blood disorder

(R)-PF-04822163 is an isomer of PF-04822163. PF-04822163 is an oral, selective PDE1 inhibitor that can cross the blood-brain barrier. PF-04822163 can be used in studies about nervous system disorders such as attention deficit hyperactivity disorder (ADHD) and Parkinson’s disease.

Dextran sulfate sodium salt (MW 4500-5500) is a polymer of dehydrated glucose and an inhibitor of complement and coagulation pathways. Dextran sulfate sodium salt (MW 4500-5500) can be used as an anticoagulant, antiviral agent and antilipidemic agent. Dextran sulfate sodium salt (MW 4500-5500) can prevent the HIV-1 virus from adsorbing onto host cells. Dextran sulfate sodium salt (MW 4500-5500) can inhibit NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 4500-5500) can inhibit the immediate blood-mediated inflammatory response (IBMIR).

4-Hydroxyphenylpyruvic acid is an enzyme inhibitor.4-Hydroxyphenylpyruvic acid (4-HPPA) is a keto acid that is involved in the tyrosine catabolism pathway. It is a product of the enzyme (R)-4-hydroxyphenyllactate dehydrogenase (EC 1.1.1.222) and is formed during tyrosine metabolism. The conversion from tyrosine to 4-HPPA is catalyzed by tyrosine aminotransferase. Additionally, 4-HPPA can be converted to homogentisic acid which is one of the precursors to ochronotic pigment. The enzyme 4-hydroxyphenylpyruvic acid dioxygenase (HPD) catalyzes the reaction that converts 4-hydroxyphenylpyruvic acid to homogentisic acid. A deficiency in the catalytic activity of HPD is known to lead to tyrosinemia type III, an autosomal recessive disorder characterized by elevated levels of blood tyrosine and massive excretion of tyrosine derivatives into urine. It has been shown that hawkinsinuria, an autosomal dominant disorder characterized by the excretion of 'hawkinsin,' may also be a result of HPD deficiency . Moreover, 4-hydroxyphenylpyruvic acid is also found to be associated in phenylketonuria, which is also an inborn error of metabolism. There are two isomers of HPPA, specifically 4HPPA and 3HPPA, of which 4HPPA is the most common.

BPN 0026709（MT-228） is a selective, blood-brain barrier-permeable non-muscle myosin II inhibitor. BPN 0026709 demonstrates enhanced tolerability by preferentially targeting NMIIB (KI = 1.5 μM) over CMII (KI = 17 μM), with SmMll MD sharing 83.6% sequence identity with NMllB. BPN 0026709 exhibits sustained efficacy in animal models of stimulant use disorder.

ZZL-7 is a fast-onset antidepressant agent that disrupts the interaction between neuronal nitric oxide synthase (nNOS) and the serotonin transporter (SERT) in the dorsal raphe nucleus (DRN). It easily crosses the blood-brain barrier and has research value in major depressive disorder (MDD).

EHMT2-IN-1 is a potent EHMT inhibitor used in blood disorder and cancer research, with IC50 values all below 100 nM for EHMT1 peptide, EHMT2 peptide, and cellular EHMT2.

Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatmen

INI-4001, a TLR7 8 agonist, exhibits EC50 values of 1.89 μM and 4.86 μM for TLR7 and TLR8, respectively. This compound induces signal transduction and SEAP production through TLR7 and TLR8. Furthermore, INI-4001 stimulates the production of high-affinity, fentanyl-specific antibodies, effectively preventing fentanyl from crossing the human blood-brain barrier. It serves as an effective adjuvant in anti-fentanyl vaccines for individuals with opioid use disorder (OUD).

Lu AF90103 (Compound 42e) is the methyl ester prodrug of compound 42d, capable of crossing the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1 GluN2B complex, with an efficacy of 24% and an EC50 value of 78 nM. Lu AF90103 plays a significant role in neuropsychiatric disorder research.

Droxidopa (L-DOPS) is an effective orally active norepinephrine precursor capable of crossing the blood-brain barrier. It can increase standing blood pressure, improve symptoms of orthostatic hypotension, and enhance standing ability. Droxidopa is commonly used in studies of neurogenic orthostatic hypotension (nOH) and alternative treatments for attention-deficit/hyperactivity disorder (ADHD).

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes. This product contains a mixture of hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs).

Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes. This product contains a mixture of hydroxy and non-hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs).

Droxidopa (L-DOPS) hydrochloride is a potent, orally active precursor to norepinephrine that elevates standing blood pressure, mitigates orthostatic hypotension symptoms, and enhances standing capability. It holds promise for research in neurogenic orthostatic hypotension (nOH) and alternative attention deficit hyperactivity disorder (ADHD) treatments [1] [2] [3] [4].

UCPH-102 can be used in Alzheimer's disease, amyotrophic lateral sclerosis, chronic pain and obsessive compulsive disorder studies with good blood-brain permeability. UCPH-102 is a highly selective inhibitor of EAAT1 with an IC50 value of 0.43 μM. UCPH-102 also shows a specific anti-proliferative effect on T-ALL cells [1] [2] [3] [4].

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier, with an EC50 of 1.14 nM and a Ki of 0.37 nM. Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM), and can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective MOR antagonist with the ability to penetrate the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). This compound can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 4 (compound 31) is a potent and selective MOR antagonist that permeates the blood-brain barrier (Ki: 0.38 nM, EC50: 0.38 nM) and can be used to study opioid use disorder (OUD).

VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR ( IC 50 =36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) [1] [2] .

SR 142948 dihydrochloride is a selective, orally active, non-peptide neurotensin receptor (NT) antagonist, featuring IC50 values of 1.19 nM, 0.32 nM, and 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. It effectively inhibits NT-induced inositol monophosphate formation in HT-29 cells (IC50 = 3.9 nM) and blocks NT-induced hypothermia, analgesia, and steering behavior in vivo. Furthermore, it demonstrates blood-brain barrier permeability, positioning it as a potential tool for psychiatric disorder research [1] [2].

PKR activator 4 (example 7A), a potent activator of pyruvate kinase R (PKR), holds promise for blood disorder research [1].

Dazukibart is a humanized IgG1κ anti-IFNB1 monoclonal antibody of murine origin, being investigated as a potential treatment for dermatomyositis, a complex autoimmune disorder pathologically characterized by the pronounced overexpression of interferon (IFN) inducible genes present within the blood, skin, and muscle tissue of affected patients.

3β,5α,6β-Trihydroxycholanic acid, a metabolite derived from 5α,6β-dihydroxycholestanol, exhibits elevated levels in dried blood spots of patients diagnosed with Niemann-Pick disease type C, a neurodegenerative disorder characterized by the accumulation of cholesterol and sphingolipids in lysosomes.