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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
318 Results for "
Subtype selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (318)
318 Results for "Subtype selectivity" in MCE Product Catalog:
35
35 Publications Verification
Synonyms: BMS-986165
18
Target:
Forschungsgebiete:
Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
18
18 Cited Publications
Target:
13
13 Cited Publications
Art. -Nr.: HY-17015
CAS. Nr.: 1041434-82-5
Synonyms: RWJ 270201 trihydrate; BCX 1812 trihydrate
Forschungsgebiete:
Peramivir trihydrate (RWJ-270201 trihydrate) is a highly potent, selective and orally active influenza virus neuraminidase (NA) inhibitor, with IC50 values ranging from 0.9 to 4.3 nM for nine NA subtypes .
11
11 Cited Publications
Art. -Nr.: HY-18732
CAS. Nr.: 17035-90-4
Synonyms: Tilarginine; Methylarginine
Target:
Forschungsgebiete:
L-NMMA (Tilarginine) is a non-selective and competitive inhibitor of nitric oxide synthase. L-NMMA inhibits three subtypes, namely nNOS, eNOS, and iNOS, and reduces NO production . L-NMMA alleviates mechanical allodynia, thermal hyperalgesia, and choroidal fibrosis. L-NMMA is applicable to research related to nociception, bone cancer pain, and myopia .
11
11 Cited Publications
Art. -Nr.: HY-18732A
CAS. Nr.: 53308-83-1
Synonyms: Tilarginine acetate; Methylarginine acetate
Category:
Cardiovascular Disease Natural Products Endogenous metabolite Disease Research Fields Cancer
Target:
11
11 Cited Publications
Synonyms: Debio 0719
Target:
Forschungsgebiete:
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 .
9
9 Cited Publications
Synonyms: 8-Hydroxy-DPAT hydrobromide
Target:
Forschungsgebiete:
8-OH-DPAT (8-Hydroxy-DPAT) hydrobromide is a potent, brain-penetrant and selective 5-HT1A agonist with a pIC50 of 8.19. 8-OH-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site .
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7 Cited Publications
Forschungsgebiete:
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 .
4
4 Cited Publications
Art. -Nr.: HY-122560
CAS. Nr.: 755002-90-5
Target:
Forschungsgebiete:
VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV .
4
4 Cited Publications
Target:
Forschungsgebiete:
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV .
4
4 Cited Publications
Art. -Nr.: HY-16787
CAS. Nr.: 313254-51-2
Target:
Forschungsgebiete:
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
4
Target:
Forschungsgebiete:
Ozanimod (RPC-1063) is a CNS-penetrant sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
4
4 Cited Publications
Synonyms: RPC-1063 hydrochloride
Target:
Forschungsgebiete:
Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .
3
3 Cited Publications
Synonyms: OPA-15406
Target:
Forschungsgebiete:
Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD) .
3
3 Cited Publications
Target:
Forschungsgebiete:
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 .
3
3 Cited Publications
Target:
Forschungsgebiete:
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor .
3
3 Cited Publications
Art. -Nr.: HY-17416A
CAS. Nr.: 29110-47-2
Target:
Forschungsgebiete:
Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
3
3 Cited Publications
Art. -Nr.: HY-17416
CAS. Nr.: 29110-48-3
Target:
Forschungsgebiete:
Cardiovascular Disease Infection Neurological Disease Metabolic Disease
Guanfacine hydrochloride is an orally active and blood-brain barrier permeability noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
2
Category:
Alkaloids Neurological Disease Other Alkaloids Anisodus tanguticus (Maxinowicz) Pascher Plants Solanaceae Disease Research Fields
Target:
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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
