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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
116 Results for "
ER blockade
" in MedChemExpress (MCE) Product Catalog:
Products (116)
116 Results for "ER blockade" in MCE Product Catalog:
Cat. No.: HY-182372
CAS No.: 1638153-78-2
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SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
Cat. No.: HY-188081
CAS No.: 3112733-78-2
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YH-36400 is an orally bioavailable inhibitor of HIF-1α and HIF-2α. YH-36400 disrupts the dimerization of HIF-1α and HIF-1β and triggers proteasomal degradation, thereby inhibiting the transcriptional activities of HIF-1 and HIF-2. YH-36400 reduces the expression of PD-L1 and CD73, reprograms the tumor immune microenvironment, inhibits angiogenesis, and can be used in combination with immune checkpoint blockade therapy. YH-36400 is applicable to research related to breast cancer, lung cancer, melanoma, pancreatic cancer, colorectal cancer, prostate cancer, and head and neck squamous cell carcinoma .
Cat. No.: HY-B0653AS
Synonyms: (S)-(–)-Bupivacaie-d9hydrochloride
Cat. No.: HY-P991740
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Cat. No.: HY-12502B
CAS No.: 111011-53-1
Synonyms: NZ-105 hydrochloride; (±)-Efonidipine hydrochloride
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Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Cat. No.: HY-169232
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Cat. No.: HY-P992353
Cat. No.: HY-P99916
CAS No.: 2449199-61-3
Synonyms: AMG-427
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Cat. No.: HY-108482
CAS No.: 132746-60-2
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Cardiovascular Disease Neurological Disease Inflammation/Immunology
CP-96,345 is a non-peptide selective NK-1 receptor antagonist (Ki = 0.31 nM). CP-96,345 inhibits cell rolling, adhesion, and plasma extravasation, and inhibits degranulation and pancreatic MPO activity. CP-96,345 attenuates neurogenic inflammation, edema, and adhesion molecule expression. CP-96,345 attenuates static contraction- and muscle stretch-evoked pressor reflexes through blockade of NK-1 receptors in the dorsal horn. CP-96,345 impairs post-ischemic recovery of LVDevP, HR, and CF in isolated hearts and increases reperfusion fibrillation. CP-96,345 can be used for research on chronic colitis, myocardial ischemia-reperfusion injury, smoke inhalation and burn injury, acute pancreatitis, oxazolone colitis, and neurogenic inflammation .
Cat. No.: HY-184119
CAS No.: 3061276-55-6
Synonyms: IM502
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Pabgraminone C (IM502) is a Fungal metabolite and PI3Kγ inhibitor with an IC50 of 61.7 nM against PI3Kγ. Pabgraminone C shifts the STAT signaling pathway in cells from an immunosuppressive STAT3/STAT6-dominant profile to an immunostimulatory STAT1/STAT2-dominant profile, driving cells toward a pro-inflammatory phenotype. Pabgraminone C reprograms cells from an immunosuppressive state to an immunostimulatory state, reversing their suppressive effect on anti-tumor immunity. Pabgraminone C inhibits established tumor growth and metastasis across multiple cancer types. Pabgraminone C overcomes resistance to PD-1 checkpoint blockade strategies. Pabgraminone C can be used in research related to liver cancer, melanoma, and colorectal cancer .
Cat. No.: HY-P991193
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LYP-IN-3 is a selective, orally active and reversible lymphoid-tyrosine phosphatase (LYP) inhibitor (IC50 = 2.55 μM, Ki = 0.93 μM). D34 exhibits high selectivity of PTP1B, PTPN12, PTPN5 and SSH2. LYP-IN-3 regulates the T-cell receptor (TCR) signaling by specifically inhibiting LYP. LYP-IN-3 does not significantly inhibit MC38 cell viability; its anti-tumor effect stems from immune regulation. LYP-IN-3 can significantly upregulate PD-L1 or PD-1 expression in different immune cells. LYP-IN-3 facilitates T-cell infiltration and enhances T-cell functions. LYP-IN-3 synergizes with PD-L1 blockade can significantly improve colorectal tumor regression. LYP-IN-3 can be used for the study of colorectal cancer .
Cat. No.: HY-189235
CAS No.: 3078735-55-1
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IHCH-8110 is a peripherally restricted, non-brain-penetrant 5-HT2AR and 5-HT2CR agonist (Ki=47.86 nM) that antagonizes 5-HT2BR. IHCH-8110 induces CXCL10 and IL-18 expression by activating 5-HT2AR on enteric glial cells, thereby promoting CD8 + T cell recruitment and effector polarization, and avoids the risk of cardiac valvulopathy associated with 5-HT2BR activation. IHCH-8110 exhibits a low risk of hERG channel inhibition (IC50=5.96 μM) and is well tolerated, sensitizing immunologically cold colorectal cancer to PD-1 blockade therapy, making it suitable for research related to colorectal cancer .
Cat. No.: HY-12502AR
CAS No.: 111011-76-8
Synonyms: NZ-105 hydrochloride monoethanolate (Standard); (±)-Efonidipine hydrochloride monoethanolate (Standard)
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Efonidipine (NZ-105) hydrochloride monoethanolate (Standard) is the analytical standard of Efonidipine hydrochloride monoethanolate (HY-12502AR). This product is intended for research and analytical applications. Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Synonyms: 5,6-EET; (±)5,6-EpETrE
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5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
Cat. No.: HY-P990955
CAS No.: 2839652-75-2
Synonyms: ADX-097
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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
