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brain penetration

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143

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4

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13318
    Oseltamivir acid
    Maximum Cited Publications
    75 Publications Verification

    GS 4071; Ro 64-0802; Oseltamivir carboxylate

    		 Influenza Virus Drug Metabolite Infection Neurological Disease
    Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .
    Oseltamivir acid
  • HY-B0250
    Lamivudine
    15+ Cited Publications

    BCH-189

    		 HIV Reverse Transcriptase HBV Infection Cancer
    Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
    Lamivudine
  • HY-100788
    2-PMPA
    5 Publications Verification

    2-(Phosphonomethyl)pentanedioic acid

    		 Carboxypeptidase Neurological Disease
    2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA is applicable to the research of neurological diseases .
    2-PMPA
  • HY-101855
    Emrusolmin

    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-115340
    Decanoic acid sodium
    4 Publications Verification

    Sodium decanoate; Sodium caprate

    		 Biochemical Assay Reagents Others
    Decanoic acid sodium, also known as Decanoic acid sodium, is a salt of the fatty acid capric acid. It is easily soluble in water and has a slightly soapy smell. Decanoic acid sodium acts as a penetration enhancer, which means it increases the absorption and bioavailability of drugs across biological membranes, including the intestinal epithelium and the blood-brain barrier. This property makes it useful in pharmaceutical formulations to improve drug delivery and effectiveness. Furthermore, Decanoic acid sodium has potential applications in food preservatives and cosmetics due to its antibacterial properties.
    Decanoic acid sodium
  • HY-P9967
    Aducanumab

    BIIB037

    		 Amyloid-β Neurological Disease
    Aducanumab (BIIB037) is a human monoclonal antibody that selectively targets aggregated amyloid-beta (Aβ). Aducanumab shows blood-brain-barrier penetration, and can be used for Alzheimer's disease (AD) research .
    Aducanumab
  • HY-12599
    URMC-099
    5+ Cited Publications

    		 Mixed Lineage Kinase Autophagy Neurological Disease Cancer
    URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
    URMC-099
  • HY-108463
    A-967079
    15+ Cited Publications

    		 TRP Channel Neurological Disease Inflammation/Immunology
    A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the blood-brain barrier .
    A-967079
  • HY-148811
    Zurletrectinib

    ICP-723

    		 c-Met/HGFR Trk Receptor Cancer
    Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC50 = 0.81 nM; TRKB IC50 = 0.145 nM; TRKC IC50 = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma .
    Zurletrectinib
  • HY-12624
    Narazaciclib
    2 Publications Verification

    ON123300

    		 CDK AMPK PDGFR Cancer
    Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
    Narazaciclib
  • HY-175715
    NRG1271

    		Mitochondrial Metabolism Neurological Disease
    NRG1271 is an orally active mitochondrial permeability transition pore (mPTP) inhibitor with blood-brain barrier penetration. NRG1271 can be used for the study of Neurological Disease .
    NRG1271
  • HY-17037
    Pirenzepine dihydrochloride
    5 Publications Verification

    LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride

    		 mAChR Metabolic Disease Cancer
    Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
    Pirenzepine dihydrochloride
  • HY-100788C
    2-PMPA sodium
    5 Publications Verification

    2-(Phosphonomethyl)pentanedioic acid sodium

    		 Carboxypeptidase Neurological Disease
    2-PMPA (2-(Phosphonomethyl)pentanedioic acid) sodium is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA sodium shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA sodium is applicable to the research of neurological diseases .
    2-PMPA sodium
  • 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-17037A
    Pirenzepine
    5 Publications Verification

    LS 519 free base; Pirenzepin; Gastrozepin

    		 mAChR Metabolic Disease Cancer
    Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
    Pirenzepine
  • HY-120619
    BMS-193885
    1 Publications Verification

    		 Neuropeptide Y Receptor Neurological Disease Endocrinology
    BMS-193885 is a selective neuropeptide Y1 receptor antagonist (Ki=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases .
    BMS-193885
  • 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-127106
    VU0810464
    1 Publications Verification

    		 Potassium Channel Neurological Disease
    VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration .
    VU0810464
  • HY-116578
    Metopimazine
    3 Publications Verification

    EXP999; RP9965

    		 Dopamine Receptor Neurological Disease
    Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
    Metopimazine
  • HY-164782
    PT3

    		HDAC Neurological Disease Metabolic Disease Cancer
    PT3 is a selective inhibitor of HDAC3 with an IC50 value of 0.25 μM. PT3 exhibits good brain penetration ability and bioavailability upon oral administration. PT3 can be used in the research of Alzheimer’s disease .
    PT3
  • HY-100238
    Antihistamine-1

    		Histamine Receptor Cytochrome P450 Potassium Channel Neurological Disease Endocrinology
    Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
    Antihistamine-1
  • HY-11044
    PF-03654746 Tosylate

    		Histamine Receptor Neurological Disease Metabolic Disease Inflammation/Immunology
    PF-03654746 Tosylate is a potent, selective and brain-penetrant histamine H3 receptor antagonist. 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-120124
    Samelisant

    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-145313
    TTBK1-IN-2

    		Tau Protein 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-148825
    NP10679

    		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-108340
    PF-06767832

    		mAChR Neurological Disease
    PF-06767832 is a potent muscarinic M1 selective positive allosteric modulator (PAM), with the EC50 of 60 nM. PF-06767832 has good brain penetration .
    PF-06767832
  • HY-P11195
    Angiopep-2 azide

    		Drug Derivative Neurological Disease
    Angiopep-2 azide is a peptide derivative of Angiopep-2 (HY-P2341) bearing a side chain azide (N3) group. Angiopep-2 exhibits high blood-brain barrier (BBB) penetration capability and can be used for brain compound delivery .
    Angiopep-2 azide
  • HY-N4134
    Ciwujianoside C3

    		NO Synthase Inflammation/Immunology
    Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory .
    Ciwujianoside C3
  • HY-14325
    L-745870
    3 Publications Verification

    		 Dopamine Receptor Neurological Disease
    L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
    L-745870
  • HY-14325B
    L-745870 hydrochloride
    3 Publications Verification

    		 Dopamine Receptor Neurological Disease
    L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
    L-745870 hydrochloride
  • HY-128865
    BPR1M97

    		Opioid Receptor Neurological Disease
    BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects .
    BPR1M97
  • HY-101834
    ACT-462206

    		Orexin Receptor (OX Receptor) Others
    ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .
    ACT-462206
  • HY-116625
    PF-04628935

    		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-N12614
    Diorcinol

    		SHP1 Phosphatase Metabolic Disease
    Diorcinol is a potent SHP1 inhibitor with an IC50 value of 0.96 μM. Diorcinol can be isolated from Aspergillus sydowii. Diorcinol has good blood-brain barrier penetration and can be used for diabetes research .
    Diorcinol
  • HY-167876
    PQR514

    		PI3K Cancer
    PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors .
    PQR514
  • HY-118363
    Lu AE51090

    		mAChR Neurological Disease
    Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS) .
    Lu AE51090
  • HY-W278021
    BTA-1

    		Amyloid-β Others
    BTA-1 is an uncharged derivative of thioflavin-T. BTA-1 has a high affinity for Aβ fibrils and shows very good brain penetration and clearance .
    BTA-1
  • HY-139300A
    Epitinib succinate

    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-155672
    JPC0323

    		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-105860
    Selurampanel

    BGG 492

    		 iGluR Neurological Disease
    Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research .
    Selurampanel
  • HY-10104
    GRL-8234

    		Beta-secretase Neurological Disease
    GRL-8234 is a potent β-secretase (BACE1) inhibitor with blood-brain barrier penetration (Ki = 1.8 nM). GRL-8234 can rescue age-related cognitive decline in Tg2576 mice. GRL-8234 can be used in the research related to Alzheimer's disease (AD) .
    GRL-8234
  • HY-100788R
    2-PMPA (Standard)

    2-(Phosphonomethyl)pentanedioic acid (Standard)

    		 Reference Standards Carboxypeptidase Neurological Disease
    2-PMPA (2-(Phosphonomethyl)pentanedioic acid) Standard is the analytical standard of 2-PMPA (HY-100788). This product is intended for research and analytical applications. 2-PMPA (2-(Phosphonomethyl)pentanedioic acid) sodium is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA sodium shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA sodium is applicable to the research of neurological diseases.
    2-PMPA (Standard)
  • HY-102043
    PDM-631

    		Phosphodiesterase (PDE) Neurological Disease
    PDM-631 is a selective and orally active PDE2A inhibitor with blood-brain barrier penetration. PDM-631 exhibits potent inhibitory activity against human and rat recombinant PDE2A with IC50 values of 1.5 nM and 4.2 nM, respectively. PDM-631 increases cGMP levels in the rat cerebral cortex. PDM-631 can be used for the study of schizophrenia and neurodegenerative disorders .
    PDM-631
  • HY-123410
    KM-233

    		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-156717
    RE-33

    		Drug Isomer Inflammation/Immunology
    RE-33 is an analgesic compound. RE-33 has blood brain barrier penetration ability .
    RE-33
  • HY-167927
    Mefuparib

    CVL218

    		 PARP Cancer
    Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
    Mefuparib
  • HY-10550B
    Tariquidar dimesylate

    XR9576 dimesylate

    		 P-glycoprotein Cardiovascular Disease Others
    Tariquidar dimesylate (XR9576 dimesylate) is a P-glycoprotein (P-gp) inhibitor. Tariquidar dimesylate increases the concentration of the drug in the brain by binding to P-glycoprotein, preventing it from transporting the drug from inside to outside the brain. Tariquidar dimesylate can be used in the study of blood-brain barrier penetration and multidrug resistance .
    Tariquidar dimesylate
  • HY-15112
    JTP-4819

    		Prolyl Endopeptidase (PREP) Infection
    JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096) .
    JTP-4819
  • HY-14325R
    L-745870 (Standard)

    		Dopamine Receptor Neurological Disease
    L-745870 (Standard) is the analytical standard of L-745870. This product is intended for research and analytical applications. L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
    L-745870 (Standard)
  • HY-163825
    RNB-61

    		Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    RNB-61 is an oral active agonist of cannabinoid CB2 receptor (CB2R), with the Ki ranging from 0.13 nM to 1.81 nM. RNB-61 has nephroprotective and/or antifibrotic effects. RNB-61 has negligible penetration into the brain .
    RNB-61

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