SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].
(2R,3S)-Fmoc-Abu(3-N3)-OH is a click chemistry reagent containing an azide group[1].
IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM.
Isoescin IA is a triterpenoid saponin isolated from the seeds of Aesculus chinensis. Isoescin IA has anti-HIV-1 protease activity[1].
C18:1 Glucosyl ceramide-d5 is deuterium labeled C18:1 Glucosyl ceramide.
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model[1][2].
GSK1034702 is a M1 mAChR allosteric agonist. GSK1034702 shows procognitive effects in rodents. GSK1034702 modulates hippocampal function to improve memory encoding in nicotine abstinence model of cognitive dysfunction[1].
(10-BRomodecyl)phosphonic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.IC50 value: 23 nM (EC50)Target: Orexin 2 ReceptorOrexin 2 Receptor Agonist shows not only potentactivity but also high selectivity for OX2R over OX1R. In CHO cells overexpressing hOX1R and HEK-293 cells overexpressing hOX2R, compound 26 displaced [125I]orexin-A in a concentration dependent manner: 26 bound to hOX2R and hOX1R with Ki of 0.14 and 0.77 μM, respectively.[1]
Cetrorelix Acetate is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM. Sequence: N-acetyl-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-Ser-Tyr-{Cit}-Leu-Arg-Pro-Ala-NH2.
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM[1].
Fipexide is a psychoactive drug of the piperazine chemical class, used as a nootropic drug, mainly for the treatment of senile dementia.
THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research[1].
NLRP3-IN-9 is a potent NLRP3 inhibitor. NLRP3-IN-9 inhibits IL-1β release. NLRP3-IN-9 reduces inflammation and mechanical hyperalgesia. NLRP3-IN-9 has the potential for the research of gout[1].
PDE4-IN-14 (Compound 1) is a PDE4 inhibitor that can be used in the study of PDE4-related diseases (such as inflammatory and immune diseases, cancer, and metabolic diseases, etc.)[1].
ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modulates oncogenic signaling through changes in GSK3, GS and β-catenin phosphorylation and MCL1 expression; suppresses tumor growth and inflammation-driven gastrointestinal disease symptoms without organ or hematological toxicity in vivo.
(2R)-SR59230A is the inactive isomer of SR59230A (HY-100672), and can be used as an experimental control. SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].
Topterone is a topical antiandrogen.
PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and with great potential for use in the treatment of inflammatory disorders and cancer metastasis[1].
Azilsartan mepixetil potassium (QR-01019K) is the antagonist of angiotensin II receptor. Azilsartan mepixetil potassium has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil potassium has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A)[1].
(R)-SLV 319 is a potent and selective cannabinoid receptor 1 (CB1) antagonist with a Ki value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319[1]
Biotin-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.
Eclalbasaponin I is isolated from Eclipta prostrata L with antitumor activity. Eclalbasaponin I inhibits the proliferation of hepatoma cell smmc-7721 with an IC50 value of 111.1703 μg/ml[1].
Emylcamate is a potent muscle relaxant. Emylcamate has the potential for the research of neurological diseases[1].
Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
CDK8-IN-10 (compound 2) is a potent, selective cyclin-dependent kinase (CDK8) inhibitor with an IC50 value of 8.25 nM. CDK8-IN-10 can be used for research of cancer[1].
JB062 is a nonmuscle myosin inhibitor with IC50 values of 1.6, 5.4, and >100 μM for Skeletal muscle myosin, Cardiac muscle myosin, and Smooth muscle myosin II, respectively. JB062 has cytotoxic to human cancer cells but not normal cells. JB062 can be used in research of muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy[1].
Tolvaptan-D7 (OPC-41061-D7) is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation[1][2].
Clobetasone butyrate is a synthetic glucocorticoid and has topical anti-inflammatory activity especially in skin. Clobetasone butyrate can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis and psoriasis[1].