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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
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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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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DC78153 (1R,2S)-Dihydrobupropion
(1R,2S)-Dihydrobupropion is a norepinephrine-dopamine reuptake inhibitor. (1R,2S)-Dihydrobupropion is one of the active metabolites of Bupropion. (1R,2S)-Dihydrobupropion can be used for the researches of neurological disease and inflammation.
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DC78151 KRG-3332 hydrochloride
KRG-3332 (hydrochloride) is a selective α1A receptor antagonist. KRG-3332 (hydrochloride) can be used in Glaucoma.
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DC78144 Ifoxetine
Ifoxetine (CGP 15210G) is an inhibitor of 5-HT reuptake. Ifoxetine specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine has antidepressant properties.
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DC78143 OPC-4392
OPC-4392 is a orally active presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist. OPC 4392 reverses the Reserpine-induced dopamine accumulation, inhibits Apomorphine-induced stereotypic and climbing behaviors in mouse models. OPC-4392 can be used as antipsychotic agent.
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DC78135 Sigma-2 Receptor ligand 1
Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective Sigma-2 receptor ligand with a Ki value of 40 nM. Sigma-2 Receptor ligand 1 is promising for research of Alzheimer's disease.
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DC78134 S-14489
S-14489 is an orally active selective postsynaptic 5-HT1A receptor antagonist with a pKi of 9.2. S-14489 can act as a 5-HT1A autoreceptor agonist and inhibit striatal 5-hydroxytryptophan accumulation. S-14489 can be used for the research of neurological disease.
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DC78129 Phenethyl 4-ANPP
Phenethyl 4-ANPP is a MOR (μ-opioid receptor) agonist. Phenethyl 4-ANPP is an analytical reference standard that is structurally similar to known opioids.
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DC78108 JNJ-17166864
JNJ-17166864 is a highly selective CCR2 antagonist. JNJ-17166864 has low oral bioavailability. JNJ-17166864 can significantly reduce the area of alveolar bone loss in a mouse model of periodontitis induced by Porphyromonas gingivalis infection. JNJ-17166864 can be used in the research of inflammatory diseases such as allergic rhinitis and periodontitis.
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DC78089 A-75998
A-75998 is an antagonist of luteinizing hormone-releasing hormone (LHRH). A-75998 can be used in the research of diseases such as hormone-sensitive cancers and endometriosis.
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DC78085 KC-11458
KC-11458 is a motilin agonist. KC-11458 can accelerate gastric emptying.
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DC78080 Dazodeunetant
Dazodeunetant (Example 56) is a nitrogen-containing fused ring derivative. Dazodeunetant is an inhibitor of neurokinin (NK). Dazodeunetant has an IC50 0f 75.99 nM against NK3R in HEK293-NK3 (IP1). Dazodeunetant can be studied in research for menopausal hot flashes.
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DC78044 GSK1842799
GSK1842799 is an orally active selective S1P1 receptor agonist prodrug. GSK1842799 is promising for research of multiple sclerosis.
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DC78029 RS130-180
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression.
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DC78011 CH0076989
CH0076989 is a specific CCR3 agonist. CH0076989 activates eosinophils and transfectants expressing both wild-type CCR3 and a CCR1:CCR3 chimaeric receptor lacking the CCR3 amino-terminus. CH0076989 has a direct interaction with the transmembrane helices of CCR3, supported by the complete loss of its activity due to mutations of the residues Y41, Y113 and E287. CH0076989 can be used for the study of inflammation and allergic diseases (such as asthma).
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DC78004 Zilebesiran sodium
Zilebesiran sodium is a siRNA that reduce hepatic angiotensinogen levels through RNA interference. it is used for the study of mild to moderate Hypertension. Angiotensinogen is the predominant precursor of angiotensin peptides and a key regulator of syste
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