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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
238 Results for "
peripheral selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (238)
238 Results for "peripheral selectivity" in MCE Product Catalog:
Art. -Nr.: HY-P991481
Target:
Forschungsgebiete:
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 .
Art. -Nr.: HY-155297
CAS. Nr.: 55248-23-2
Synonyms: FLA-136
Target:
Forschungsgebiete:
Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
Art. -Nr.: HY-179047
CAS. Nr.: 3040320-18-8
Forschungsgebiete:
SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8 +T cells. SMU-L11-R shows potential in colorectal cancer studies .
Art. -Nr.: HY-187618
CAS. Nr.: 1508276-29-6
Target:
Forschungsgebiete:
GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx .GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity .GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses .GRC-17536 exhibits antitussive activity .GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study .GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough .
Art. -Nr.: HY-A0249
CAS. Nr.: 59170-23-9
Synonyms: SOM3355 free base
Forschungsgebiete:
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 .
Art. -Nr.: HY-P11896
CAS. Nr.: 3081054-30-7
Forschungsgebiete:
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 .
Art. -Nr.: HY-P1723A
Synonyms: Neuropeptide Q TFA
Forschungsgebiete:
Art. -Nr.: HY-P5640
CAS. Nr.: 179264-81-4
Art. -Nr.: HY-118917
CAS. Nr.: 297730-05-3
Target:
Forschungsgebiete:
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 .
Art. -Nr.: HY-134092
CAS. Nr.: 131391-65-6
Synonyms: N-Methyl-LTC4
Target:
Forschungsgebiete:
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 .
Art. -Nr.: HY-14977
CAS. Nr.: 840523-39-9
Target:
Forschungsgebiete:
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) .
Art. -Nr.: HY-121186R
CAS. Nr.: 42864-78-8
Synonyms: SOM3355 (Standard)
Bevantolol hydrochloride (Standard) (SOM3355 (Standard)) is the analytical standard of Bevantolol hydrochloride (HY-121186). This product is intended for research and analytical applications. 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 .
Art. -Nr.: HY-121186S
Synonyms: SOM3355-d7
Forschungsgebiete:
Bevantolol-d7 hydrochloride (SOM3355-d7) is the d7-labeled Bevantolol hydrochloride (HY-121186). 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 .
Art. -Nr.: HY-P4764
CAS. Nr.: 819048-44-7
Synonyms: Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2
Target:
Forschungsgebiete:
LY2112688 (Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2) is a synthetic peptide selective melanocortin 4 receptor (MC4R) agonist with a Ki of 0.13 nM for human MC4R and Ki values of 165, 74, and 1713 nM for human MC1R, MC3R, and MC5R, respectively. LY2112688 activates MC4R-mediated cAMP signaling and promotes PYY and GLP-1 release by activating peripheral MC4R in enteroendocrine L cells; Kir7.1 signaling in MC4R neurons is involved in its sustained suppression of food intake. LY2112688 inhibits food intake in vivo and can elevate heart rate and blood pressure. LY2112688 is useful for research on obesity, energy homeostasis, and MC4R signaling .
Art. -Nr.: HY-187014
CAS. Nr.: 141360-03-4
Target:
Forschungsgebiete:
NNC 09-0026 is a neuronal calcium channel inhibitor. NNC 09-0026 exhibits IC50 values of 10 μM and 13 μM against neuronal L-type voltage-gated calcium channels, and an IC50 value of 13 μM against rat neuronal N-type voltage-gated calcium channels, with higher selectivity for neuronal L-type channels over peripheral L-type channels. NNC 09-0026 inhibits voltage-dependent Ca 2+ channel currents, blocks Ca 2+ influx through neuronal L-type and N-type voltage-gated calcium channels, and reduces potassium-stimulated calcium uptake in rat cerebral cortex synaptosomes. NNC 09-0026 inhibits TTX-sensitive Na + channel currents in rat cerebellar Purkinje neurons. NNC 09-0026 attenuates ischemia-induced neuronal death, infarct volume and neurological deficits in rat models of cerebral ischemia. NNC 09-0026 can be used for studies on global cerebral ischemia, focal ischemia and cerebral ischemia-related research .
Art. -Nr.: HY-119820
CAS. Nr.: 135354-02-8
Synonyms: SR57746A free base
Target:
Akt Dopamine Receptor Trk Receptor 5-HT Receptor PKC JNK ERK
Forschungsgebiete:
Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
Art. -Nr.: HY-14604R
CAS. Nr.: 90494-79-4
Synonyms: SR57746A (Standard); SR57746 hydrochloride (Standard)
Forschungsgebiete:
Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
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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
