s-enantiomer

GSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).

Cipropride S enantiomer is the S enantiomer of cipropride which is an antiemetic drug.

PNU-282987 S enantiomer free base is an agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR).

Selisistat S-enantiomer (EX-527 S-enantiomer) is an effective and specific SIRT1 inhibitor (IC50 = 98 nM) and shows >200-fold selectivity against SIRT2 3.

Firsocostat S enantiomer is the less active S enantiomer of Firsocostat.

MK-7246 S enantiomer is a potent and selective CRTH2 antagonist.

LY 344864 S-enantiomer, the S-enantiomer of LY344864, serves as a 5-HT1F receptor agonist.

(S)-PNU-282987 is the absolute stereochemistry form of PNU-282987. PNU 282987, a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors (nAChRs) with Ki of 26 nM for the rat receptor, has negligible activity against α1β1γδ and α3β4 nAC

Necrostatin 2 (S enantiomer) is the S enantiomer of Necrostatin 2.

Ruxolitinib S enantiomer (INCB18424) is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.

Firsocostat S enantiomer (ND-630 S enantiomer) is the less active S enantiomer of Firsocostat. Firsocostat is an acetyl-CoA carboxylase ( ACC ) inhibitor.

Tipifarnib S enantiomer ((S)-(-)-R-115777) is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase inhibitor (IC50: 0.6 nM).

Nazartinib is an EGFR inhibitor. Nazartinib S-enantiomer is the less active S-enantiomer of Nazartinib.

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, inhibiting CDK9 CycT1 with an IC50 of 16 nM.

Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant S enantiomer dihydrochloride is an low activity enantiomer of elacestrant dihydrochloride.

Elacestrant S enantiomer is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

Veledimex S enantiomer is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system and CYP3A4/5 inhibitor.

Gepotidacin S enantiomer is an S enantionmer of gepotidacin.

The S-enantiomer of BET-BAY 002, referred to as BET-BAY 002 S enantiomer, is a potent inhibitor of BET (Bromodomain and Extra-Terminal motif proteins).

GDC-0834, the S-enantiomer, is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK).

Fulvestrant S enantiomer is the less active S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.

AMG 487 S-enantiomer, the S enantiomer of AMG 487, is a CXCR3 antagonist.

IACS-8968 S-enantiomer is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).

(S)-AK-242 ((S)-Resatorvid) is a cytokine inhibitor used in the treatment of heart disease, autoimmune disease, and inflammatory disease.

Ribocil-B is the active S-isomer of ribocil, capable of inhibiting flavin mononucleotide (FMN, KD of 6.6 nM).

INT-777 is the R-enantiomer of INT-777, less potent than INT-777,EC50 of 4.79 μM for TGR5.

Levamlodipine (S-amlodipine) belongs to the dihydropyridine group of calcium channel blockers. Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however, with differing nomenclature. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Chirocaine. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Adverse drug reactions (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic reactions can rarely occur.

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

Levamlodipine besylate ((S)-Amlodipine Besylate (103129-82-4(free base))) , also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. Levamlodipine besylate belongs to the dihydropyridine group of calcium channel blockers. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however, with differing nomenclature. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor and the pure S(-)-enantiomer of bupivacaine, used as a long-acting local anesthetic.

Escitalopram Oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.

N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide is a racemic form of Cl-amidine (S enantiomer). Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor.

α1 adrenoceptor-MO-1 (S enantiomer) has affinity at alpha 1 adrenergic receptor with alphalytic activity and analgesic action. It has more active than R enantiomer.

(S)-VB 201 is the S-enantiomer of VB 201.VB 201 oxidizes lipid compounds, has anti-inflammatory activity, and can be used for inflammation caused by coronavirus infection.

(S)-Lisofylline is the inactive optical enantiomer of (R)-lisofylline which is an anti-inflammatory agent. (S)-Lisofylline is exclusively converted to pentoxifylline in human liver microsomes.

(S)-ErSO is an inactive dextrorotatory enantiomer of ErSO.

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is an S enantiomer of blebbistatin. It is a potent and selective myosin II inhibitor with IC50 ranging from 0.5 to 5 μM.

Levosulpiride (S-(-)-Sulpiride) is the (S)-enantiomer of sulpiride, which is a D2 receptor antagonist, an atypical antipsychotic drug of the benzamide class.

(R)-GNE-140 (GNE-140) is an effective LDHA LDHB inhibitor (IC50s: 3 5 nM) and is 18-fold more potent than S enantiomer.

S-Dihydrodaidzein ((3S)-7-hydroxy-3-(4-hydroxyphenyl)-2,3-dihydrochromen-4-one) is an enantiomer of dihydrodaidzein which is involved in equol biosynthesis in a lactic acid bacterium, Lactococcus sp. strain.

MDL 100009, the S-enantiomer of MDL 100151 and the opposite enantiomer of MDL 100907, is a selective antagonist of 5-HT2A.

(S)-crizotinib (ent-crizotinib) （IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

(S)-(+)-Rolipram ((+)-Rolipram) inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM and exhibits anti-inflammatory and anti-depressant activity in the central nervous system, though it is less potent than its R enantiomer.

(±)-Equol ((R,S)-Equol) is a non-steroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzen by human intestinal microflora. The estrogen receptor (ER) agonist activity of the naturally occurring (S)-enantiomer (EC50 = 85 and 65 nM for human ERα and ERβ, respectively) is similar to that of genistein but exceeds that of daidzein. (±)-Equol preferentially binds ERβ (Ki = 0.73 nM) and demonstrates approximately 9-fold lower affinity for ERα (Ki = 6.41 nM). (±)-Equol is also a potent antagonist of dihydrotestosterone, which has important implications for prostate cancer and other androgen-mediated pathologies.

P7C3-OMe, a pro-neurogenic agent, has therapeutic benefits in neurodegenerative diseases. The R-enantiomer of P7C3-OMe is far more active than the S-enantiomer.

11(S)-HETE, an (S) enantiomer of 11(R)-HETE and a type of oxylipin, is non-enzymatically synthesized from arachidonic acid. Compared to its counterpart, 11(S)-HETE levels are found to be elevated in both isolated human plasma and serum, as well as in LPS-stimulated isolated human plasma. Notably, patients with allergic rhinitis exhibit a decrease in 11(S)-HETE levels in their serum following one year of double-mite subcutaneous immunotherapy (DM-SCIT), correlating with an enhanced quality of life, particularly in aspects related to rhinoconjunctivitis.

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

(±)-4-hydroxy Propranolol β-D-glucuronide is a metabolite of (±)-4-hydroxy propranolol , which is a metabolite of propranolol. The apparent half-life of (±)-4-hydroxy propranolol β-D-glucuronide is similar to propranolol and 4-hydroxy propranolol. Propranolol is a β-adrenergic antagonist, and the active enantiomer, (S)-(-)-propranolol , has log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively.