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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-167151
CAS No.: 2107327-36-4
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PaPE-1 is a pathway-preferential estrogen receptor (ER) agonist that preferentially activates ER non-nuclear-initiated signaling while minimally activating nuclear-initiated signaling. PaPE-1 exhibits Ki values of 10 μM and 25 μM for human ERα and ERβ, respectively. The relatively low ER affinity and rapid receptor dissociation of PaPE-1 facilitate the triggering of non-nuclear mTOR/MAPK/AKT signaling, while reducing the recruitment of ERα to chromatin and sustained nuclear ER-dependent transcription. PaPE-1 is suitable for research related to non-nuclear ER signaling, metabolic disorders, ischemic brain injury, Alzheimer's disease, and ER-positive breast cancer .
Cat. No.: HY-173408
CAS No.: 2899254-71-6
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Nuclear Hormone Receptor 4A/NR4A Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase
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Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research .
Cat. No.: HY-P11246
CAS No.: 3057097-31-8
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Cat. No.: HY-P990291
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Cat. No.: HY-U00050S
Synonyms: E-10-OH-NT-d3
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(E)-10-Hydroxynortriptyline-d3 (E-10-OH-NT-d3) is the deuterated-labeled (E)-10-Hydroxynortriptyline (HY-U00050). (E)-10-Hydroxynortriptyline (E-10-OH-NT) is a blood-brain barrier-permeable norepinephrine uptake inhibitor. (E)-10-Hydroxynortriptyline effectively promotes central norepinephrine neuronal transmission, with little interindividual variation in in vivo potency. (E)-10-Hydroxynortriptyline has low affinity for muscarinic receptors, exhibits only extremely weak anticholinergic activity, and does not inhibit salivary secretion. (E)-10-Hydroxynortriptyline can be used in studies related to depression .
Cat. No.: HY-P84960
Synonyms: IL-3R common β chain; CDw131; Beta-C antibody; CD131 antibody; CDw131 antibody; Colony stimulating factor 2 receptor beta antibody; Colony stimulating factor 2 receptor beta low affinity; granulocyte macrophage; antibody; Common beta chain antibody; Csf2rb antibody; Cytokine receptor common beta chain antibody; Cytokine receptor common beta chain precursor; CDw131 antigen; antibody; Cytokine receptor common subunit beta antibody; GM CSF/IL 3/IL 5 receptor common beta chain antibody; GM-CSF/IL-3/IL-5 receptor common beta subunit antibody; granulocyte-macrophage colony-stimulating factor receptor; beta antibody; IL3RB antibody; IL3RB_HUMAN antibody; IL5RB antibody; Interleukin 3 receptor; beta antibody; Interleukin 3 receptor/granulocyte macrophage colony stimulating factor 3 receptor beta; high affinity; antibody; Interleukin 5 receptor; beta antibody; SMDP5 antibody; stimulating factor 3 receptor; beta; high affinity; antibody;
Cat. No.: HY-100966S
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-16950AR
CAS No.: 68392-35-8
Synonyms: Afimoxifene (Standard); 4-OHT (Standard)
Cat. No.: HY-178945
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KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation .
Cat. No.: HY-L110
100 compounds
Cyclic peptides are polypeptide chains taking cyclic ring structure, which exhibit diverse biological activities, such as antibacterial activity, immunosuppressive activity and anti-tumor activity. Cyclic peptides, with the features of good binding affinity, target selectivity and low toxicity, show great success as therapeutics. Multiple cyclic peptides are currently in clinical use, for examples, gramicidin and tyrocidine with bactericidal activity, cyclosporin A with immunosuppressive activity, and vancomycin with antibacterial activity. Furthermore, cyclic peptides usually have the sufficient size and a balanced conformational flexibility/rigidity for binding to flat protein-protein interaction (PPI) interfaces, which have potential to develop PPI drugs.
MCE offers a unique collection of 100 cyclic peptides, all of which have good bioactivities. MCE Cyclic Peptide Library is a powerful tool for drug discovery and PPI inhibitor screening.
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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-115702S
CAS No.: 211106-54-6
Synonyms: (Rac)-PAF (C16)-d4
Cat. No.: HY-120247
CAS No.: 1520893-08-6
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TASP0434299 (Compound 10) is a labeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography .
Cat. No.: HY-156807
CAS No.: 210751-39-6
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LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
Cat. No.: HY-175532
CAS No.: 3062458-27-6
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M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
Cat. No.: HY-D1056B1
Synonyms: LPS, from bacterial (Proteus vulgaris)
It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
Cat. No.: HY-P991525
CAS No.: 2923542-55-4
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Cat. No.: HY-W043748
CAS No.: 38862-24-7
Synonyms: N-Succinimidyl acrylate
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2,5-Dioxopyrrolidin-1-yl acrylate (N-Succinimidyl acrylate) is a lysine residue modifier and coupling monomer. 2,5-Dioxopyrrolidin-1-yl acrylate covalently modifies the primary amines of lysine residues on monoclonal anti-horseradish peroxidase IgG antibodies, neutralizes positive charges and replaces them with low-affinity acrylate groups. 2,5-Dioxopyrrolidin-1-yl acrylate inhibits the formation of rapid hard coronas on citrate-coated gold nanoparticles, induces antibody unfolding and loss of antigen-binding function, but does not affect the antigen-binding function of antibodies in free solution. 2,5-Dioxopyrrolidin-1-yl acrylate reacts with the ε-amino groups on lysine residues of L-asparaginase, introduces vinyl groups and generates N-hydroxysuccinimide. 2,5-Dioxopyrrolidin-1-yl acrylate regulates the activity of L-asparaginase .
Cat. No.: HY-160062
S2.2 aptamer sodium is a nucleic acid-based MUC1-binding aptamer with high affinity and low toxicity. Upon binding to its target, S2.2 aptamer sodium undergoes a conformational switch and restores fluorescence signal, serving as a targeted imaging agent for MUC1-positive cancer cells. S2.2 aptamer sodium enables targeted delivery to breast cancer cells with overexpressed MUC1. When formulated as the S2.2-PEG-MZF molecular probe, S2.2 aptamer sodium possesses the functions of T2 signal inhibition, magnetic field-induced hyperthermia and targeted magnetic resonance molecular imaging. In the S2.2-PEG-MZF/DOX nanoliposome, S2.2 aptamer sodium supports targeted thermochemotherapy, effectively inhibiting cancer cell proliferation and invasion as well as inducing apoptosis, and is widely used in studies related to breast cancer .
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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
