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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
3035 Results for "
modulating
" in MedChemExpress (MCE) Product Catalog:
Products (3035)
3035 Results for "modulating" in MCE Product Catalog:
Cat. No.: HY-117106
CAS No.: 200266-76-8
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PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
Synonyms: PF-06372865; CVL-865
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Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .
Cat. No.: HY-123382
CAS No.: 1695551-19-9
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GSK-1482160 isomer is the isomer of GSK-1482160 (HY-19888). GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
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-129138R
CAS No.: 2611-67-8
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Cat. No.: HY-131997
CAS No.: 89112-85-6
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2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .
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MitoPBN is a AMPK/SIRT3/PGC-1α axis modulator, reactive oxygen species scavenger and mitochondrial function enhancer. MitoPBN increases the phosphorylation level of AMPK, restores SIRT3 expression and reverses the down-regulation of PGC-1α, thereby promoting mitochondrial biogenesis. MitoPBN regulates glucose metabolism, reduces blood glucose by inhibiting hepatic gluconeogenesis and increasing hepatic glucose uptake, while scavenging mitochondrial superoxide anion/hydrogen peroxide, maintaining membrane potential and increasing ATP production. MitoPBN also reduces cell apoptosis, improves sperm motility, survival rate and membrane integrity, but may induce reductive stress in cryopreserved sperm at high concentrations. MitoPBN is widely applicable to research related to diabetes and type 2 diabetes .
Cat. No.: HY-15446R
CAS No.: 802906-73-6
Synonyms: RG7090 (Standard); RO4917523 (Standard)
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Basimglurant (RG7090; RO4917523) (Standard) is the analytical standard of Basimglurant. This product is intended for research and analytical applications. Basimglurant is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [ 3H]-ABP688 (HY-110141)) and 35.6 nM (against [ 3H]-MPEP (HY-14609A)). Basimglurant inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant can be used in research on depression, fragile X syndrome, anxiety disorders, etc.
Cat. No.: HY-159007
CAS No.: 58213-75-5
Synonyms: R,S-1,3-Butanediol acetoacetate diester
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Pyroptosis NF-κB NOD-like Receptor (NLR) Caspase Apoptosis Autophagy Reactive Oxygen Species (ROS) Oxidative Phosphorylation Interleukin Related
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Neurological Disease Metabolic Disease Inflammation/Immunology
BD-AcAc2 (R,S-1,3-Butanediol acetoacetate diester) is an orally active, CNS-penetrant antiepileptic agent. BD-AcAc2 inhibits NF-κB, NLRP3 inflammasome, caspase-1/3, pyroptosis, apoptosis, and enhances autophagy. BD-AcAc2 exhibits antioxidant activity by modulating ROS, MDA, SOD, and GSH levels, and alleviates oxidative stress. BD-AcAc2 mitigates chronic colitis, counteracts Dextran Sodium Sulfate (DSS)-induced pathology, protects against central nervous system oxygen toxicity and acute lung injury, and exhibits anti-seizure efficacy. BD-AcAc2 can be used for the research of colitis, sarcopenia, acute lung injury, seizure, and obesity .
Cat. No.: HY-160550
CAS No.: 3018836-86-4
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DPM-1003 is a modulator of protein tyrosine phosphatase 1B (PTP1B) and C-X-C chemokine receptor 4 (CXCR4). DPM-1003 binds to the non-catalytic disordered C-terminal fragment of PTP1B. DPM-1003 inhibits the PI3Kγ-mediated AKT/mTOR signaling pathway downstream of CXCR4. DPM-1003 improves the survival rate of mice in a transfusion-related acute lung injury model, and exerts a lung injury protective effect in preclinical mouse models of acute lung injury and sepsis. DPM-1003 can be used in research related to acute lung injury, acute respiratory distress syndrome, transfusion-related acute lung injury and sepsis .
Cat. No.: HY-16443
CAS No.: 173534-37-7
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S-4048 is a glucose-6-phosphate translocase modulator and hypoglycemic agent. S-4048 is taken up by hepatocytes via OATP-1 and is rapidly eliminated via the hepatobiliary system in rats. S-4048 blocks glucose-6-phosphate translocase, prevents glucose-6-phosphate from entering the endoplasmic reticulum, and thereby interferes with the glucose-6-phosphatase system (i.e., the final step of hepatic gluconeogenesis and glycogenolysis) to regulate hepatic glucose production. S-4048 completely inhibits glucose production from pyruvate in GLUT2-deficient hepatocytes without affecting the release of cytoplasmic glucose. S-4048 effectively reduces blood glucose levels in rats and has been used in studies related to type 2 diabetes .
Cat. No.: HY-16950AR
CAS No.: 68392-35-8
Synonyms: Afimoxifene (Standard); 4-OHT (Standard)
Cat. No.: HY-170935
SRSF1-IN-1 is a SRSF1 inhibitor. SRSF1-IN-1 inhibits SRSF1 expression, thereby modulating the splicing of Bcl-x pre-mRNA. SRSF1-IN-1 inhibits the proliferation of various cancer cells. SRSF1-IN-1 induces apoptosis in gastric cancer cells, reduces Bcl-xl expression, and upregulates cleaved PARP and caspase 3. SRSF1-IN-1 induces autophagy and promotes cell death. SRSF1-IN-1 exhibits anti-tumor activity in a mouse gastric cancer xenograft model. SRSF1-IN-1 can be used for the research of various cancers including liver cancer, gastric cancer, breast cancer, colon cancer, glioma, and melanoma .
Cat. No.: HY-172736
CAS No.: 3005272-36-3
Synonyms: BMS-986458
Toviblideg (BMS-986458) is a highly selective, orally active cereblon-based BCL6 PROTAC degrader and antitumor agent. Toviblideg selectively degrades BCL6 by binding cereblon to the BTB domain of BCL6, thereby regulating the cell cycle, antiproliferative and interferon signaling pathways, and upregulating the expression and distribution of CD20. Toviblideg modulates the phenotype of follicular helper T cells and reduces circulating tumor DNA levels. The combination of Toviblideg with CD20xCD3 bispecific antibody also enhances the efficiency of T cell tumor infiltration and expansion. Toviblideg induces regression of BCL6-positive tumors and prolongs survival, and it is suitable for research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma .
Cat. No.: HY-173062
CAS No.: 2994635-04-8
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BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, BRD2-BD1 and BRD2-BD2 with IC50s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models .
Cat. No.: HY-173679
CAS No.: 2569517-30-0
RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD + site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections .
Cat. No.: HY-175504
CAS No.: 932544-59-7
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MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .
Cat. No.: HY-178281
CAS No.: 931928-13-1
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E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research .
Cat. No.: HY-179585
DD-CIP2 is a DNA damage and apoptosis inducer. DD-CIP2 demonstrates effective anti-proliferative activity against multiple cancer cell. DD-CIP2 modulates the DNA damage response pathway, triggering robust DNA damage, cell cycle arrest, and apoptosis in vitro. DD-CIP2 demonstrates significant anti-tumor efficacy in vivo at well-tolerated doses, without substantial toxicity. DD-CIP2 exhibits superior cytotoxic potency against a broad panel of blood-and solid-tumor-derived cancer cell lines independent of their BRCA1/2 status. DD-CIP2 can be used for small-cell lung cancer (SCLC) and non small-cell lung cancer (NSCLC) research .
Cat. No.: HY-18102BS
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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
