Neurological Disease

FUB 349 (Compound 8) is a selective Aromatase inhibitor with an IC₅₀ of 12  μM. FUB 349 is also a H3 receptor antagonist with K_is of 12 and 2.1 nM for rH3R and hH3R, respectively. FUB 349 can be used for neurological diseases such as cognitive impairment research.

Indisetron dihydrochloride is a 5-HT3 receptor antagonist with anti-emetic activity.

ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a K_i of 0.21 nM.

FKBP51-Hsp90-IN-1 (Compound D10) is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, with an IC₅₀ value of 0.1 μM against FKBP51. FKBP51-Hsp90-IN-1 can be used in the research of stress-related diseases, Alzheimer's disease, and metabolic disorders.

Nav1.8-IN-15 (compound 6) is a potent Nav1.8 inhibitor. Nav1.8-IN-15 shows analgesic effect. Nav1.8-IN-15 has the potential for the research of chronic pain.

PACAP (1-38), human, ovine, rat-¹³C₅,¹⁵N (Pituitary Adenylate Cyclase Activating Polypeptide 38-¹³C₅,¹⁵N) TFA is the ¹³C, ¹⁵N-labeled PACAP (1-38), human, ovine, rat (TFA) (HY-P0221A). PACAP (1-38), human, ovine, rat TFA is a PAC₁ receptor agonist. PACAP (1-38), human, ovine, rat TFA binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC₅₀s of 4 nM, 2 nM, and 1 nM, respectively. PACAP (1-38), human, ovine, rat TFA increases the α-secretase activity. PACAP (1-38), human, ovine, rat TFA elevates cytosolic Ca²⁺, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP (1-38), human, ovine, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP (1-38), human, ovine, rat TFA can be used for neurotrophic and neuroprotective research.

THK-5105, an arylquinoline derivative, displays high binding affinity to tau fibrils. THK-5105 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD)  brain homogenates. 18F-THK-5105 has the potential to act as a tau imaging PET probe.

N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function.

Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation.

Adipiplon (NG2-73) is a selective GABA_A receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.

Fasciculin-I is isolated from the mambas venom. Fasciculin-I exerts its toxic effects by inhibiting acetylcholinesterase (AChE). Fasciculin-I blocks α-neurotoxins of nicotinic acetylcholine receptors and cardiac toxins that interact with cell membranes .

Uncarine F (Speciofiline) is a pentacyclic oxindole alkaloid found in Uncaria tomentosa. Uncaria alkaloids have wide medicinal properties, including neuroprotective, anticancer, and antihypertensive activities. Uncaria alkaloids may stimulate the immune system, relax smooth muscles, dilate blood vessels, and act as a diuretic. Uncarine F can be used for the researches of cancer, immunology, cardiovascular and neurological disease.

NLRP3-IN-63 (Compound 7) is an inhibitor for NLRP3, that inhibits the NLRP3 activation with an EC₅₀ of 13 nM.

(S)-Baclofen hydrochloride is a GABAB receptor agonist that crosses the blood-brain barrier and is orally active, with IC₅₀ values ​​of 1.77 μM for GABAB and 1564 μM for GABAA. (S)-Baclofen hydrochloride can be used in research on muscle disorders such as spasticity.

4-Methyl-2-(1-piperidinyl)-quinoline-d₁₀ is the deuterium labeled ML204 (HY-12949). ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels.

Benserazide-d₃ (hydrochloride) is the deuterium labeled Benserazide hydrochloride (HY-B0404A). Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma.

Deschloro W-19 (hydrochloride) is an analytical reference standard with structural similarity to known analgesics.

Pleurotus eryngii extract is an extract from king oyster mushroom (Pleurotus eryngii) that can be used in research on neurological diseases such as dementia, Alzheimer's disease, and Parkinson's disease.

Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor.

Ishophloroglucin A is an orally active phlorotannin compound found in Ishige okamurae. Ishophloroglucin A can alleviate Dexamethasone (HY-14648)-induced muscle atrophy through muscle protein metabolism. Ishophloroglucin A can improve impaired protein synthesis (PI3K and Akt) or degradation (muscle-specific ubiquitin ligase muscle RING finger and atrogin-1). Ishophloroglucin A can be used for research of muscle atrophy-related diseases.