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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
30 Results for "
Non-peptide blockers
" in MedChemExpress (MCE) Product Catalog:
Products (30)
30 Results for "Non-peptide blockers" in MCE Product Catalog:
7
7 Publications Verification
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Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome .
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7 Publications Verification
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LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
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7 Publications Verification
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LM11A-31, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
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6 Cited Publications
Cat. No.: HY-50688
CAS No.: 211096-49-0
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SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively .
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Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities .
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1 Cited Publications
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SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
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1 Cited Publications
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Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities .
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1 Cited Publications
Cat. No.: HY-107664A
Purity: 98.6%
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SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
Cat. No.: HY-19307
CAS No.: 205678-31-5
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Cardiovascular Disease Inflammation/Immunology Endocrinology Cancer
SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with Ki values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. .
Cat. No.: HY-N2600
CAS No.: 76472-87-2
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CP 339818 hydrochloride is a non-peptide Kv1.3 channel (IC50 = 200 nM) and Kv1.4 channel blocker. CP 339818 hydrochloride inhibits HCN channel with IC50s of 18.9 μM and 43.4 μM against HCN1 and HCN4 (high Cl -). CP 339818 hydrochloride has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels. CP 339818 hydrochloride selectively blocked Kv1.3, thereby inhibiting the activation process of human T cells. CP 339818 hydrochloride can be used to study the physiological functions of HCN and Kv channels .
Cat. No.: HY-19732
CAS No.: 133085-33-3
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BIBS 39 is a non-peptide angiotensin II receptor antagonist with antihypertensive activity, with higher affinity for the AT1 receptor than for the AT2 receptor. BIBS 39 competitively blocks AT1-mediated vasoconstriction and pressor responses, and effectively inhibits the activity of the renin-angiotensin-aldosterone system. BIBS 39 reduces diastolic blood pressure and induces mild, transient reflex tachycardia, with no off-target functional activity on the norepinephrine, K +/Cl − or vasopressin pathways. BIBS 39 can be used in research related to hypertension and renal hypertension [1][2 ][3].
Cat. No.: HY-108479
CAS No.: 153050-21-6
Synonyms: SR140333
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Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
Cat. No.: HY-19374
CAS No.: 202855-56-9
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BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC50 value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .
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NS-638 is a small nonpeptide molecule with Ca 2+-channel blocking properties. K +-stimulated intracellular Ca 2+-elevation is blocked with an IC50 value of 3.4 μM.
Cat. No.: HY-107664B
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SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders .
Cat. No.: HY-10382
CAS No.: 114773-44-3
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EXP-6803 is a specific nonpeptide angiotensin II receptor antagonist with antihypertensive activity. EXP-6803 inhibits the contractile response to angiotensin II with a pA2 value of 7.20. EXP-6803 effectively blocks responses to angiotensin I and II while not affecting responses to bradykinin or acetylcholine in guinea pig ileum. EXP-6803 can be used for hypertension research .
Cat. No.: HY-120308
CAS No.: 154728-59-3
Synonyms: SR140603
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(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
Cat. No.: HY-113730
CAS No.: 860002-95-5
VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
Cat. No.: HY-17012
CAS No.: 153438-49-4
Synonyms: RPR 100893
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Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the human NK1 receptor. It belongs to the 7,7,4-trimethylperhydroisoindole class of compounds. Dapitant inhibits the binding of Substance P to NK1 receptors, thereby blocking its neurokinin-mediated effects. This novel antagonist represents a potential therapeutic option for conditions involving Substance P, such as neurogenic inflammation and pain modulation .
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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
