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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
78 Results for "
subtype-selective
" in MedChemExpress (MCE) Product Catalog:
Products (78)
78 Results for "subtype-selective" in MCE Product Catalog:
11
11 Publications Verification
Synonyms: Debio 0719
Target:
Research Areas:
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
7
7 Cited Publications
Research Areas:
A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
3
3 Cited Publications
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NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .
2
Category:
Alkaloids Neurological Disease Other Alkaloids Anisodus tanguticus (Maxinowicz) Pascher Plants Solanaceae Disease Research Fields
Target:
2
2 Cited Publications
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LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor
positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM) .
2
2 Cited Publications
Cat. No.: HY-N0584A
CAS No.: 55449-49-5
Synonyms: 6-Hydroxyhyoscyamine hydrobromide
Category:
Alkaloids Pyrrole Alkaloids Anisodus tanguticus (Maxinowicz) Pascher Plants Solanaceae Disease Research Fields Inflammation/Immunology
Target:
1
1 Cited Publications
Target:
Research Areas:
(S)-SNAP5114 is a non-covalent murine GABA transporter inhibitor with blood-brain barrier penetration ability, which exhibits significant subtype-selective inhibitory activity against mGAT4 (pIC50=5.71, pKi=4.56), much higher than its effects on mGAT1, mGAT2 and mGAT3. (S)-SNAP5114 elevates extracellular GABA concentrations by blocking the GABA reuptake mechanism, thereby enhancing thalamus-specific GABAergic signaling and exerting potential neuromodulatory effects. (S)-SNAP5114 is widely used in studies related to epilepsy, neuropathic pain, anxiety and depression, and various neurodegenerative diseases .
1
1 Cited Publications
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Research Areas:
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
1
1 Cited Publications
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GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity .
Cat. No.: HY-165559
CAS No.: 2019994-90-0
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Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC50s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively. Trpvicin exhibits minimal effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1 and TRPM8). Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state via VSLD-PD binding. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel symmetry and block the channel. Trpvicin inhibits itch and hair loss in mouse models. Trpvicin can be used for study of inflammation and immunology .
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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TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.
Research Areas:
PROTAC TYK2 degrader-2 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degrader-2 has TYK2 degradation activity with DC50 value of 14 nM. PROTAC TYK2 degrader-2 can be used for the research of autoimmune disease .
Synonyms: (-)-Willardiine
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Research Areas:
(S)-Willardiine ((-)-Willardiine) is a subtype-selective glutamate receptor agonist and the active isomer of Willardiine. Willardiine binds to and activates hGluR1, hGluR2, hGluR4 and hGluR5, with Ki values of 3.6 nM and 0.24 nM for hGluR4 and hGluR5, respectively. (S)-Willardiine is used to investigate the distribution and physiological functions of glutamate receptor subunits in the central nervous system .
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GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
Cat. No.: HY-18060
CAS No.: 639489-84-2
Synonyms: TC-5619
Target:
Research Areas:
Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
Synonyms: MRK-409
Target:
Research Areas:
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .
Cat. No.: HY-175728
Research Areas:
VU6032735 is a potent and subtype-selective sperm-specific potassium channel 3 (SLO3) inhibitor with IC50 values of 165 nM (hSLO3) and 730 nM (mSLO3). VU6032735 also inhibits sodium channel and L-type calcium channel VU6032735 can sustain high tissue exposure in the fertilized oviduct. VU6032735 can be used for the research of contraception .
Target:
Research Areas:
L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions
Cat. No.: HY-161169A
CAS No.: 2865106-78-9
TP0628103 TFA is a potent and highly selective MMP-7 inhibitor with an IC50 of 0.17 nM. TP0628103 TFA undergoes structural optimization via molecular isoelectric point shifting, which reduces organic anion transporter (OAT)-mediated clearance, while maintaining potent MMP-7 inhibitory activity and enhancing MMP subtype selectivity. TP0628103 TFA is applicable for research on the regulatory mechanisms of MMP-7-related matrix metalloproteinases .
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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
