Search results for: 'trv130 hcl'
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ALK5 inhibitor
TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. -
PDE-KRAS inhibitor
Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling. -
MAO Inhibitor
Bifemelane hydrochloride is an antidepressant MAO inhibitor. Reverses catalepsy induced by tetrabenazine in mice and increases locomotor activity in MPTP-treated marmosets. -
EDG-1 (S1P1) agonist
CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM). -
5-HT4 Receptor Antagonist
SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist. -
norepinephrine reuptake inhibitor
Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor -
FPTase inhibitor
L-778123 HCl is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination. - Prodigiosin (Prodigiosine) HCl is a potent proapoptotic agent, and inhibits Wnt/β-catenin pathway.
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beta-Adrenergic agonist
Ractopamine HCl is a beta-Adrenergic agonist. It acts by being a full agonist at the TAAR1. -
CaSR activator
AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium. -
RTK inhibitor
Anlotinib, also known as AL3818, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. CAS: 1058156-90-3 (free base) 1360460-82-7 (HCl) -
P2X7 receptor antagonist
A-438079 HCl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 >> 10 uM). -
pan-PIM/FLT3 inhibitor
SEL24-B489 HCl is a potent, dual pan-PIM/FLT3 inhibitor. -
nAChR agonist
ABT-418 HCl is a neuronal nicotinic acetylcholine receptor agonist. -
dopamine D2 receptor antagonist
Metoclopramide HCl is a selective dopamine D2 receptor antagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Histamine H1 receptor antagonist
Promethazine HCl is a potent histamine H1 receptor antagonist. -
5-HT2 receptor antagonist
Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations. -
serotonin/NE reuptake inhibitor
Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor. - Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
- Fmoc-L-Lys(Me2)-OH HCl is a modified Lysine used to study histone modifications.
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β-adrenoceptor agonist
Bambuterol HCl is a potent β-adrenoceptor agonist, used in the treatment of asthma. -
LOXL2 inhibitor
LOXL2-IN-1 HCl is a selective LOXL2 inhibitor with an IC50 of 126 nM. -
Voltage-gated sodium channels antagonist
Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM. -
Sodium channel blocker/DNMT inhibitor
Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor. - Demeclocycline HCl is a tetracycline antibiotic via inhibition of protein synthesis by bacteria
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Dopamine receptor antagonist
Alizapride HCl is a dopamine receptor antagonist used for the theropy of nausea and vomiting. -
β2-adrenergic receptor agonist
Clorprenaline HCl is a β2-receptor agonist, it has a significant expansion of the bronchial effect. - 3-methoxy Tyramine (HCl) is a natural metabolite of dopamine, produced by catechol-O-methyltransferase (COMT).
- Hexaminolevulinate HCl is the hexyl ester of 5-aminolevulinic acid (ALA) with photodynamic properties.
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carbonic anhydrase inhibitor
Dorzolamide HCl is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent and topically applied in the form of eye drops. Dorzolamide HCl is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension. -
COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist -
alpha1/beta adrenergic receptors antagonist
Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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nAChR Agonist
Desformylflustrabromine HCl is a positive allosteric modulator of α4β2 and also a muscle-type nAChR inhibitor. - Arzoxifene HCl is the hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist.
- Sumit Bansal, .et al. , J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405 PMID: 30918069
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LXR-like receptors agonist
GW3965 HCl is a selective and orally active liver X receptor (LXR) full agonist.- Mohácsik P, .et al. , Endocrinology, 2018, Feb 1;159(2):1159-1171 PMID: 29253128
- Pencheva N, .et al. , Cell., 2014, 156(5):986-1001 PMID: 24581497
- Bin Dong, .et al. , J Lipid Res., 2013, May; 54(5): 1241-1254 PMID: 23427282
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AChR inhibitor
Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug -
Renin inhibitor
VTP-27999 HCl is a potent inhibitor of renin with IC50 value of 0.3 nM for human renin. -
M2/M3 antagonist
Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02. -
histamine H3 receptors agonist
S38093 is an inverse agonist at histamine H3 receptors. CAS: 862896-30-8 (Free base) 1222097-72-4 (HCl) -
mGlu2 receptor modulator
CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM -
CDK inhibitor
Flavopiridol HCl is an inhibitor of cyclin-dependent kinases. The (-)-cis form induces apoptosis in particular tumor cells. -
Sodium channel blocker
Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative. -
Pan-PIM kinase inhibitor
LGB-321 HCl is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor).- Ricardo de Matos Simoes, .et al. , Nat Cancer, 2023, May;4(5):754-773 PMID: 37237081
- Andrea L. Casillas, .et al. , Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
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Histamine H1 receptor inhibitor
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.