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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
132 Results for "
α5
" in MedChemExpress (MCE) Product Catalog:
Products (132)
132 Results for "α5" in MCE Product Catalog:
74
Target:
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Cilengitide (EMD 121974) is a BBB-permeable integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers .
11
11 Cited Publications
Synonyms: ATN-161 TFA salt
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
11
11 Cited Publications
Cat. No.: HY-13535
CAS No.: 262438-43-7
Research Areas:
Cardiovascular Disease Infection Neurological Disease Cancer
ATN-161 is an antagonist of α5β1 integrin and αvβ3 integrin, as well as an inhibitor of fibrosis, an inhibitor of oxidative stress, a tight junction stabilizer, a mitochondrial integrity protector, an angiogenesis inhibitor and an antiviral agent. ATN-161 inhibits NLRP3, MAPK, and ROS. ATN-161 protects mice from SARS-CoV-2 infection . ATN-161 reduces infarct volume, alleviates edema, decreases immune cell infiltration, reduces the area of choroidal neovascularization lesions, lowers tumor microvessel density and viral load. ATN-161 can be used in research related to ischemic stroke, choroidal neovascularization, breast cancer, coronavirus disease 2019 (COVID-19), and liver metastasis of colorectal cancer [5].
9
9 Cited Publications
Cat. No.: HY-P1740
CAS No.: 114681-65-1
Research Areas:
9
9 Cited Publications
Cat. No.: HY-P1740A
Research Areas:
7
Target:
Research Areas:
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively .
6
6 Cited Publications
Synonyms: Ro 13-7410; Arotinoid acid; AGN191183
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
5
Target:
Research Areas:
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a molecular glue that induces the targeted degradation of splicing factor RBM39 by recruiting the E3 ubiquitin ligase CUL4-RBX1-DDB1-DCAF15 (CRL4 DCAF15). E7820 is an angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. E7820 can be used for the study of acute myeloid leukemia (AML) .
4
4 Cited Publications
Target:
Research Areas:
L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
3
2
Target:
Research Areas:
2
Target:
Research Areas:
Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
2
2 Cited Publications
Synonyms: S44819; Egis-13529
Target:
Research Areas:
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
2
2 Cited Publications
Target:
Research Areas:
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
1
Target:
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Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
1
1 Cited Publications
Synonyms: Lu 02-030 hydrochloride; THIP hydrochloride
Target:
Research Areas:
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
1
1 Cited Publications
Cat. No.: HY-P77718
Purity: ≥ 95%, as determined by reducing SDS-PAGE or Bis-Tris PAGE.
Synonyms: ITGA5; Integrin Alpha-F; Prev. FNRA; CDNA FLJ50382, Moderately Similar To Integrin Alpha-5; CD49e; Very Late Activation Protein 5, Alpha Subunit; Integrin, Alpha 5 (Fibronectin Receptor, Alpha Polypeptide); Fibronectin Receptor, Alpha Subunit; Fibronectin
1
1 Cited Publications
Cat. No.: HY-P70845A
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: MOG; MOG Alpha-5; Myelin Oligodendrocyte Glycoprotein; MOG AluA; Myelin-Oligodendrocyte Glycoprotein; MOG AluB; BTNL11; MOGIG2; BTN6; NRCLP7; MOG Ig-AluB
Target:
Research Areas:
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
Synonyms: PF-06372865; CVL-865
Target:
Research Areas:
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 .
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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
