Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure.

(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) with IC50 of 1.8 μM and pIC50 of 5.75, has high CNS penetration.

BuChE-IN-TM-10 (TM-10) is a potent inhibitor of butyrylcholinesterase (BuChE), exhibiting an IC50 of 8.9 nM. It effectively inhibits and disaggregates self-induced Aβ aggregation, displays significant antioxidant activity, and demonstrates substantial penetration through the blood-brain barrier (BBB). TM-10 holds promise as a potential treatment for Alzheimer’s disease.

Difelikefalin acetate (CR 845 acetate) is a peripherally restricted kappa opioid receptor agonist. CR845 exhibit low P450 CYP inhibition and low penetration into the brain.

LAH4 acetate is the α-helical structure of the designed amphoteric peptide antibiotic, which is capable of complexing DNA, associating with the cell surface membrane and wrapped in the endosome, which is destroyed with the decrease of pH value. It has strong antibacterial, nucleic acid transfection and cell penetration activities. LAH4 acetate has high plasmid DNA transmission capacity. LAH4 acetate has a strong affinity for anions in bacterial membranes.

Epitinib succinate (HMPL-813 succinate) is an orally active and brain penetration EGFR tyrosine kinase inhibitor and can be used in studies about cancer.

Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).

CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent.

Metronidazole (Metronidazol) is a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities.

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Certepetide (CEND-1), also known as iRGD, is a bifunctional cyclic peptide that enhances tumor penetration. By interacting with alphav-integrins through its RGD motif and activating NRP-1, it transforms the solid tumor microenvironment into a temporary conduit for therapeutic agents. This property facilitates Certepetide's accumulation in tumors, making it a valuable tool in researching pancreatic cancer and other solid tumors [1] [2] [3].

PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist, exhibiting K i values of 44.4 nM for rat A2A receptors and 360 nM for human A2A receptors. For rat and human A1 receptors, it shows significantly lower affinity with K i values of ≥10000 nM and 541 nM, respectively. The compound demonstrates poor brain penetration and is not orally absorbable. It is of interest in research related to inflammatory bowel disease (IBD) [1] [2] [3].

JDB175, a selective BTK inhibitor with oral bioavailability, demonstrates excellent penetration through the blood-brain barrier. It exhibits potent activity against central nervous system lymphoma in a mouse model, with no apparent toxicity. JDB175 effectively suppresses human lymphoma cell proliferation by inhibiting the BTK signaling pathway, induces cell cycle arrest, and promotes apoptosis[1].

PGF2α isopropyl ester is an ester prodrug of PGF2α with enhanced lipid solubility. Due to better membrane penetration, PGF2α isopropyl ester is more suitable than PGF2α or PGF2α tromethamine salt for topical application in studies on intraocular pressure. The ester functionality is readily hydrolyzed in vivo to release the active compound PGF2α. When administered topically to the eyes of cynomolgus monkeys, a 5 μg dose reduces intraocular pressure by 68% after the fourth day of treatment.

ATP-polyamine-biotin is a cell-permeable, efficient kinase cosubstrate with conversions and kinetics similar to those of other known ATP analogues. APB shows a cytotoxicity EC50 value of 19 ± 1 mM. ATP-polyamine-biotin is shown to promote biotin labeling

C24 Phytosphingosine (t18:0/24:0) is a phytoceramide, which is a family of sphingolipids found in the intestine, kidney, and extracellular spaces of the stratum corneum of the mammalian epidermis. C24 Phytosphingosine (t18:0/24:0) is composed of a phytosphingosine backbone amine-linked to a C24 fatty acid chain. It has been used with other ceramides to create stratum corneum substitutes to study percutaneous penetration and psoriasis in vitro. In a stratum corneum model of healthy skin, the incorporation of long-chain-containing phytoceramides, such as C24 phytosphingosine (t18:0/24:0), increases permeability of the membrane in comparison with incorporation of dihydroceramides.

WAY267464 is a nonpeptide small-molecule OT agonists with anxiolytic activity. WAY267464 may be used for modulation of potency, selectivity over the structurally similar vasopressin receptors, CNS penetration, and oral bioavailability.

trans-Cyclohexane-1,2-diol (trans-1,2-Cyclohexanediol) has a synergistic retardation effect on percutaneous absorption and penetration of metronidazole (MTZ).

Grepafloxacin (OPC-17116) is a fluoroquinolone antibiotic that is administered orally. It possesses strong efficacy against community-acquired respiratory pathogens, notably Streptococcus pneumonia. Grepafloxacin exhibits excellent tissue penetration and demonstrates a promising pharmacodynamic profile.

Pegsebrenatide (NLY01), a long-acting GLP-1R agonist, exhibits an extended half-life and favorable blood-brain barrier penetration. It impedes A1 astrocyte transformation, mitigates dopaminergic cell death, and ameliorates motor symptoms in mouse models of Parkinson's disease (PD) [1].

HR2-18 is a bioactive peptide that inhibits SARS-CoV penetration into cells.

This novel compound is an orally bioavailable antagonist of P2X3/P2X2/3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2/3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2/3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1/2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

Z-Glycine (Carbobenzoxyglycine) is a drug-lipid conjugates designed to promote brain penetration based on its lipophilicity and resemblance to lipids in biological membranes[1].

C16 Phytoceramide (t18:0/16:0) is a phytoceramide, which is a family of sphingolipids found in the intestine, kidney, and extracellular spaces of the stratum corneum of the mammalian epidermis. C16 Phytoceramide (t18:0/16:0) is composed of a phytosphingosine backbone amine-linked to a C16 fatty acid chain. The levels of C16 phytoceramide (t18:0/16:0) increase following heat stress in S. cerevisiae. It has been used with other ceramides to create stratum corneum substitutes to study percutaneous penetration and psoriasis in vitro.

2-n-Nonyl-1,3-dioxolane is a biochemical. It is used as an absorption and penetration enhanceron transdermal.

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).

LAH4 TFA, an alpha-helix of the designed amphipathic peptide antibiotic, demonstrates potent antimicrobial, nucleic acid transfection, and cell penetration capabilities, alongside high plasmid DNA delivery capacities. It also exhibits a strong affinity for anionic lipids present in the outer membrane of bacterial membranes [1] [2] [3].

Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration. Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl displays only a weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropy

LY393615 (NCC1048) is a novel blocker of both neuronal Ca²⁺ (calcium) and Na⁺ (sodium) channels, exhibiting half-maximal inhibitory concentrations (IC₅₀) of 1.9 µM and 5.2 µM against α1A and α1B calcium channel subunits, respectively. This compound demonstrates effective brain penetration and has shown neuroprotective effects in cerebral ischemia models, suggesting its utility in neurological disease research [1].

N-Carbobenzyloxyglycine-d2 is a deuterated compound of N-Carbobenzyloxyglycine. N-Carbobenzyloxyglycine has a CAS number of 1138-80-3. Z-Glycine (Carbobenzoxyglycine) is a drug-lipid conjugates designed to promote brain penetration based on its lipophilicity and resemblance to lipids in biological membranes[1].

AWD 12-281 is a selective phosphodiesterase 4 (PDE4) inhibitor for the treatment of lung inflammation using inhalative administration. AWD 12-281 Is Active in a New Guinea-Pig Model of Allergic Skin Inflammation Predictive of Human Skin Penetration and Suppresses Both Th1 and Th2 Cytokines in Mice. AWD 12-281 is a very promising drug candidate not only for the treatment of lung inflammation using inhalative administration but also for the treatment of atopic dermatitis.

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

SHR0687 is a Highly Potent KOR Agonist. SHR0687 showed excellent selectivity over other opioid receptors, such as MOR and DOR. In addition, SHR0687 displayed favorable PK profiles across species, as well as robust in vivo efficacy in a rat carrageenan-induced pain model. Notably, SHR0687 exhibited negligible blood−brain barrier penetration, which was meaningful in minimizing CNS-related side effects.

L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM. 

Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2].

Flutrimazole is a dual-action imidazole antifungal compound, exhibiting both anti-inflammatory and antifungal properties. Notably, flutrimazole demonstrates limited transdermal penetration, making it particularly advantageous for topical applications in the treatment of fungal infections, especially those accompanied by inflammation.

Monocarboxylate transporter (MCT1) inhibitor (pKi = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.

AZD7268 is a potent, selective, reversible, and orally bioavailable agonist of δ-opioid receptor with CNS penetration.

BAY-846 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model.

PHA-543613 hydrochloride acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.

L-745870 is a high-affinity and selective human dopamine D4 receptor antagonist (Ki: 0.43 nM). L-745870 has excellent brain penetration. It considerably weaker D2 (Ki: 960 nM) and D3 (Ki: 2300 nM) receptors affinity.

SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. SNJ-1945 protects SH-SY5Y cells against MPP(+) and rotenone. SNJ-1945 reduces murine retinal cell death in vitro and in vivo. SNJ-1945 has good aqueous solubility, can prevents the heart from KCl arrest-reperfusion injury associated with the impairment of total Ca(2+) handling by inhibiting the proteolysis of alpha-fodrin as a cardioplegia.

GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC 50 of 35 nM. GSK-3β inhibitor 9 exhibits good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 is able to be used for the research of Alzheimer’s disease [1].

Valanafusp alfa (AGT-181) is a recombinant fusion protein that combines a chimeric monoclonal antibody targeting the human insulin receptor (HIR) with human iduronidase (IDUA), facilitating brain penetration. It is utilized in researching Mucopolysaccharidosis type I (MPS I) [1].

PF-06447475 trihydrochloride is a potent, selective LRRK2 kinase inhibitor that demonstrates excellent brain penetration, exhibiting IC50 values of 3 nM for wild-type LRRK2 and 11 nM for G2019S LRRK2 variants. It holds potential for Parkinson's disease (PD) research [1].

GSK-345931A, an EP(1) receptor antagonist, shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain.

Ro 64-6198 is a nonpeptide, high-affinity, and brain penetration N/OFQ receptor (NOP) agonist (EC50: 25.6 nM). Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors.

Anle138b: a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease