| DC49663 |
SB-611812 |
SB-611812 is a urotensin II receptor (UTR) antagonist with the potential in the treatment of cardiovascular disease. |
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| DC49664 |
H2L5186303
Featured
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H2L5186303 is a potent and selective LPA2 receptor (lysophosphatidic acid 2 receptor) antagonist with an IC50 of 9 nM. |
|
| DC49665 |
S1P1 agonist 5 |
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS). |
|
| DC50168 |
BMS-639623 |
BMS-639623 is a potent and orally activeCCR3 antagonist with an IC50 of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC50=38 pM). BMS-639623 can be used for the research of asthma. |
|
| DC50169 |
CCR8 antagonist 1 |
CCR8 antagonist 1 (compound 15) is a potente human CCR8 antagonist with a Ki of 1.6 nM. |
|
| DC50170 |
Fuscin |
Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor. |
|
| DC50201 |
CXCR4 antagonist 3 |
CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus. |
|
| DC50202 |
HF51116 |
HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis. |
|
| DC50203 |
CXCR4 antagonist 4 |
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM). |
|
| DC50225 |
GSK1614343 |
GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models. |
|
| DC50231 |
Deoxycholic acid-13C |
Deoxycholic acid-13C (Cholanoic acid-13C) is the 13C-labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity. |
|
| DC50232 |
Cholic acid 7-sulfate |
Cholic acid 7-sulfate (7-Sulfocholic acid), a metabolite of Cholic acid, is a Takeda G-protein receptor 5 (TGR5) agonist. Cholic acid 7-sulfate can increase Tgr5 expression and induce GLP-1 secretion. |
|
| DC50258 |
TCS-OX2-29 hydrochloride |
TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1. |
|
| DC70087 |
Desmopressin
Featured
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Desmopressin is a synthetic analogue of the antidiuretic hormone arginine vasopressin. |
|
| DC70088 |
VUF11207 fumarate |
VUF11207 fumarate is a potent CXCR7 (ACKR3) agonist with EC50 of 1.6 nM, inducse recruitment of β-arrestin2 and subsequent internalization of CXCR7 in cells. |
|
| DC70092 |
GSK3004774 |
GSK3004774 (GSK-3004774) is a potent, nonabsorbable, gastrointestinally-restricted agonist agonist of calcium-sensing receptor (CaSR) with pEC50 of 7.3. |
|
| DC70106 |
GSK598809 hydrochloride |
GSK598809 hydrochloride is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9. |
|
| DC70107 |
GSK598809 |
GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9. |
|
| DC70108 |
(–)-IHCH7041 |
(–)-IHCH7041 is a potent, selective partial agonist at DRD2/3 and 5-HT1AR, EC50 of 1.38 nM in Gαi1–γ9 dissociation and 2.75 nM in β-arrestin2 recruitment assays, with negligible 5-HT2AR binding (>100-fold selectivity).(–)-IHCH7041 exhibits negligible affinities for a large number of tested GPCRs, ion channels and transporters (Ki>500 nM), good affinities for DRD2 and DRD3 (Ki=14.42 nM), and moderate binding to 5-HT1A (Ki=60.62 nM).(–)-IHCH7041 behaves as a partial agonist in both G-protein signaling and β-arrestin recruitment activities at DRD2, DRD3 and 5-HT1AR.(–)-IHCH7041 displayed potent antipsychotic activity and has antidepressant properties and reverses cognitive impairmentin mice. |
|
| DC70110 |
(R)-LMI |
(R)-LMI (H2N-R-Leu-Met-Ile-COOH) is a tripeptide analogue of corticotropin-releasing factor (CRF) and CRF antagonist targeting the N-domain of CRF1 receptor;
(R)-LMI inhibits CRF-stimulated cAMP accumulation with IC50 of 1.7 uM.
(R)-LMI inhibits the production of interleukins by adipocytes and the proliferation rate of RAW 264.7 cells. |
|
| DC70112 |
(R,S′)-MNF |
(R,S′)-MNF is a bi-functional GPR55 inhibitor and biased β2 adrenergic agonist, inhibits proliferation of PDAC cell lines (IC50=0.11 uM, PANC-1 cells).
(R,S′)-MNF is a biased β2-AR agonist that selectively signals through Gαs and does not recruit β-arrestin-2.
(R,S′)-MNF attenuates pro-oncogenic signaling and cellular proliferation in PANC-1 cells.
(R,S′)-MNF (1 uM) significantly decreased ERK phosphorylation stimulated by the GPR55 ligand O-1602, (R,S′)-MNF is an effective inhibitor of GPR55 internalization and signaling.
(R,S′)-MNF (20-40 mg/Kg) reduces PANC-1 tumor growth in a mouse xenograft model. |
|
| DC70128 |
ALT-1188 |
A novel potent, nonpeptide CXCR4 antagonist with IC50 of 0.93 nM; induces increased and prolonged mobilization of murine HSPC compared to AMD3100. |
|
| DC70129 |
PRX-177561 |
A novel potent, selective, brain-penetrating, orally active CXCR4 antagonist with Ki of 3 nM; inhibits tumor growth alone, increases the antitumor effects of bevacizumab and sunitinib in preclinical models of human glioblastoma; reduces the expression of Nestin in vivo, reduces tumor cell proliferation and accelerates cancer stem cell differentiation in glioblastoma preclinical models. |
|
| DC70134 |
Oxytocin GMP grade
Featured
|
A peptide hormone and neuropeptide that is released into the bloodstream as a hormone in response to stretching of the cervix and uterus during labor and with stimulation of the nipples from breastfeeding. |
|
| DC70135 |
Bremelanotide
Featured
|
A peptide, non-selective melanocortin receptor agonist for treatment for female sexual dysfunction; selectively stimulates solicitational behaviors in the female rat, without affecting lordosis, pacing, or other sexual behaviors, does not cause generalized motor activation; a peptide analogue of α-MSH. |
|
| DC70139 |
GSK 2041706 |
A potent, selective and orally bioavailable GPR119 agonist with EC50 of 4 nM, with good selectivity versus a battery of receptors, ion channels and enzymes; causes greater reductions in cumulative food intake and higher fed plasma GLP-1 and peptide tyrosine tyrosine levels and decreased plasma insulin and glucose-dependent insulinotropic polypeptide levels, when combined with metformin, in diet-induced obese mice. |
|
| DC70140 |
GSK 163929 |
A potent, selective CCR5 antagonist and HIV-1 entry inhibitor with pIC50 of 8.37 and 8.46 in HOS and PBL assays, respectively. |
|
| DC70141 |
GSK 214096 |
A potent, selective CCR5 antagonist and HIV-1 entry inhibitor. |
|
| DC70147 |
GSK962040 |
A potent, selective, small molecule motilin receptor agonist with pEC50 of 7.9 (hMTL-R); displays selectivity over closely related human ghrelin acceptor (pEC50< 6.0) and no liabilities at the hERG
channel; possesses highly excellent pharmacokinetic profiles in both rat and dog. |
|
| DC70148 |
GSK962040 hydrochloride |
A potent, selective, small molecule motilin receptor agonist with pEC50 of 7.9 (hMTL-R); displays selectivity over closely related human ghrelin acceptor (pEC50< 6.0) and no liabilities at the hERG
channel; possesses highly excellent pharmacokinetic profiles in both rat and dog. |
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