brain penetrant — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T15275	Fenobam		GluR
	Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric mo...		GluR
T9346	CVN424		GPR
	CVN424 is a selective and novel GPR6 Inverse agonist effective in models of Parkinson Disease.		GPR
T9466	RTICBM-189		Others
	RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectivel...		Others
T9452	PW0787		GPR
	PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM).		GPR
T9697	ASK1-IN-1		ASK
	ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.		ASK
T4081	MPTP hydrochloride	MPTP-hydrochloride	Apoptosis , Dopamine Receptor
	MPTP hydrochloride is a precursor of MPP+, a dopamine neurotoxin with blood-brain barrier permeability. MPTP hydrochloride is toxic to dopaminergic neurons, which can lead to Parkinson's disease, and is widely used in th...		Apoptosis , Dopamine Receptor
T12998	SR10067		Others , Autophagy
	SR10067 is a potent, selective and brain penetrant agonist of Rev-Erbα/β(IC50 of 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively),has anxiolytic activity.		Others , Autophagy
T21747	VU0483605		GluR
	VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.		GluR
T8554	KCC-07		DNA Alkylator/Crosslinker
	KCC-07 is a selective, potent and brain-penetrant inhibitor of methyl-CpG-binding domain protein 2(MBD2) with anticancer activity. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenes...		DNA Alkylator/Crosslinker
T3707	GNE-3511	GNE3511	DNA Alkylation , MAPK
	GNE-3511 is a potent and selective dual leucine zipper kinase inhibitors.		DNA Alkylation , MAPK
T6031	GNE0877	GNE 0877,GNE-0877	LRRK2
	GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).		LRRK2
T7100	PLX5622	PLX-5622	c-Fms , CSF-1R
	PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor.		c-Fms , CSF-1R
T27620	IP7e	IP 7e,IP-7e,isoxazolo-pyridinone 7e	Others
	IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC50 value of 3.9 nM.		Others
T21793	CGP 35348		GABA Receptor
	CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice.		GABA Receptor
T0492	Dimethyl fumarate	DMF	Reactive Oxygen Species , HIV Protease , Nrf2 , Endogenous Metabolite , Autophagy
	Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.
T21652	RN-1 dihydrochloride		Histone Demethylase , MAO
	RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).		Histone Demethylase , MAO
T6504	Flupirtine maleate	Katadolon maleate	Potassium Channel , NMDAR , iGluR
	Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.		Potassium Channel , NMDAR , iGluR
T15781	LP-935509		Serine/threonin kinase , AAK1 (AP2 associated kinase 1)
	LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure. LP-935509 is also an effective inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-...		Serine/threonin kinase , AAK1 (AP2 associated kinase 1)
T9146	Ms48107	Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-	Others
	MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion ch...		Others
T9157	GP130 receptor agonist-1	N-(4-Fluorophenyl)-4-phenyl-2-thiazolami	Interleukin
	GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.		Interleukin