2) receptor (EP 1), with a pA2 of 8.1. SC-51322 has the pain-relieving effect. |
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DC49655 |
8-Isoprostaglandin E2 |
8-Isoprostaglandin E2 (iPE2-III) is a member of the isoprostane class of prostanoids. 8-Isoprostaglandin E2 acts at the receptor for thromboxane A2 (the TP) in vivo to induce vasoconstriction and platelet aggregation. 8-Isoprostaglandin E2 enhances receptor-activated NFkappa B ligand (RANKL)-dependent osteoclastic potential of marrow hematopoietic precursors via the cAMP pathway. |
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DC49656 |
11β-Prostaglandin E2 |
11β-Prostaglandin E2 (11β-Dinoprostone), a Prostanoid derivative, inhibits [3H]PGE2 binding to hypothalamic membranes in the rat with a Ki of 53.3 nM. |
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DC49657 |
Tetranor-PGDM |
Tetranor-PGDM is an abundant urinary metabolite reflects biosynthesis of prostaglandin D2. |
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DC49658 |
Thielavin A |
Thielavin A is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin A specifically inhibits the conversion of arachidonic acid into prostaglandin H2. Thielavin A has no anti-inflammatory activity on intravenous injection or on oral administration. |
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DC49659 |
Thielavin B |
Thielavin B is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin B effectively influences the prostaglandin E2 synthesis from the endoperoxide. Thielavin B is significantly effective on carrageenan-induced oedema of rats when administered intravenously. |
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DC49660 |
Cicaprost |
Cicaprost (ZK 96480), an orally active prostacyclin (IP) analogue, is a selective IP receptor agonist. Cicaprost inhibits platelet aggregation in both in vitro and animal studies. Cicaprost inhibits the induction of cyclin A and activation of the cyclin A promoter in primary and established rodent aortic smooth muscle cells. |
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DC49661 |
AGI-43192
Featured
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AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease. |
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DC49662 |
AGI-41998 |
AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease. |
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