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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC78388 CGS 15873A
CGS 15873A is an orally active benzopyranopyridine derivative. CGS 15873A has selective dopamine receptor activation activity. CGS 15873A can be used for research on schizophrenia or Parkinson's disease.
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DC78387 CQP-201403
CQP-201403 is a dopamine receptor agonist. CQP-201403 can be used for the research of neurological disease.
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DC78381 ORG 31433
ORG 31433 is an orally active peptide related to the ACTH-(4-9) analog ORG 2766. ORG 31433 shows neuroprotective effect.
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DC78379 1-Hexadecyl lysophosphatidic acid sodium
1-Hexadecyl lysophosphatidic acid (1-Hexadecyl LPA) sodium, an ether analog of lysophosphatidic acid (LPA), is a LPA receptor activator.
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DC78372 (Z)-Flupenthixol decanoate
(Z)-Flupenthixol decanoate is the cis form of Flupenthixol decanoate. (Z)-Flupenthixol decanoate is a potent dopamine D1/D2 receptor antagonist. (Z)-Flupenthixol decanoate shows antipsychotic effect.
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DC78367 BBL454
BBL454 (Compound 43) is a Cholecystokinin 2B (CCK2B) receptor agonist. BBL454 induces hyperactivity and improves memory in rat models while it has weak activity on the peripheral CCK2 receptor and no anxiogenic activity. BBL454 increases gastric acid output in anesthetised rat models. BBL454 can be used for diabetes research.
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DC78365 U-46619 Glycine methyl ester
U-46619 Glycine methyl ester has a modification at the C-1 position of U-46619, which uniquely alter its binding properties to the TP receptor or any of the PGH2-metabolizing enzymes. U-46619 is a stable analog of the endoperoxide PGH2. U-46619 is also an agonist of TP receptor. U-46619 can change the shape of platelet, aggregation and contraction of vascular smooth muscle. U-46619 Glycine methyl ester can be studied in research to explore the inhibition of various enzymes in the arachidonic acid metabolic pathway. U-46619 Glycine methyl ester can also act as a lipophilic prodrug form of U-46619 that alters its distribution and pharmacokinetic properties.
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DC78364 EXP-7711
EXP-7711 is a non peptide angiotensin II (Ang II) AT1 receptor antagonist. EXP-7711’s affinity for wild-type AT1 receptor (Ki =180 nM) is lower than peptide antagonists, but higher than losartan (Ki = 12 nM). EXP-7711 can be used for research on cardiovascular conditions.
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DC78363 CR 3834
CR 3834 is a angiotensin-AT1 antagonist. CR 3834 can be used for the research of cardiovascular disease.
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DC78362 Carbaprostacyclin-biotin
Carbaprostacyclin-biotin (cPGI-biotin; Carbacyclin-biotin) is a biotin-bound Carbacyclin (Carbaprostacyclin)). Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
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DC78359 (±)5(6)-EET Ethanolamide
(±)5(6)-EET Ethanolamide is a metabolite of Anandamide generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has Ki values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.
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DC78352 P2Y12R ligand-1
P2Y12R ligand-1 (Compound 41) is a high-affinity P2Y12R ligand with a Ki value of 17.1 nM. P2Y12R ligand-1 labeled with [18F] can be used in studies of brain PET imaging.
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DC78351 MRS8454
MRS8454 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). MRS8454 can significantly enhance the maximum effect of the standard agonist Cl-IB-MECA by approximately 286%-300%, and significantly reduce its EC50 value. MRS8454 effectively enhances the ability of A3AR agonists to inhibit the cAMP accumulation induced by Forskolin. MRS8454 can be used for the development of molecular probes.
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DC78348 YM-358 hydrate potassium
YM-358 hydrate (potassium) is an orally active angiotensin II type 1 (AT1)-receptor antagonist. YM-358 hydrate (potassium) can decrease cardiac volume overload. YM-358 hydrate (potassium) can be used for the research of cardiovascular disease, such as hypertension.
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DC78340 SRI-45949
SRI-45949 is an allosteric modulator of the HIV-DAT-Tat interaction. SRI-45949 has IC50 values of 9.56 μM and 9.34 μM for [3H]DA uptake and [3H]WIN35,428 binding, respectively. SRI-45949 can be used in research related to HIV-associated neurocognitive disorders.
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DC78328 VU6008055
VU6008055 is a potent, selective, cross the blood-brain barrier and orally actively M4 positive allosteric modulator with EC50 values of 73.4, 19.5 nM for hM4, rM4, respectively. VU6008055 shows antipsychotic-like activity.
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DC78322 GSK-958108
GSK-958108 is a highly selective 5-HT1A receptor antagonist. GSK-958108 is commonly used in the study of neurological conditions.
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DC78317 MCI-225 hydrate hydrochloride
MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder.
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DC78308 PSB-22219
PSB-22219 is a highly selective non-nucleotidic ligand acting on P2Y12 receptors (KD=4.57 nM). PSB-22219 is promising for research of P2Y12 receptor-associated neuroinflammation.
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DC78307 MEPB
MEPB is a modulator of AF-2 of the androgen receptor. MEPB increases co-repressor binding of AR. MEPB can bind to the BF3 pockeet of AR specifically, thereby modulating the binding of co-regulators to the AF2 domain. MEPB alleviates degeneration in spinal bulbar muscular atrophy mouse model.
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DC78299 4-Hydroxy xylazine O-glucuronide lithium
4-Hydroxy xylazine O-glucuronide (lithium) is a metabolite of the α2-adrenergic receptor agonist xylazine. 4-Hydroxy xylazine O-glucuronide (lithium) can be synthesized from xylazine via the intermediate metabolite 4-hydroxy xylazine.
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DC78275 VU6002703
VU6002703 (Compound 17) is a BBB-penetrable M4 mAChR positive allosteric modulator (PAM) with an EC50 of 0.6  μM for hM4. VU6002703 can be used for neuropsychiatric and rare genetic CNS disorders research.
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DC78238 4-AcO-DALT hydrochloride
4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, histamine receptor 1 (H1), muscarinic M2 receptor and Sigma 2 receptor. 4-AcO-DALT hydrochloride shows Ki values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors.
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DC78223 S 33138
S33138 is a D3 receptor antagonist. S33138 inhibits addiction in animal models of addiction. S33138 reduces cognitive impairment in rodent and primate models of schizophrenia and Parkinson's disease. S33138 can be used in research on neurological disorders such as schizophrenia and Parkinson's disease.
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DC78216 EMD 386088 free base
EMD386088 free base is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 free base induces cell death. EMD386088 free base regulates the activity of ERK1/2. EMD386088 free base has the potential for the research of alzheimer's disease (AD) and schizophrenia.
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DC78205 GSK-1292263 hydrochloride
GSK-1292263 (hydrochloride) is an orally active GPR119 agonist (pEC50 of approximately 6.9 and 6.7 nM for human and rat GPR119, respectively). GSK-1292263 is used in the research of type 2 diabetes and dyslipidemia.
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DC78204 BI-5756
BI-5756 is a CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. BI-5756 can significantly increase HDL-C levels and reduce LDL-C levels. BI-5756 can also enhance the function of regulatory T cells while maintaining T cell-mediated anti-tumor activity. BI-5756 can directly inhibit the growth of tumor cells and upregulate the expression of MHC I, MHC II, and CD80 on tumor cells. BI-5756 has a protective effect in graft-versus-host disease models. BI-5756 can be used in research on tumors, graft-versus-host disease, and metabolic diseases.
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DC78200 WAY-207024
WAY-207024 is an orally active gonadotropin releasing hormone receptor (GnRH-R) antagonist (human GnRH: IC50 of 12 nM, rat GnRH: IC50 of 71 nM). WAY-207024 inhibits rat LH release with an IC50 of 350 nM. WAY-207024 lowers rat plasma leuteinizing hormone (LH) levels after oral administration.
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DC78186 (S)-Ebalzotan
(S)-Ebalzotan is the S-form of Ebalzotan. Ebalzotan is a 5-HT1A receptor agonist with activity in the study of depression. Ebalzotan can serve as a precursor to important active pharmaceutical ingredients. The synthesis of Ebalzotan involves a multi-enzyme catalyzed reduction reaction to obtain saturated primary or secondary alcohols in high yields and high enantioselectivity.
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DC78165 L-695499
L-695499 is a potent and orally active leukotriene D4 receptor antagonist. L-695499 can be used for the researches of inflammation and immunology.
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