| DC70897 |
VU6028418 |
VU6028418 (VU 6028418) is a potent, highly selective, orally bioavailable M4 mAChR antagonist for the treatment of dystonia and other movement disorders. |
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| DC70906 |
WW-III-55 |
WW-III-55 is a high-affinity, selective dopamine D3 receptor (D3R) partial agonist with Ki value of 20 nM, exhibits >800-fold binding selectivity for D3R compared with the D2R.WW-III-55 (0-5.6 mg/kg) reduced cocaine self-administration, also reduced responding for sucrose and locomotor activity.WW-III-55 attenuated yawning induced by low doses of 7-OH-DPAT (a D3R-mediated behavior).WW-III-55 (10 mg/kg) inhibited the head twitch response (HTR) by 95% in DBA/2J mice. |
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| DC70932 |
Zevaquenabant |
Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual CB1 receptor/iNOS inhibitor.Zevaquenabant ((S)-MRI-1867) (3 mg/kg, p.o.) ameliorated obesity-induced kidney morphological and functional changes via decreasing kidney inflammation, fibrosis, oxidative stress, and renal injury.The hybrid CB1R/iNOS inhibitor Zevaquenabant ((S)-MRI-1867) has greater antifibrotic efficacy than inhibition of CB1R alone.(S)-MRI-1867 reduced hepatic steatosis and the rate of hepatic VLDL secretion, upregulated hepatic LDLR expression, and reduced the circulating levels of proprotein convertase subtilisin/kexin type 9 (PCSK9) in diet-induced obesity (DIO mice). |
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| DC70940 |
ZY12201 |
ZY12201 is a potent, selective, orally bioavailable TGR5 agonist with hTGR5 EC50 of 57 pM and mTGR EC50 of 62 pM.ZY12201 displays a favorable pharmacokinetic properties and demonstrated in-vivo glucose lowering effects in animal models (ED50 of 7.9 mg/kg and ED90 of 29.2 mg/kg). |
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| DC70943 |
N-Arachidonyldopamine |
N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM. |
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| DC70950 |
GAT564 |
GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma. |
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| DC70967 |
Eptazocine |
Eptazocine (Sedapain) is a κ-opioid receptor agonist and μ-opioid receptor antagonist. Eptazocine has the effect of relieving pain. |
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| DC70980 |
U-75302 |
U-75302 is a potent inhibitor of leukotriene B4. U-75302 is a pyridine analogue. U-75302 has the potential for the research of inflammatory diseases. |
|
| DC71003 |
AP5 sodium |
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research. |
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| DC71006 |
ATL-801 |
ATL-801, an A2B receptor selective antagonist, ameliorates murine colitis. |
|
| DC71022 |
CP 93129 dihydrochloride |
CP 93129 dihydrochloride is a potent 5HT1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research. |
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| DC71032 |
DS-3801b
Featured
|
DS-3801b is a potent and non-macrolide agonist of GPR38. DS-3801b is expected to be novel gastrointestinal prokinetic agents for the research of functional gastrointestinal disorders such as gastroparesis and chronic constipation. |
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| DC71049 |
GP1a |
GP1a is a potent agonist of cannabinoid receptor 2 (CB2). Gp1a is beneficial to skin wound healing. GP1a inhibits inflammation and fibrogenesis while promoting re-epithelialization. |
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| DC71057 |
Indoramin |
Indoramin is an orally active antihypertensive agent. Indoramin is also selective for the α1A-adrenoceptor. |
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| DC71070 |
L-817818 |
L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions |
|
| DC71079 |
MAP4 |
MAP4 is a selective group III mGluR antagonist in some electrophysiological systems. |
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| DC71084 |
ML 10302 |
ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases. |
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| DC71111 |
S 25585 |
S 25585 is a potent and selective neuropeptide Y (NPY) Y5 receptor antagonist. S 25585 reduces food intake but not through blockade of the NPY Y5 receptor. |
|
| DC71114 |
SM-2470 |
SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats. SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization. |
|
| DC71125 |
Thromboxane B1 |
Thromboxane B1 (TXB1) is one of thromboxane B (TXB) family members. Thromboxane is a member of the family of lipids known as eicosanoids. Thromboxane is named for its role in blood clot formation (thrombosis). |
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| DC71132 |
UCM707 |
UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of Anandamide. |
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| DC71155 |
Sigma-LIGAND-1 hydrochloride |
Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor. |
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| DC71156 |
SR2640 hydrochloride
Featured
|
SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma. |
|
| DC71157 |
Sulfinalol |
Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity. |
|
| DC71158 |
Trimazosin |
Trimazosin is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenoceptors. |
|
| DC71160 |
Lerisetron |
Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats. |
|
| DC71192 |
ABP688 |
ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor. |
|
| DC71194 |
DCB |
DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). |
|
| DC71204 |
Sabcomeline |
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research. |
|
| DC71205 |
SC 51089 |
SC-51089 is a selective antagonist of EP1 receptor with analgesic activity in vivo. |
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