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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
937 Results for "
peripheral restriction
" in MedChemExpress (MCE) Product Catalog:
Products (937)
937 Results for "peripheral restriction" in MCE Product Catalog:
Cat. No.: HY-P11896
CAS No.: 3081054-30-7
Research Areas:
Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 is a MOR-selective antagonist with a pA2 value of 9.9. Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 blocks G protein- and β-arrestin2-mediated downstream signaling pathways of MOR. Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 significantly delays the development of μ-opioid agonist-induced analgesic tolerance by blocking peripheral MOR. Tyr-c[D-Lys-p-Br-Phe-Phe-Asp]-D-Pro-NH2 is applicable to studies related to opioid receptor function and analgesic tolerance .
Cat. No.: HY-P1723A
Synonyms: Neuropeptide Q TFA
Research Areas:
Cat. No.: HY-P1764
CAS No.: 149146-12-3
Target:
Dopamine Receptor Caspase NOD-like Receptor (NLR) IGF-1R VEGFR FGFR AMPK ERK p38 MAPK JAK Bcl-2 Family STAT Apoptosis
Research Areas:
Secretoneurin, rat is a 33-amino acid neuropeptide produced by proteolytic processing of chromogranin II, widely distributed in the central and peripheral nervous systems, and its release is calcium-dependent. Secretoneurin, rat modulates the activities of caspase-3, caspase-1, the NLRP3 inflammasome, IGF-1R, VEGFR1, VEGFR2, FGFR3, AMPK, ERK1/2/MAPK, and Jak2/Stat3 pathways. Secretoneurin, rat regulates neuronal apoptosis, synaptic structure, inflammation, neurogenesis, angiogenesis, oxidative stress, cardiomyocyte hypertrophy, dopamine release, and cell migration and proliferation. Secretoneurin, rat is used in studies of global cerebral ischemia, myocardial infarction, stroke, and cardiac hypertrophy .
Cat. No.: HY-P5640
CAS No.: 179264-81-4
Cat. No.: HY-P990160
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Cat. No.: HY-P992426
Target:
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Cat. No.: HY-W005255S
Research Areas:
3-(3-Hydroxyphenyl)propionic acid- 13C is the 13C-labeled 3-(3-Hydroxyphenyl)propionic acid (HY-W005255). 3-(3-Hydroxyphenyl)propionic acid (3HPPA) is an endothelium-dependent nitric oxide (NO) release promoter and endothelial nitric oxide synthase (eNOS) activator. 3-(3-Hydroxyphenyl)propionic acid activates eNOS to mediate vascular smooth muscle relaxation and enhances endothelial cell NO synthesis, inducing vasodilation and reducing peripheral vascular resistance. 3-(3-Hydroxyphenyl)propionic acid can dose-dependently reduce systolic and diastolic blood pressure in spontaneously hypertensive rats (SHR) without affecting cardiac contractility or heart rate. 3-(3-Hydroxyphenyl)propionic acid has antihypertensive and vascular protective effects and can be used in the prevention and treatment of cardiovascular diseases .
Cat. No.: HY-103078R
CAS No.: 5496-35-5
Research Areas:
I-XW-053 (Standard) is the analytical standard of I-XW-053 (HY-103078). This product is intended for research and analytical applications. I-XW-053 is a specific anti-HIV-1 capsid inhibitor (IC50=164.2 μM). By binding to the CA NTD-NTD hexamerization interface and the R173 region of CTD (Kd=66.3 μM), I-XW-053 disrupts capsid function and reduces polymerization levels. I-XW-053 effectively blocks HIV-1 uncoating, inhibits reverse transcription and early replication, and exhibits broad-spectrum activity against primary HIV-1 isolates in peripheral blood mononuclear cells. I-XW-053 can be widely used in studies related to HIV-1 infection .
Cat. No.: HY-106224AS1
Synonyms: Hypocretin-1-13C18,15N3 (human, rat, mouse) TFA
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Target:
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3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells . 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Cat. No.: HY-118917
CAS No.: 297730-05-3
Target:
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VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with Ki values for IMPDH Ⅱ and IMPDH Ⅰ of 6 and 14 nM respectively. VX-148 can significantly inhibit the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated by T-cell mitogen (PHA) or B-cell mitogen (SPAS). VX-148 has high selectivity for lymphocytes (such as L1210, Jurkat T cells, and Raji B cells), but has no significant toxicity to non-lymphoid cells. VX-148 can inhibit antibody responses in mouse models and significantly prolong the survival time of transplanted skin in allogeneic skin transplantation models. VX-148 can be used in the research of autoimmune diseases (such as rheumatoid arthritis, psoriasis) and organ transplantation anti-rejection .
Cat. No.: HY-134092
CAS No.: 131391-65-6
Synonyms: N-Methyl-LTC4
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N-Methyl Leukotriene C4 (N-Methyl-LTC4) is a non-metabolizable LTC4 analog and a selective cysteinyl leukotriene receptor 2 (CysLT2) agonist, with an EC50 of 46.1 nM for mouse CysLT2 and an EC50 value of 122.3 nM for human CysLT2. N-Methyl Leukotriene C4 shows low potency against CysLT1. N-Methyl Leukotriene C4 activates human and mouse CysLT2 receptors, triggering calcium signaling, β-arrestin-2 binding to phosphorylated receptors, vascular leakage, hypotension, tachycardia, contraction of guinea pig ileum and trachea, mild bronchoconstriction, as well as hypertension associated with peripheral vasoconstriction. N-Methyl Leukotriene C4 can be used in research on asthma, rhinitis, sinusitis, cerebral inflammation and edema, pulmonary arterial hypertension, and cardiovascular diseases .
Cat. No.: HY-134440
CAS No.: 104809-20-3
Target:
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α,β-Methylene-ATP dilithium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP dilithium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP dilithium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP dilithium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
Cat. No.: HY-134440A
CAS No.: 7292-42-4
Target:
Research Areas:
α,β-Methylene-ATP is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
Cat. No.: HY-14977
CAS No.: 840523-39-9
Target:
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CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
Cat. No.: HY-173447
CAS No.: 344402-39-7
8-BuS-AMP is a NTPDase1 inhibitor and a CD73/CD39 inhibitor, with an IC50 of 35 μM and a Ki value of 0.292 μM against human NTPDase1; its Ki values against human CD73 and CD39 are 1.19 μM and 0.847 μM, respectively. 8-BuS-AMP binds to the substrate-binding pockets of NTPDase1 and CD73 to effectively block the conversion of ATP and AMP to adenosine, thereby enhancing the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP possesses excellent enzymatic hydrolysis resistance and metabolic stability, resists hydrolysis by multiple NTPDase subtypes, and shows no activity against P2Y1 and P2Y12 receptors. 8-BuS-AMP can be used in purinergic signaling pathway and cancer-related studies .
Cat. No.: HY-182047
CAS No.: 2983098-90-2
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PD-1/PD-L1-IN-61 is a PD-1/PD-L1 interaction inhibitor with a human IC50 of 5.3 nM. PD-1/PD-L1-IN-61 embeds into the hydrophobic pocket at the PD-L1 dimer interface, stabilizing binding through hydrogen bonds and π-π stacking with PD-L1 residues. PD-1/PD-L1-IN-61 acts as an immune activator, enhances immune-killing activity of peripheral blood mononuclear cells against cancer cells, restores T-cell immune function, and promotes IFN-γ secretion. PD-1/PD-L1-IN-61 can be used for the research of triple-negative breast cancer .
Cat. No.: HY-184915
CAS No.: 3065495-08-8
Research Areas:
APH003 is an orally active IRAK4 PROTAC degrader with a DC50 of 0.74 nM in human peripheral blood mononuclear cells (hPBMCs). APH003 recruits IRAK4 to CRBN to form a ternary complex, mediates the ubiquitination and degradation of IRAK4 via the ubiquitin-proteasome pathway, and inhibits the kinase activity of IRAK4. APH003 inhibits LPS- or IL-1β/LPS-induced phosphorylation of ERK, JNK and NF-κB. APH003 inhibits the secretion of TNF-α, IL-6, IL-8 and IL-13 by stimulated hPBMCs. APH003 exhibits anti-inflammatory activity in rat TNBS-induced intestinal inflammation models and mouse IL-33-induced skin inflammation models. APH003 can be used in research related to inflammatory bowel disease and skin inflammation .
Cat. No.: HY-188122
CAS No.: 113960-50-2
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Meglumine cyclic adenylate is a cAMP analog. Meglumine cyclic adenylate promotes STAT3 phosphorylation at Ser727 and mitochondrial translocation. Meglumine cyclic adenylate inhibits cell apoptosis by reducing cytochrome c release and caspase-3 activation. Meglumine cyclic adenylate suppresses the expression of NF-κBp65, activates adenylate cyclase 3, and inhibits phosphodiesterase 4D. Meglumine cyclic adenylate enhances myocardial contractility, increases myocardial Ca 2+ influx, dilates peripheral blood vessels, improves hypotension and bradycardia, promotes spinal cord function recovery, and regulates fear extinction and anxiety-like behaviors. Meglumine cyclic adenylate can be used in research related to cerebral ischemia/reperfusion injury, systemic inflammatory response syndrome, acute T4 thoracic spinal cord injury, and post-traumatic stress disorder (PTSD) .
Synonyms: Leurocristine sulfate (Standard); NSC-67574 sulfate (Standard); 22-Oxovincaleukoblastine sulfate (Standard)
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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
