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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
735 Results for "
partial
" in MedChemExpress (MCE) Product Catalog:
Products (735)
735 Results for "partial" in MCE Product Catalog:
Cat. No.: HY-109112R
CAS No.: 1239729-06-6
Synonyms: RP5063 (Standard)
Research Areas:
Brilaroxazine (Standard) is the analytical standard of Brilaroxazine. This product is intended for research and analytical applications. 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: SOM3355
Bevantolol hydrochloride (SOM3355) is a selective β1-adrenergic receptor antagonist, with an IC50 of 35 nM for β1-adrenergic receptor and an IC50 of 60 nM for VMAT2. Bevantolol hydrochloride blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol hydrochloride reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol hydrochloride is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease .
Cat. No.: HY-162083
CAS No.: 2821085-76-9
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CB2R/5-HT1AR agonist 1 (Compound 2o) is an orally active partial agonist of the CB2 receptor (EC50=479.6 nM). CB2R/5-HT1AR agonist 1 is a full agonist of 5-HT1A receptor (EC50=2.7 μM). CB2R/5-HT1AR agonist 1 exhibits anti-anxiety and anti-depressive effects. CB2R/5-HT1AR agonist 1 possesses favorable pharmacokinetic properties .
Cat. No.: HY-165459
CAS No.: 401907-57-1
Synonyms: MK-056
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KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (Ki=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus .
Cat. No.: HY-18102BS
Cat. No.: HY-18137
CAS No.: 1331782-27-4
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PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .
Cat. No.: HY-19689
CAS No.: 90043-86-0
Synonyms: NIK-247; Amiridine
Research Areas:
Ipidacrine (NIK-247; Amiridine) hydrochloride is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine hydrochloride has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine hydrochloride is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine hydrochloride is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine hydrochloride is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
Cat. No.: HY-A0249
CAS No.: 59170-23-9
Synonyms: SOM3355 free base
Research Areas:
Bevantolol (SOM3355 (free base)) is a selective β1-adrenergic receptor antagonist, with an IC50 of 35 nM for β1-adrenergic receptor and an IC50 of 60 nM for VMAT2. Bevantolol blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease .
Cat. No.: HY-B0696AR
CAS No.: 145821-59-6
Synonyms: NO050328 hydrochloride (Standard); NO328 hydrochloride (Standard); TGB hydrochloride (Standard)
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Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
Cat. No.: HY-B0696AS
Synonyms: NO050328-d4 hydrochloride; NO328-d4 hydrochloride; TGB-d4 hydrochloride
Cat. No.: HY-B0696S
CAS No.: 1217672-34-8
Synonyms: NO050328-d6; NO328-d6; TGB-d6
Cat. No.: HY-B0696S1
Synonyms: NO050328-d4; NO328-d4; TGB-d4
Cat. No.: HY-G0002S
CAS No.: 2070009-33-3
Category:
Cat. No.: HY-W004588
CAS No.: 72914-19-3
tBu2bpy is a bidentate nitrogen ligand that coordinates with Pt (II) and Pt (IV) to form functional complexes. The tBu2bpy Pt (II) bis-crown ether complex selectively recognizes Mg 2+ and Zn 2+; both ions significantly enhance the fluorescence of the complex and cause a blue shift of the absorption peak. Its six-coordinate Pt (IV) complex [Pt (X)2Me2 ( tBu2bpy)] inhibits the proliferation of tumor cells. tBu2bpy Pt (IV) complexes bind to DNA through multiple interactions including partial intercalation, groove binding, and electrostatic interaction, and can competitively displace ethidium bromide and covalently bind to purine nucleotides. tBu2bpy can be used in relevant research in fields such as organic synthesis .
Cat. No.: HY-W009009R
CAS No.: 286456-42-6
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L-838417 (Standard) is the analytical standard of L-838417 (HY-W009009). This product is intended for research and analytical applications. 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 .
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D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile .
Cat. No.: HY-114421R
CAS No.: 2064175-41-1
Synonyms: dTAG-13 (Standard)
Research Areas:
FKBP12 PROTAC dTAG-13 (Standard) is the analytical standard of FKBP12 PROTAC dTAG-13 (HY-114421). This product is intended for research and analytical applications. FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12 F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12 F36V, without degrading wild-type FKBP12 or un-fused PXR. It weakly promotes the recruitment of SRC-1, strongly inhibits the interaction between NCoR and PXR, and upregulates the expression of CYP3A4 and other drug metabolism-related genes. FKBP12 PROTAC dTAG-13 is applicable to research related to breast cancer and leukemia .
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GNE-274 is a non-degrading estrogen receptor α (ERα/ESR1) modulator structurally similar to GDC-0927 (HY-111484). GNE-274 competes for binding to the ligand-binding domain of ERα and induces a coregulator-binding conformation similar to that of antagonists, yet retains partial agonistic transcriptional activity and does not promote ERα turnover. GNE-274 effectively inhibits E2-stimulated proliferation of ER-positive, HER2-negative breast cancer cells. GNE-274 promotes the recruitment of ERα to the nucleus and chromatin, increases chromatin accessibility, while largely maintaining the intranuclear mobility of ERα. GNE-274 can be used in research on ER-positive breast cancer and ERα transcriptional dynamics .
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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
