rodent

MRT-81 is a potent antagonist of human and rodent smoothened receptors that inhibits hedgehog activity with an IC50 value of 41 nM in Shh-light2 cells.It is used in the study of cancer.

BMS-191011 (BMS-A) is an activator of large-conductance calcium-activated potassium (BKCa) channels ,effective in stroke models

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 studies.

JP1302 is a selective α2C adrenoceptor antagonist with a Kb value of 16 nM and a Ki of 28 nM for human α2C receptors.JP1302 has antidepressant activity, disrupts the FACT complex and degrades histone H1.JP1302 has been used in the study of neuropsychiatric disorders, acute renal failure, and renal injury.

N,N'-Diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits. N,N'-diacetyl-L-cystine is also an effective and orally active modulator of contact sensitivity/delayed-type hypersensitivity reactions in rodents.

Clonixin (Clonixic acid) is a non-steroidal anti-inflammatory drug (NSAID) with analgesic properties. This compound has been reported to block prostaglandin synthesis, and to block inward calcium currents.

JP1302 dihydrochloride is a selective, high affinity antagonist of the alpha2C-adrenoceptor (α2C-adrenoceptor), with a Ki (binding affinity) value of 28 nM and a Kb value (antagonist activity) of 16 nM.

ABT-384 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1.

Coenzyme Q9 (Ubiquinone 9) (CoQ9) is a normal constituent of human plasma. CoQ9 in human plasma may originate as a product of incomplete CoQ10 biosynthesis or from the diet.

AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.

ML400 (CID73050863) is an allosteric inhibitor of LMPTP with an EC50 of 1μM. ML400 displays good cell-based activity and rodent pharmacokinetics.

AHR antagonist 5 free base is an orally active AHR antagonist with IC50 of approximately 35-150 nM in human and rodent cell lines, and exhibits anticancer activity.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).

BMS-903452 is a potent and selective GPR119 agonist with an EC50 of 14 nM, indicated for the treatment of acute and chronic rodent diabetes. GPR119 is mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. BMS-903452 shows no significant inhibitory effect on 9 cytochrome P450 enzymes (IC50 > 40 μM), does not activate PXR (EC50 > 50 μM), and is not toxic to liver (HEPG2) cell lines.

Dersalazine (Dersalazine Free Base), an inhibitor of platelet-activating factor, exerts intestinal anti-inflammatory activity in different rodent types of colitis by down-regulating IL-17 expression, with potential efficacy in patients with ulcerative colitis.

Broparestrol (E)- has antifertility activity and is a potent inhibitor of rodent mammary tumorigenesis.

Flutamide (SCH 13521) is an antiandrogen with about the same potency as cyproterone in rodent and canine species.

S-Methylisothiourea sulfate ((S)-Methylisothiourea sulfate) is a potent and selective inhibitor of iNOS and exerts beneficial effects in rodent models of septic shock[1].

Acifluorfen is a protoporphyrinogen oxidase (PPO) inhibitor herbicide that promotes the accumulation of protoporphyrin IX. It induces liver tumors, liver injury, and cardiac dysfunction in rodents, and causes severe photooxidative damage to pigments and lipids in susceptible plants. It can be used to induce hepatitis and pancreatitis.

Exisulind (CP248) induces apoptosis through the activation of protein kinase G (PKG). Exisulind exhibits antineoplastic activity in solid tumour and haematological cancer cell lines and is an inhibitor of tumour growth in rodent models of colon, prostate, bladder, mammary and lung cancer.

Tebideutorexant is a selective antagonist of the orexin-1 receptor and has demonstrated anti-panic effects in both rodent and human models of panic-anxiety. Tebideutorexant provides valuable insights into orexin signaling pathways in stress response and has potential utility as a tool compound for psychiatric and neurobehavioral disorder research.

Peptide5 acetate reduces animal swelling, astrogliosis, and neuronal cell death after spinal cord injury. Peptide5 acetate significantly reduces the degree of spinal cord injury (SCI) in a rodent ex vivo model.

Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor. Aftin-4(Aftin4) increased Aβ-1-42, but not Aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes similar to those found in the brains of patients with AD. Aftin-4(Aftin4) can thus be used to induce a rapid, acute Alzheimer's disease-like toxicity in the rodent brain.

ML 145 is a selective and potent antagonist of human GPR35, with no significant activity against GPR35 in any of its immediate rodent homologs.ML 145 has potential anti-inflammatory activity for the study of immunoinflammation.ML 145 is a novel non-steroidal anti-inflammatory agent for the study of rheumatoid arthritis.