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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
587 Results for "
partial agonists
" in MedChemExpress (MCE) Product Catalog:
Products (587)
587 Results for "partial agonists" in MCE Product Catalog:
Cat. No.: HY-100634
CAS No.: 14133-90-5
Synonyms: (±)-4-hydroxy Propranolol hydrochloride
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4-Hydroxypropranolol hydrochloride is a non-cardiac selective β-adrenergic receptor antagonist and a metabolite produced after oral administration of Propranolol (HY-B0573B). 4-Hydroxypropranolol hydrochloride also acts as a membrane stabilizer and possesses intrinsic sympathomimetic inhibitory activity. 4-Hydroxypropranolol hydrochloride blocks β-adrenergic receptors to antagonize the effects of catecholamines, acts as a partial β-adrenergic receptor agonist, and induces membrane stabilization. 4-Hydroxypropranolol hydrochloride alters heart rate, left ventricular contractility, and atrioventricular conduction time. 4-Hydroxypropranolol hydrochloride can be used in research related to cardiovascular and cerebrovascular diseases .
Cat. No.: HY-111254R
CAS No.: 870554-67-9
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GQ-16 (Standard) is the analytical standard of GQ-16 (HY-111254). This product is intended for research and analytical applications. GQ-16 is an orally active PPARγ partial agonist with an IC50 of 1.84 μM and a Ki of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer .
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LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties .
Synonyms: (1S,5R)-CP-601927
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CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
Cat. No.: HY-148032
CAS No.: 20776-45-8
Synonyms: 5-BT
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5-Benzyloxytryptamine (5-BT) is a selective partial agonist for 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors with an IC50 value of 40 nM for bovine caudate 5-HT1D and reduced affinity for other receptors (5-HT2 IC50>470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase to decrease neurotransmitter release and downregulate cAMP signaling. 5-Benzyloxytryptamine is promising for research of neurotransmitter imbalance-related disorders like migraine .
Cat. No.: HY-19842
CAS No.: 618380-90-8
Synonyms: CVT 3619
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GS-9667 (CVT 3619), a novel N 6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA) .
Cat. No.: HY-G0002
CAS No.: 186204-33-1
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Lurasidone metabolite 14326 is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 can be used in the research of schizophrenia and bipolar depression .
Cat. No.: HY-G0002A
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Lurasidone metabolite 14326 hydrochloride is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 hydrochloride shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 hydrochloride can be used in the research of schizophrenia and bipolar depression .
Cat. No.: HY-W742404
CAS No.: 1794891-82-9
Synonyms: (±)-Bopindolol-d9
Synonyms: RP5063
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Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .
Synonyms: OPC-34712-d8
Synonyms: OPC-34712-d8-1
Category:
Alkaloids other families Monophenols Other Diseases Phenols Plants Disease Research Fields Isoquinoline Alkaloids
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Cat. No.: HY-P1650
CAS No.: 215713-39-6
Synonyms: B 9870
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Breceptin (B 9870) is an antagonist of the bradykinin B1/B2 receptor (B1/B2R). Breceptin exhibits an irreversible antagonist effect on B2R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B2R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer .
Cat. No.: HY-W009009
CAS No.: 286456-42-6
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L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2. L-838417 has anti-anxiety activity .
Cat. No.: HY-108548
CAS No.: 185246-32-6
Synonyms: Rp-8-Bromo-PET-cGMPS
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Rp-8-Br-PET-cGMPS sodium (Rp-8-Bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
Cat. No.: HY-115857
CAS No.: 872874-00-5
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SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
Cat. No.: HY-116982
CAS No.: 21102-94-3
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BMY 7378 (free base) is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 (free base) binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 (free base) is a 5-HT1A receptor partial agonist .
Cat. No.: HY-175070
Synonyms: Ins(2,4,5)P3 sodium salt; 2,4,5-IP3 sodium salt
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D-myo-Inositol-2,4,5-triphosphate (Ins(2,4,5)P3) (sodium salt) is a second messenger produced in cells by phospholipase C-mediated hydrolysis of phosphatidylinositol-4,5-biphosphate. D-myo-Inositol-2,4,5-triphosphate (sodium salt) can open calcium channels and increase intracellular calcium upon binding to its receptors on the endoplasmic reticulum. D-myo-Inositol-2,4,5-triphosphate (sodium salt) also acts as a partial agonist at rat hepatic IP3 receptors. D-myo-Inositol-2,4,5-triphosphate (sodium salt) can be studied in research on calcium ions signaling pathway .
Cat. No.: HY-176287
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ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
