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Cat. No. Product Name Field of Application Chemical Structure
DC70149 AZ 13381758 A potent, small molecule CXCR2 inhibitor with IC50 of 26 nM and 30 nM for mCXCR2 and hCXCR2, respectively; inhibits the growth and metastatic potential pancreatic ductal adenocarcinoma, enhances sensitivity to anti-PD1 immunotherapy in vivo; chemical analog of AZD 5069.
DC70151 Pasireotide ditrifluoroacetate A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively); effectively inhibits GHRH-induced growth hormone release in primary cultures of rat pituitary cells with IC50 of 0.4 nM, also potently suppresses GH secretion in rats.
DC70176 AGH-107 Featured AGH-107 is a potent, selective 5-HT7 receptor agonist with Ki of 6 nM and EC50 of 19 nM, 176-fold selectivity over 5-HT1AR.AGH-107 exhibited high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.
DC70177 AGH-192 AGH-192 is a potent, selective, orally bioavailable 5-HT7 receptor agonist with Ki of 4 nM.AGH-192 displays excellent water solubility, high selectivity over related CNS targets, high metabolic stability, oral bioavailability and low cytotoxicity.AGH-192 could crosses blood-brain barrier to a high extent.AGH-192 alleviates the symptoms of neuropathic pain in a mouse model.
DC70181 ALESIA ALESIA is a specific sphingosine-1-phosphate receptor 3 (S1PR3)-G12-biased agonist and selectively induces G12 signal.ALESIA promotes nitric oxide production and oxidative stress.ALESIA selectively induces apoptosis in cancer cells because of low glucose levels.Intraperitoneal administration of ALESIA improved the survival of mice with peritoneally disseminated rhabdomyosarcoma.ALESIA (Anticancer Ligand Enhancing Starvation-induced Apoptosis) is a new anticancer compound for glucose starvation therapy.
DC70190 AMD3451 AMD3451 is a specific, dual CXCR5/CXCR4 antagonist with antiviral activity against a wide variety of HIV-1 and HIV-2 (IC50=1.2 to 26.5 uM) in vitro.AMD3451 has antiviral activity against a wide variety of R5, R5/X4, and X4 strains if HIV-1 and HIV-2 in various T-cell lines, CCR5- or CXCR4-transfected cells, PBMCs, and monocytes/macrophages.AMD3451 inhibited R5, R5/X4, and X4 HIV-1 primary clinical isolates in PBMCs (IC50, 1.8 to 7.3 uM), AMD3451 blocks R5 and X4 HIV-1 infection at the virus entry stage.AMD3451 dose-dependently inhibited the intracellular Ca2+ signaling induced by the CXCR4 ligand CXCL12 in T-lymphocytic cells and in CXCR4-transfected cells, as well as the Ca2+ flux induced by the CCR5 ligands CCL5, CCL3, and CCL4 in CCR5-transfected cells.AMD3451 did not interfere with chemokine-induced Ca2+ signaling through CCR1, CCR2, CCR3, CCR4, CCR6, CCR9, or CXCR3 and did not induce intracellular Ca2+ signaling by itself at 400 uM.AMD3451 inhibited CXCL12- and CCL3L1-induced endocytosis in CXCR4- and CCR5-transfected cells.AMD3451 does not inhibit the binding of CXCR4- or CCR5-specific MAbs.
DC70215 ASP2205 ASP2205 (ASP2205 fumarate) is a potent, selective 5-HT2C receptor agonist with EC50 of 0.85/2.5 nM for human/rat 5-HT2C in the intracellular Ca2+ mobilization assays, respectively.ASP2205 showed partial agonistic action on human 5-HT2A receptor with EC50 of 96 nM, no agonistic action against 5-HT2B.ASP2205 (0.1-1 mg/kg, i.d.) significantly elevated the leak point pressure (LPP) in anesthetized rats in a dose-dependent manner.ASP2205 is a more potent and selective 5-HT2C receptor agonist than lorcaserin.
DC70216 ASP8302 Featured ASP8302 (ASP 8302) is a potent, selective, positive allosteric modulator (PAM) of muscarinic M3 receptor.Threonine 230 (Thr 230) is the amino acid essential for the PAM effect of ASP8302.
DC70219 AstraZeneca CCR4 antagonist AstraZeneca CCR4 antagonist is a potent, selective CCR4 antagonist, inhibits CCR4 ligand macrophage-derived chemokine (MDC/CCL22) in CCR4+CD4+ T cells.
DC70257 BL-6020 979 BL-6020/979 (SNT207979) is an orally available, selective, potent MC4R antagonist with IC50 of 19 nM; weakly binds to MC-3 and MC-5 receptors with IC50 of 2.7 uM and 0.89 uM, respectively, >10,000-fold selectivity over MC-1R; demonstrates in animal models and presents a promising candidate suitable for further development towards a first-in-class treatment option for cachexia.
DC70261 BMS-570520 BMS-570520 is a potent, selective CCR3 antagonist with IC50 of 1.9 nM, inhibits eotaxin-induced chemotaxis with IC50 of 0.068 nM.BMS-570520 displays reduced inhibition on CYP2D6 (IC50=1300 nM) compared with DPC168 (IC50=30 nM), also possesses >100-fold selectivity over 5-HT2a, DAT and NET.BMS-570520 showed good activity in murine models of CCR3 antagonism and greater in vitro potency and in vivo in the mouse intranasal eotaxin challenge mode.
DC70263 BMS-846372 BMS-846372 (BMS846372) is a potent, selective, orally active CGRP receptor antagonist with Ki of 0.07 nM (hCGRP).BMS-846372 inhibited CGRP-stimulated cAMP production in SK-N-MC cells with IC50 of 0.22 nM, could completely inhibited CGRP-mediated elevation of cAMP.BMS-846372 showed exposure-dependent inhibition of CGRP-induced increases in marmoset facial blood flow upon subcutaneous (sc) dosing in hαCGRP-induced increases in facial blood flow model.
DC70268 BPR1M97 BPR1M97 is a dual-acting mu-opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively.BPR1M97 elicited full agonist properties for all cell-based assays tested in MOP-expressing cells.BPR1M97 acted as a G protein-biased agonist for NOP.BPR1M97 initiated faster antinociceptive effects after subcutaneous injection and elicited better analgesia in cancer-induced pain than morphine.BPR1M97 caused less respiratory, cardiovascular, and gastrointestinal dysfunction, compared with morphine.
DC70278 BX471 hydrochloride BX471 is a potent, selective, orally available CCR1 antagonist with Ki of 1 nM for hCCR1, displays 100 times less affinity for rat CCR1; shows 10,000-fold selectivity for CCR1 compared with 28 GPCRs (); displays CCR1 ligands MIP-1α, RANTES, and MCP-3 with high affinity (Ki=1-5.5 nM), inhibits a number of CCR1-mediated effects including Ca(2+) mobilization, increase in extracellular acidification rate, CD11b expression; effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis.
DC70290 CCR2 Covalent-IN-14 CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.CCR2 covalent-IN-14 is more potent than non-covalent analogue and wash-resistant in functional assays (IC50=33 nM in GTPγS binding assay on U2OS-CCR2 cell membranes, IC50=4 nM in β-arrestin recruitment assays).CCR2 covalent-IN-14 displays little to no inhibitory potency on CCR1 and CCR5.The affinity of CCR2 covalent-IN-14 for both the C70S and C75S CCR2 mutants is significantly decreased compared to WT CCR2.
DC70291 CCR2 inhibitor SD-24 CCR2 inhibitor SD-24 is a potent selective CCR2 antagonist with pKi of 8.5.
DC70292 CCR4-IN-38 Featured CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade.
DC70293 CCR7 inhibitor Cmp1205 CCR7 inhibitor Cmp1205 is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with Kd of 3 nM, suppresses arrestin binding in response to activation by CCL19 with IC50 of 7.3 uM.Cmp1205 binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8.Cmp1205 allosterically inhibits binding of the native chemokine CCL19 ligand in a membrane-based competition binding experiment with IC50 of 35 nM.
DC70295 CCX-6239 CCX-6239 is a novel potent, orally available CCR4 inhibitor with potential utility in the treatment of allergic airways disease.
DC70310 CJ-1639 CJ-1639 (CJ1639) is a potent, highly selective dopamine D3 receptor (D3R) full agonist with Ki of 0.5 nM, >5,000-fold selectivity over D1 and D2 receptors in binding assays.CJ-1639 binds to human D3 receptor with a K(i) value of 3.61 nM and displays over >1000-fold selectivity over human D1 and D2 receptors.CJ-1639 is an excellent pharmacological tool to elucidate the role of the D3 receptor in different neurological conditions in animal models.
DC70320 Cotadutide Cotadutide (MEDI-0382) is a dual GLP-1/glucagon receptor peptide agonist with robust anti-obesity and metabolic effects.
DC70333 CXCR6 inhibitor 81 Featured CXCR6 inhibitor 81 is a potent (EC50=40 nM) and selective orally bioavailable small molecule antagonist of human CXCR6 receptor; Compound 81 displays >10-fold improvement in potency in both the β-arrestin and cAMP assays (IC50 =40 and 540 nM, respectively) compared to ML339. CXCR6 inhibitor 81 inhibits migration of SK-HEP-1 hepatoma cells in a dose dependent manner. Compound 81 has promising oral DMPK data, significantly decreases tumor growth in a 30-day mouse xenograft model of HCC.
DC70334 CXCR7 modulator 20 CXCR7 modulator 20 is a small molecule modulator of the atypical chemokine receptor CXCR7 with Ki of 52 nM.
DC70338 DA-1241 DA-1241 (DA1241) is a novel potent, highly selective GPR119 agonist, activates human GPR119 (EC50=4.37 nM) in increasing cAMP levels in GPR119-overexpressing HEK293 cells.DA-1241 increased cAMP levels via activated mouse GPR119 (EC50, 71.5 nM) and rat GPR119 (EC50, 156 nM).DA-1241 showed no significant activity against 156 off-target proteins at 10 uM, including human GLP-1 receptor and human GPR40.DA-1241 stimulated insulin secretion in hamster insulinoma HIT-T15 cells with EC50 of 22.3 nM, association with enhanced human insulin promoter activity.DA-1241 significantly reduced postprandial glucose excursion, significantly preserved β-cell mass with reduced PDX1 levels in the islets from HFD/STZ diabetic mice.DA-1241 reduced triglyceride content in the liver thereby improved fatty liver, reduced gluconeogenic enzyme expression in HepG2 cells and mouse liver, reduced autophagic flow in HepG2 cells.
DC70345 DCP1-3 DCP1-3 is a novel allosteric ligand of the angiotensin receptor AT1R, displays NAM potency on AngIV with IC50 of 0.29 uM.DCP1-3 reduces AngII-induced contraction in renal and iliac arteries in mice.DCP1-3 inhibits IgG binding to HEK-AT1R cells with IC50 of 2.9 nM.DCP1-3 reverses PAM effect of the IgG on the agonist-induced calcium response.
DC70360 DL-175 DL-175 is a potent and selective biased GPR84 agonist with EC50 of 33 nM.DL-175 exhibits no significant activity in a panel of 168 other GPCRs.DL-175 display significantly biased signaling across GPR84-overexpressing cells, primary murine macrophages, and human U937 cells.DL-175 markedly different abilities to induce chemotaxis in human myeloid cells, while causing similar levels of phagocytosis enhancement.
DC70366 DPC168 DPC168 (DPC-168) is a highly potent, selective CC chemokine receptor-3 (CCR3) antagonist with IC50 of 2.0 nM, inhibits eotaxin-induced chemotaxis with IC50 of 0.034 nM.DPC168 demonstrates potency for mouse CCR3 (chemotaxis IC50=41 nM) and oral bioavailability in mice (20% F).DPC168 reduced eosinophil recruitment into the lungs in a dose-dependent manner in these animal models.
DC70384 EMU-116 EMU-116 (EMU-000116) is a potent, selective CXCR4 antagonist with IC50 29.6 nM in Ca2+ flux assay.
DC70388 Enerisant Enerisant (S091,TS-091) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.Enerisant inhibited R-α-methylhistamine–stimulated [35S]GTPγS binding to human histamine H3 receptor and rat histamine H3 receptor with IC50 values of 1.06 and 10.05 nM, respectively, inhibited basal [35S]GTPγS binding to human histamine H3 receptor with an EC50 value of 0.357 nM.Enerisant displays negligible effects on binding to human histamine H1, H2, and H4 receptor subtypes, as well as negligible affinities for 66 other receptors, transporters, and ion channels at 1-10 uM.Oral administration of enerisant hydrochloride attenuated the dipsogenia response on R-α-methylhistamine–induced dipsogenia in rats, the intraperitoneal administration of enerisant hydrochloride increased the total extracellular acetylcholine levels in the mPFC.Enerisant hydrochloride significantly decreased slow-wave deep sleep at doses of 1-10 mg/kg (P < 0.01-0.05). Enerisant hydrochloride (1, 3 and 10 mg/kg, p.o.) did not affect the accumulated locomotor activity time at up to 7 hours after administration.
DC70389 Enerisant hydrochloride Enerisant hydrochloride (TS091 hydrochloride) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.Enerisant inhibited R-α-methylhistamine–stimulated [35S]GTPγS binding to human histamine H3 receptor and rat histamine H3 receptor with IC50 values of 1.06 and 10.05 nM, respectively, inhibited basal [35S]GTPγS binding to human histamine H3 receptor with an EC50 value of 0.357 nM.Enerisant displays negligible effects on binding to human histamine H1, H2, and H4 receptor subtypes, as well as negligible affinities for 66 other receptors, transporters, and ion channels at 1-10 uM.Oral administration of enerisant hydrochloride attenuated the dipsogenia response on R-α-methylhistamine–induced dipsogenia in rats, the intraperitoneal administration of enerisant hydrochloride increased the total extracellular acetylcholine levels in the mPFC.Enerisant hydrochloride significantly decreased slow-wave deep sleep at doses of 1-10 mg/kg (P < 0.01-0.05). Enerisant hydrochloride (1, 3 and 10 mg/kg, p.o.) did not affect the accumulated locomotor activity time at up to 7 hours after administration.

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