rodent-active — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T9786	Lu AF27139		P2X Receptor
	Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases st...		P2X Receptor
T39762	AHR antagonist 5 free base		Aryl Hydrocarbon Receptor
	AHR antagonist 5 free base is an orally active antagonist of AHR with IC50s of ~35-150 nM in human and rodent cell lines.		Aryl Hydrocarbon Receptor
T12419	PF-04634817 succinate		COX
	PF-0463481 succinate is a potent and orally active dual antagonist of CCR2/CCR5 with comparable human and rodent CCR2 potency with IC50 of 20.8 nM.		COX
T12419L	PF-04634817		CCR
	PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 pote...		CCR
T16113	ML753286		AMPK
	ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.		AMPK
T38666	CP-346086 dihydrate
	CP-346086 dihydrate is a potent and orally active inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM for both human and rodent MTP. This compound effectively lowers plasma cho...
TP2340	Hemoregulatory peptide 5b	hp 5B,Pglu-glu-asp-cys-lys-OH,Peedck,Glp-glu-asp-cys-lys-OH,SP1 Pentapeptide
	Hemoregulatory peptide 5b is a synthetic analog of granulocyte chalone which initially identified in extracts of rodent bone marrow and human leukocytes. Monomer inhibits both formations of GM-CFC colonies and cytotoxic ...
T21886	HE-3235
	Apoptone is a synthetic analogue of 3β-androstanediol which is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer [1].
T60537	ARUK3001185
	ARUK3001185 (Compound 8l) is a potent, selective, orally active, and brain-penetrant Notum inhibitor(IC50 = 6.7 nM) that is suitable for oral dosing in rodent models of disease [1].
T39587	APJ receptor agonist 4
	APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models an...
T28937	Tebuquine	WR-228,258,WR 228,258,CI 897,CI897,CI-897
	Tebuquine is an antimalarial agent. Tebuquine is active against P. falciparum in vitro. Tebuquine in vitro shows a chloroquine-like effect, but not in vivo, suggesting that its mode of action in vivo is different from th...
T72861	(6R)-ML753286
	'(6R)-ML753286, an isomer of ML753286, is an orally active, selective Breast Cancer Resistance Protein (BCRP) inhibitor, demonstrating an IC50 of 0.6 μM. It exhibits high permeability and low to medium clearance in roden...
T35731	Deethylindanomycin
	Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of...
T63153	APJ receptor agonist 5
	APJ receptor agonist 5 (compound 3) is a potent and orally active apelin receptor (APJ) agonist (EC 50:0.4 nM). APJ receptor agonist 5 has excellent pharmacokinetic profiles in rodent models of heart failure (HF) and an ...
T78827	CVN417
	CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC5...
T78649	MAO-B-IN-4		Monoamine Oxidase
	MAO-B-IN-4 (Compound 26) is a reversible monoamine oxidase B (MAO-B) inhibitor with potent in vitro activity, characterized by an IC50 value of 9 nM. This orally active compound exhibits favorable metabolic stability, a ...		Monoamine Oxidase
T63096	SB-277011 hydrochloride
	SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally active, dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier with Ki values of 10.7 nM and 11.2 nM for rodent and hu...
T82684	Connexin mimetic peptide 40,37GAP26
	Connexin mimetic peptide 40,37GAP26, a biologically active peptide, matches the GAP26 domain of the extracellular loop of major vascular connexins Cx37 and Cx40, referred to as 37,40Gap26 based on Cx homology. It has bee...