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penetration

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171

Inhibitors & Agonists

3

Fluorescent Dye

5

Biochemical Assay Reagents

12

Peptides

2

Inhibitory Antibodies

6

Natural
Products

4

Isotope-Labeled Compounds

2

Click Chemistry

2

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-102032

    Adrenergic Receptor Endocrinology
    Butyryltimolol, an effective precursor of Timolol, improves the corneal penetration of Timolol . Butyryltimolol is a β-adrenergic blocker .
    Butyryltimolol
  • HY-129060
    Flutrimazole
    1 Publications Verification

    Fungal Infection
    Flutrimazole is an imidazole antifungal with dual anti-inflammatory and antifungal activity. Flutrimazole shows scarce transdermal penetration. Flutrimazole has the advantageous in the research of topical fungal infections with an inflammatory component .
    Flutrimazole
  • HY-A0147A

    OPC-17116 hydrochloride; dl-Grepafloxacin hydrochloride

    Antibiotic Bacterial Infection
    Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile .
    Grepafloxacin hydrochloride
  • HY-102032A

    Adrenergic Receptor Others
    (RS)-Butyryltimolol is the racemate of Butyryltimolol. Butyryltimolol, an effective proagent of Timolol, improves the corneal penetration of Timolol . Butyryltimolol is a β-adrenergic blocker .
    (RS)-Butyryltimolol
  • HY-101281

    mAChR Neurological Disease
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .
    VU 6008667
  • HY-101281A

    mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration .
    (Rac)-VU 6008667
  • HY-A0147

    OPC-17116; dl-Grepafloxacin

    Antibiotic Bacterial Infection
    Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile .
    Grepafloxacin
  • HY-147013

    Influenza Virus Orthopoxvirus Infection
    Caprochlorone has antiviral activity against orthopoxvirus. Caprochlorone can inhibit cell penetration by virus, also delays release of newly formed virus from the cell. Caprochlorone decreases the titers of influenza virus in infected-mice lungs .
    Caprochlorone
  • HY-125692

    Cholecystokinin Receptor Metabolic Disease
    L-740093 is a potent cholecystokinin-B receptor antagonist. L-740093 has excellent central nervous system (CNS) penetration .
    L-740093
  • HY-116625

    GHSR Neurological Disease
    PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research .
    PF-04628935
  • HY-138879

    nAChR Neurological Disease
    CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .
    CP-601927
  • HY-129060R

    Fungal Infection
    Flutrimazole (Standard) is the analytical standard of Flutrimazole. This product is intended for research and analytical applications. Flutrimazole is an imidazole antifungal with dual anti-inflammatory and antifungal activity. Flutrimazole shows scarce transdermal penetration. Flutrimazole has the advantageous in the research of topical fungal infections with an inflammatory component .
    Flutrimazole (Standard)
  • HY-139322

    Biochemical Assay Reagents Others
    PEG-8 laurate is a single chain surfactant. PEG-8 laurate reduces the skin barrier, and acts as a penetration enhancer. PEG-8 laurate can be used to synthesize elastic vesicles .
    PEG-8 laurate
  • HY-119063

    Carbonic Anhydrase Others
    L-645151 is a carbonic anhydrase inhibitor with ocular penetration and hypotensive activity. L-645151 lowers the elevated intraocular pressure (IOP) of o-chymotripsinized (o-CT) rabbit eyes. L-645151 is promising for research of an ocular hypotensive agent .
    L-645151
  • HY-P9967

    BIIB037

    Amyloid-β Neurological Disease
    Aducanumab (BIIB037) is a human monoclonal antibody that selectively targets aggregated amyloid-beta (Aβ). Aducanumab shows brain penetration, and can be used for Alzheimer's disease (AD) research .
    Aducanumab
  • HY-144696

    DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .
    Dyrk1A/α-synuclein-IN-2
  • HY-101076

    Phosphatase Metabolic Disease
    L-690488 is a proagent of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. L-690488 has more effective cell penetration than L-690330 .
    L-690488
  • HY-144695

    DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .
    Dyrk1A/α-synuclein-IN-1
  • HY-139300

    HMPL-813

    EGFR Cancer
    Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer . Epitinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Epitinib
  • HY-116016

    L-DOPA ethyl ester; Levodopa ethyl ester

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester), an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .
    Etilevodopa
  • HY-116016A

    L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .
    Etilevodopa hydrochloride
  • HY-111406

    DE-117

    Prostaglandin Receptor Inflammation/Immunology
    Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering agent.
    Omidenepag isopropyl
  • HY-139300A

    HMPL-813 succinate

    EGFR Cancer
    Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Epitinib succinate
  • HY-149065

    α-synuclein Neurological Disease
    D-685, a prodrug of D-520, exhibits higher in vivo anti-Parkinsonian efficacy in a reserpinized Parkinson's disease (PD) animal model than the parent D-520. D-685 reduces accumulation of human α-synuclein (α-syn) protein. D-685 exhibits facile brain penetration .
    D-685
  • HY-120124

    SUVN-G3031

    Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
    Samelisant
  • HY-11044

    Histamine Receptor Neurological Disease Inflammation/Immunology Endocrinology
    PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms . PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
    PF-03654746 Tosylate
  • HY-10096

    GSK-3 Neurological Disease
    TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
    TCS2002
  • HY-145313

    Others Neurological Disease
    TTBK1-IN-2 (compound 29) is a potent Tau-Tubulin kinase (TTBK1) inhibitor with IC50s of 0.24 and 4.22 µM, respectively. TTBK1-IN-2 reveals good brain penetration in vivo and is able to reduce TDP-43 phosphorylation not only in cell cultures but also in the spinal cord of transgenic TDP-43 mice .
    TTBK1-IN-2
  • HY-101855

    Anle138b

    Amyloid-β Neurological Disease
    Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
    Emrusolmin
  • HY-155672

    5-HT Receptor Neurological Disease
    JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
    JPC0323
  • HY-108460

    TRP Channel Neurological Disease
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .
    A-784168
  • HY-12844
    Ro 64-6198
    1 Publications Verification

    Opioid Receptor Neurological Disease
    Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia .
    Ro 64-6198
  • HY-123934

    P-glycoprotein Neurological Disease
    VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
    VU6007477
  • HY-122608

    SUVN-G3031 free base

    Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
    Samelisant free base
  • HY-123410

    Cannabinoid Receptor Cancer
    KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research .
    KM-233
  • HY-144388

    Cholinesterase (ChE) Amyloid-β Neurological Disease
    ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and 1-42 aggregation inhibitor with IC50s of 0.062, 0.767 and 1.227 µM for AChE, BuChE and Aβ1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent .
    ChE/Aβ1-42-IN-1
  • HY-144389

    Cholinesterase (ChE) Amyloid-β Neurological Disease
    hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD) .
    hAChE/Aβ1-42-IN-1
  • HY-14205

    Monoamine Oxidase Neurological Disease
    NW-1772 (methanesulfonate) (compound 22b) is a potent and selective monoamine oxidase (MAO) B inhibitor. NW-1772 has some advantages, such as rapid blood-brain barrier penetration, short-acting and reversible inhibitory activity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. NW-1772 can be used for the research of neurodegenerative diseases .
    NW-1772
  • HY-148825

    iGluR Histamine Receptor Potassium Channel Cytochrome P450 Adrenergic Receptor Metabolic Disease Inflammation/Immunology Cancer
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes .
    NP10679
  • HY-110206

    Cannabinoid Receptor Metabolic Disease
    AM6545 is a peripherally active, cannabinoid receptor antagonist with limited brain penetration. AM6545 binds to CB1 and CB2 receptors with Kis of 1.7 nM and 523 nM, respectively. AM6545 is a neutral antagonist. AM6545 can be used for the research of obesity and its complications .
    AM6545
  • HY-B1747A

    Others Others
    Pyrithione sodium has poor skin penetration.
    Pyrithione sodium
  • HY-147999

    Bacterial Fungal Cytochrome P450 Infection
    GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .
    GlcN-6-P Synthase-IN-1
  • HY-120184

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
    VU0467485
  • HY-115727

    Epigenetic Reader Domain Others
    BET-IN-1 is a potent BET inhibitor that has excellent brain penetration and reasonable metabolic stability.
    BET-IN-1
  • HY-156717

    Others Inflammation/Immunology
    RE-33 is an analgesic compound. RE-33 has blood brain barrier penetration ability .
    RE-33
  • HY-147151

    Others Others
    AMCPy is a potent electron paramagnetic resonance (EPR) brain imaging agent, possessing excellent lipophilicity for blood−brain barrier (BBB) penetration .
    AMCPy
  • HY-117776

    ICMT Cancer
    CAY10677 (compound 15) is a potent ICMT inhibitor that inhibits cancer cell proliferation. CAY10677 has good PAMPA penetration .
    CAY10677
  • HY-130121

    OGA Neurological Disease
    MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (Ki=7.9 nM for hOGA) with excellent CNS penetration .
    MK-8719
  • HY-137207
    MK-28
    5 Publications Verification

    PERK Neurological Disease
    MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice .
    MK-28
  • HY-13011S

    CH5424802-d8; RO5424802-d8; AF802-d8

    Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
    Alectinib-d8

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