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Blood-Brain Barrier (BBB) Penetration

" in MedChemExpress (MCE) Product Catalog:

13

Inhibitors & Agonists

1

Peptides

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108625
    SHA 68
    1 Publications Verification

    		 Neuropeptide S Receptor Neurological Disease
    SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
    SHA 68
  • HY-P11195
    Angiopep-2 azide

    		Drug Derivative Neurological Disease
    Angiopep-2 azide is a peptide derivative of Angiopep-2 bearing a side chain azide (N3) group. Angiopep-2 exhibits high blood-brain barrier (BBB) penetration capability and can be used for brain drug delivery .
    Angiopep-2 azide
  • HY-147151
    AMCPy

    		Biochemical Assay Reagents Others
    AMCPy is a potent electron paramagnetic resonance (EPR) brain imaging agent, possessing excellent lipophilicity for blood brain barrier (BBB) penetration .
    AMCPy
  • HY-164512
    NRMA-I

    		Drug Intermediate Neurological Disease
    NRMA-I is the amide produrg of the small molecule nuclear receptor modulator. NRMA-I exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-I can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .
    NRMA-I
  • HY-114320
    BuChE-IN-TM-10

    TM-10

    		 Cholinesterase (ChE) Neurological Disease
    BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease .
    BuChE-IN-TM-10
  • HY-164505
    NRMA-9

    		Drug Intermediate Neurological Disease
    NRMA-9 is the amide produrg of the small molecule nuclear receptor modulator. NRMA-9 exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-9 can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .
    NRMA-9
  • HY-143413
    BuChE-IN-2

    		Amyloid-β Neurological Disease Inflammation/Immunology
    BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu 2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease .
    BuChE-IN-2
  • HY-N4190
    Britannilactone diacetate

    1,6-O,O-Diacetylbritannilactone; Di-O-acetylbritannilactone

    		 NO Synthase Neurological Disease Inflammation/Immunology
    Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC50 value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property .
    Britannilactone diacetate
  • HY-108625R
    SHA 68 (Standard)

    		Neuropeptide S Receptor Neurological Disease
    SHA 68 (Standard) is the analytical standard of SHA 68. This product is intended for research and analytical applications. SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
    SHA 68 (Standard)
  • HY-168241
    Flucopride

    		Cholinesterase (ChE) 5-HT Receptor Infection
    Flucopride (Compound 4a) is an AChE inhibitor (IC50: 24 nM), and a partial 5-HT4R agonist (Ki: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT4R (EC50: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay) .
    Flucopride
  • HY-175670
    GABAA receptor modulator-10

    		GABA Receptor Neurological Disease
    GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .
    GABAA receptor modulator-10
  • HY-178964
    PROTAC RET Degrader 1

    		PROTACs RET Cancer
    PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .
    PROTAC RET Degrader 1
  • HY-175675
    P2Y1 antagonist 4

    		P2Y Receptor Keap1-Nrf2 Cardiovascular Disease Neurological Disease
    P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca 2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction .
    P2Y1 antagonist 4

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