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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
346 Results for "
low affinity
" in MedChemExpress (MCE) Product Catalog:
Products (346)
346 Results for "low affinity" in MCE Product Catalog:
Cat. No.: HY-103336
CAS No.: 1186195-59-4
Synonyms: T1117
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Tocrifluor 1117 is a selective GPR55 ligand and fluorescent probe. Tocrifluor 1117 shows extremely low affinity for mouse CB1 receptors (Ki >1000 nM) and only weakly displaces CB1 agonists. Tocrifluor 1117 specifically activates GPR55 to trigger intracellular calcium oscillations, and binds to vascular smooth muscle, endothelial and adventitial cells; all these binding effects are inhibited by pretreatment with unlabeled AM251 or O1602. Tocrifluor 1117 can clearly visualize the distribution of GPR55 in vascular tissues via confocal microscopy, while its uptake in cancer cells is completely dependent on GPR55 expression .
Cat. No.: HY-106993AR
CAS No.: 223420-20-0
Synonyms: GT-2331 maleate (Standard)
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Cipralisant maleate (Standard) is the analytical standard of Cipralisant (maleate) (HY-106993A). This product is intended for research and analytical applications. Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research . Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Category:
Alkaloids Ricinus communis L. Other Diseases Pyridine Alkaloids Plants Disease Research Fields Euphorbiaceae Extract
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Cat. No.: HY-123480
CAS No.: 755040-97-2
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EGIS-7625 is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human Ki value of 1 nM. EGIS-7625 shows low affinity for 5-HT2A and 5-HT2C receptors. The pKi values of EGIS-7625 for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 alleviates mCPP-induced hypoactivity .
Cat. No.: HY-159829
CAS No.: 1803346-98-6
Synonyms: NBI-1117568; HTL-0016878
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Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
Cat. No.: HY-Z12208
CAS No.: 1305124-48-4
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Cat. No.: HY-106993R
CAS No.: 213027-19-1
Synonyms: GT-2331 (Standard)
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Cipralisant (Standard) (GT-2331 (Standard)) is the analytical standard of Cipralisant (HY-106993). This product is intended for research and analytical applications. Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research . Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-159829A
CAS No.: 3028447-14-2
Synonyms: NBI-1117568 citrate; HTL-0016878 citrate
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Direclidine (NBI-1117568, HTL-0016878) citrate is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. Direclidine citrate binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine citrate specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine citrate can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
Cat. No.: HY-180526
CAS No.: 2055901-03-4
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PDE2A-IN-2 is a selective and brain-penetrant PDE2A inhibitor (Ki = 5.49 nM and 100 > fold selectivity over other PDE isoforms). The 11C-labeled PDE2A-IN-2 serves as a positron emission tomography (PET) tracer for brain imaging in patients with neurodegenerative diseases. PDE2A-IN-2 educes the radiotracer signal in PDE2A-rich regions in vitro. PDE2A-IN-2 exhibits low binding affinity in vivo. PDE2A-IN-2 can be used for neurodegenerative diseases .
Cat. No.: HY-181472
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10 (11)-Cl-BBQ is a high-affinity aryl hydrocarbon receptor (AhR) agonist. 10 (11)-Cl-BBQ is a mixture of 10-Cl-BBQ and 11-Cl-BBQ, among which 11-Cl-BBQ exhibits higher AhR activation potency than 10-Cl-BBQ. Low-dose/short-term AhR activation by 10 (11)-Cl-BBQ promotes IL-17 production, while high-dose/sustained activation induces regulatory T cells and suppresses immune responses. 10 (11)-Cl-BBQ can be used in immunomodulation research .
Cat. No.: HY-182381
CAS No.: 84226-14-2
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FLA-797 is a brain-penetrant dopamine D2 receptor blocker and very low affinity for dopamine D1 receptors. FLA-797 selectively binds to and blocks postsynaptic dopamine D2 receptors. FLA-797 induces catalepsy in male rats. FLA-797 blocks dopamine agonist-induced hypothermia in male rats. FLA-797 contributes marginally to the dopamine D2 receptor-blocking activity of Remoxipride (HY-101313) in male rats. FLA-797 does not mimic the atypical antipsychotic profile of Remoxipride. FLA-797 can be used for research on mental disorders .
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-D3439
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Phazr-N3 is a near-infrared (NIR) environment-sensitive fluorescent probe used to monitor the entire aggregation process of Aβ42 (amyloid-β42) from monomers/early aggregates to mature fibrils and plaques. Phazr-N3 binds Aβ42 in a structure-independent manner, exhibits low micromolar affinity (Kd = 6.6 μM) for free, disordered Aβ42 under non-aggregating conditions, and produces a solvatochromic fluorescence shift driven by local polarity changes during aggregation. Phazr-N3 uses a 580/680 nm excitation/emission setting in Aβ aggregation [1].
Cat. No.: HY-DY2037
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Lignin Staining Solution (Safranin Method) is a histochemical staining solution for lignin with Safranin O as the active component. Lignin Staining Solution (Safranin Method) enables lignified cell walls to appear red to deep red (pinkish in regions with low lignification) via the high affinity of the dye for lignin. Lignin Staining Solution (Safranin Method) can be used to visualize lignin distribution in ex vivo thick sections of annual shoots from woody plants and vibratome sections of stems from herbaceous plants (such as Arabidopsis and flax), as well as for in situ quantification of cell wall substructural regions (cell corners, intercellular layers, secondary walls) based on Safranin O ratiometric fluorescence .
Cat. No.: HY-P5362
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Cat. No.: HY-P5396
CAS No.: 152468-44-5
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Cat. No.: HY-P5396A
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Cat. No.: HY-W742404
CAS No.: 1794891-82-9
Synonyms: (±)-Bopindolol-d9
Cat. No.: HY-W782446
CAS No.: 136321-15-8
Synonyms: DMSO-13C2
Cat. No.: HY-Z15823
CAS No.: 38321-02-7
Synonyms: Dexverapamil
Research Areas:
(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Cav1.2) (IC50 > 300 μM), and its IC50 for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC50 of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp) .
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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
