| DC44750 |
Butaprost |
Butaprost is a selective prostaglandin E receptor (EP2) agonist with a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost effectively mitigates renal fibrogenesis. |
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| DC44752 |
L-803087 TFA |
L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic respon |
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| DC44778 |
Protirelin Acetate |
Protirelin (Thyrotropin-releasing-hormone, TRH, Thyroliberin) acetate is a highly conserved neuropeptide that exerts the hormonal control of thyroid-stimulating hormone (TSH) levels as well as neuromodulatory functions. |
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| DC44779 |
SGS518 oxalate |
SGS518 oxalate is a selective 5-HT6R antagonist. SGS518 oxalate can be used for the research of cognitive impairments such as amnesia, anxiety and depression, and it is effective in protecting mouse retina at high doses[1] |
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| DC44780 |
NPS ALX Compound 4a dihydrochloride |
NPS ALX Compound 4a dihydrochloride is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM. |
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| DC44781 |
Pimethixene maleate
Featured
|
Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.,5-HT2B [1](Cell-free assay)
5-HT2A [1](Cell-free assay)
Histamine H1 Receptor [1](Cell-free assay)
Muscarinic M2 [1](Cell-free assay)
Muscarinic M1 [1](Cell-free assay)
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10.44(pKi)
10.22(pKi)
10.14(pKi)
9.38(pKi)
8.61(pKi) |
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| DC44790 |
Ro 363 hydrochloride |
Ro 363 hydrochloride is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility. |
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| DC44791 |
Guanoxabenz hydrochloride |
Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor. |
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| DC44792 |
O-Desmethyl Mebeverine alcohol hydrochloride |
O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract. |
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| DC44793 |
FFN270 hydrochloride |
FFN270 hydrochloride, a fluorescent tracer of norepinephrine, is a fluorescent substrate of the norepinephrine and vesicular monoamine transporters. FFN270 hydrochloride exhibits two resolved absorption/excitation maxima depending on solvent pH (FFN270 ex: 320 nm or 365 nm, em: 475 nm) and can function as ratiometric fluorescent pH-sensors. |
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| DC44799 |
Angiotensin (1-7) (acetate) |
Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. |
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| DC44800 |
Angiotensin I/II (1-6) (TFA) |
Angiotensin I/II (1-6) TFA contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. The precursor angiotensinogen is cleaved by renin to form angiotensin I. Angiotensin I ishydrolyzed by angiotensin-converting enzyme (ACE) to form the biologically active angiotensin II. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy. |
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| DC44801 |
Novokinin TFA |
Novokinin TFA is a peptide agonist of the angiotensin AT2 receptor. |
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| DC44832 |
RVD-Hpα |
RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM). |
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| DC44834 |
TC14012 |
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity. |
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| DC44835 |
CTCE-9908 |
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells. |
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| DC44836 |
(R,R)-CXCR2-IN-2 |
(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively. |
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| DC44912 |
K-(D-1-Nal)-FwLL-NH2 |
K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways. |
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| DC44915 |
Ac-hMCH(6–16)-NH2 |
Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R. |
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| DC44942 |
H2L 5765834 |
H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, with IC50s of 94, 752, and 463 nM respectively. |
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| DC44944 |
JHU37160
Featured
|
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue. |
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| DC44945 |
JHU37152
Featured
|
JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay)
hM3Dq [1](Cell-free assay)
hM3Dq [1](Cell-free assay)
hM4Di [1](Cell-free assay)
0.5 nM(EC50)
1.8 nM(Ki)
5 nM(EC50)
8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1] |
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| DC44948 |
MSG606 |
MSG606 is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 exhibits binding affinity for A375 melanoma cells in vitro. MSG606 reverses morphine-induced hyperalgesia in female mice, with no effect in male mice. |
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| DC44949 |
JKC363 |
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect. |
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| DC44950 |
α-Melanocyte-Stimulating Hormone (MSH), amide TFA |
α-Melanocyte-Stimulating Hormone (MSH), amide TFA is an endogenous neuropeptide, with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist. |
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| DC44951 |
γ-1-Melanocyte Stimulating Hormone (MSH), amide |
γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na+) balance and blood pressure through activation of the melanocortin receptor 3 (MC3-R). |
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| DC44952 |
L-AP4 monohydrate |
L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively. |
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| DC44953 |
ML337 |
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile. |
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| DC44954 |
VU-1545 |
VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM. |
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| DC44955 |
RO0711401
Featured
|
RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM. |
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