penetration

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1 2 than HER4, less potent to MEK1 5, c-Met, Aurora B, Lck, CSK etc. Phase 1.

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.

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

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.

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.

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.

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.

Ganciclovir sodium (Cytovene IV sodium) is the sodium salt of Ganciclovir with antiviral activity, especially against cytomegalovirus (CMV) and herpes simplex virus type 1 (HSV-1).

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].

Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1 3 5 12 7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.

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

Maleimide (2,5-Pyrroledione) (2,5-Pyrroledone) is a new nanoparticle surface functional group which favors easy conjugation with cell penetration peptides. The conjugation is enabled via click chemistry to preserve its biofunctions.

AGI-026 (AGI-12026) is a novel and potent dual inhibitor of the mutant isocitrate dehydrogenase mIDH1 2 with the advantages of oral administration and penetration of the blood-brain barrier, with a drug concentration to plasma concentration ratio (brain plasma ratio) of 1.5 in brain tissue, and the ability to reduce the accumulation of the carcinogenic metabolite d-2-hydroxyglutarate (2-HG), which is used in the study of mIDH gliomas.

CSF1R-IN-7 is a highly selective CSF-1R inhibitor with good brain penetration for the treatment of a variety of diseases associated with microglia-mediated neuroinflammation, particularly Alzheimer's disease and other neurodegenerative disorders.CSF-1R is a type III receptor tyrosine kinase that is expressed predominantly on microglia (immune cells in the brain) and regulates the development, survival and function of microglia.

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

L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor.

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. 

Nav1.1 activator 1 is a highly potent activator of Nav1.1 with BBB penetration.

PF-03654746 Tosylate is selective antagonist of histamine H3 receptor with high brain penetration.

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

(RS)-Butyryltimolol, the racemate of Butyryltimolol, is an effective prodrug of Timolol that improves corneal penetration and acts as a β-adrenergic blocker [1][2].

Atropine methyl bromide (Methylatropine bromide) is a quaternary ammonium salt of atropine, characterized as a muscarinic receptor (mAChR) antagonist. It functions as a mydriatic to dilate the pupil during ophthalmic examination. Compared to atropine, it demonstrates reduced penetration into the central nervous system[1][2]. Its high polarity makes it particularly effective in relieving pyloric spasm in infants.