r form

Bay 65-1942 (R form) is the less active enantiomer of Bay 65-1942, a selective and ATP-competitive IKKβ inhibitor.

EMD638683 is a highly selective SGK1 inhibitor with an IC50 of 3 μM. EMD638683 (R-Form) is the R-form of this compound.

BD-AcAc 2 (Ketone Ester) is a ketone monoester and can be used as a source of oral nutritional ketones. BD-AcAc 2 can elevate plasma levels of acetoacetate and β-hydroxybutyrate, blood Na+, blood glucose levels and blood creatinine levels after oral administration in mice. BD-AcAc 2 can partly prevent muscle weakness in septic mice. BD-AcAc 2 exhibits potential to improve endurance and exercise performance in animal body. BD-AcAc 2 can also be used to research diabetes or Parkinson's disease.

Fipexide (Attentil, Vigilor), a psychoactive drug of the piperazine chemical class, was developed in Italy in 1983. It was served as a nootropic drug in France and Italy, mainly for the therapy of senile dementia, but is no longer in common use because of the occurrence of rare drug side-effects including hepatitis and fever.

Arformoterol Tartrate ((R,R)-Formoterol tartrate) is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity[2].

Pactimibe is a ACAT inhibitor. It has anti-atherosclerotic activity.

Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor, acting on ACAT1 (IC50: 4.9 μM) and ACAT2 (IC50: 3.0 μM). It inhibits oleoyl-CoA non-competitively (Ki: 5.6 μM) and significantly inhibits cholesterol ester formation (IC50: 6.7 μM). Pactimibe sulfate reduces plasma cholesterol activity and has anti-atherogenic potential.

Minnelide is an effective therapy against pancreatic cancer. Minnelide Inhibits Androgen Dependent, Castration Resistant Prostate Cancer Growth by Decreasing Expression of Androgen Receptor Full Length and Splice Variants. Minnelide reduced tumor volume in multiple models of pancreatic cancer. Minnelide was a more effective drug against pancreatic cancer models. It effectively reduced tumor burden and tumor related morbidity in different unique but complementary mouse models. It reduced metastatic spread and increased survival in the different models as well.

Arformoterol Tartrate (Standard) is the standard substance of Arformoterol Tartrate, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Arformoterol Tartrate ((R,R)-Formoterol tartrate) is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity.

(Rac)-Apremilast D5 is a deuterium-labeled version of the enantiomer (R)-Apremilast, also known as (R)-CC-10004, which itself is one specific form of Apremilast.

SAR405 (R enantiomer) is the less active form of SAR405, an inhibitor of PIK3C3/Vps34.

(R)-Pantetheine (Pantetheine) is the biologically active form of VB5 (pantothenic acid), which occurs in nature in various forms of Pantetheine-containing ligands (PCL). (R)-Pantetheine increases platelet cell membrane fluidity and inhibits platelet aggregation.

(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized conjugate for E3 ligase ligand-linker applications, combining the VH032 VHL-based ligand with a linker for PROTAC development. VH-032 is a selective and potent VHL/HIF-1α interaction inhibitor with a dissociation constant (Kd) of 185 nM, offering potential in anemia and ischemic diseases research[1].

(R,S,S)-VH032-Me is a ligand for the E3 ubiquitin ligase. It can connect with a target protein ligand via a linker to form dTAGV-1-NEG. This PROTAC can induce the ubiquitination and subsequent degradation of oncogenic proteins.

(S,R,S)-AHPC-Boc derivative 1 (Compound 80-9; VH032-Boc derivative 1) is a selective proteasomal degrader targeting MALT1, which recruits the E3 ubiquitin ligase CRBN to form a ternary complex with MALT1. This interaction leads to the ubiquitination and subsequent proteasomal degradation of MALT1. By disrupting the CBM complex, (S,R,S)-AHPC-Boc derivative 1 inhibits the NF-κB signaling pathway and shows potential in inducing apoptosis in ABC-DLBCL cells. It holds promise for research into MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL).

β2AR agonist 2 (compound 8a) is an agonist of the β2-adrenergic receptor (β2AR). It is a saturated azacyclic compound featuring a 4- to 7-membered heterocycle. The compound has a chiral structure in the -R form by incorporating a carbon with a requisite hydroxyl group, which significantly stimulates glucose uptake in skeletal muscle cells, thereby enhancing cellular glucose uptake (GU). β2AR agonist 2 is applicable in the study of type 2 diabetes (T2D).

(S,R,S)-AHPC-C7-aminedihydrochloride is the dihydrochloride salt form of (S,R,S)-AHPC-C7-amine. The compound (S,R,S)-AHPC-C7-amine is a synthetic E3 ligase ligand-linker (E3ligaseligand-linker conjugate) that includes a VHL ligand based on VH032 and one linker. It is utilized for synthesizing PROTAC degraders targeting ERRα.

(S,R,S)-AHPC-Me-piperazine-acetyl-PIP-AcOH is a conjugate of the VHL ligand of the E3 ubiquitin ligase VH032 and a linker. This linker component of (S,R,S)-AHPC-Me-piperazine-acetyl-PIP-AcOH can be further conjugated with a target protein ligand (such as BCR-ABL1) to form a PROTAC molecule.

(R,S)-Cotinine-d3N-Oxide is the deuterated form of (R,S)-Cotinine N-Oxide.

Levomefolate magnesium is the magnesium salt of the metabolite of folic acid (Vitamin B9) and it is a predominant active form of folate found in foods and in the blood circulation, accounting for 98% of folates in human plasma. It is transported across th

(R)-nitro-Blebbistatin is a more stable form of (+)-blebbistatin , which is the inactive form of (-)-blebbistatin . Prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications. The addition of a nitro group stabilizes the molecule to circumvent its degradation by prolonged blue light exposure. (R)-nitro-Blebbistatin has the same stereochemistry as the inactive (+)-blebbistatin enantiomer.

IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species with diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties [1,2,3]. It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng/ml) [1], inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg/ml), and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia [2,3]. Additionally, it is active against T. spiralis in vitro and in vivo [1].

Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid.[1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D1 is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase.[1] 17(R)-RvD1 is an aspirin-triggered epimer of RvD1 that reduces human polymorphonuclear leukocyte (PMN) transendothelial migration, the earliest event in acute inflammation, with equipotency to RvD1 (EC50 = ~30 nM).[3] 17(R)-RvD1 exhibits a dose-dependent reduction in leukocyte infiltration in a mouse model of peritonitis with maximal inhibition of ~35% at a 100 ng dose.[3] In contrast to RvD1, the aspirin-triggered form resists rapid inactivation by eicosanoid oxidoreductases. Analytical and biological comparisons of synthetic 17(R)-RvD1 with endogenously derived 17(R)-RvD1 have confirmed its identity as matching the natural product.[4]

Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of 5 mM.2,3Olsalazine (150 mg/kg for 8 days) improves stool consistency and decreases occult and gross bleeding as well as myeloperoxidase (MPO) activity and leukotriene B4levels in colon tissue in a mouse model of acute colitis induced by dextran sulfate .4Olsalazine also inhibits bovine xanthine oxidasein vitro(IC50= 3.4 mg/L) and lowers serum uric acid levels in a mouse model of hyperuricemia induced by oxonic acid when administered at a dose of 20 mg/kg.5Formulations containing olsalazine have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis. 1.Nugent, S.G., Kumar, D., Rampton, D.S., et al.Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugsGut48(4)571-577(2001) 2.Pamukcu, R., Hanauer, S.B., and Chang, E.B.Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro. Comparison with sulfasalazine and 5-aminosalicylic acidGastroenterology95(4)975-981(1988) 3.Mohsen, A.Q.M., Mulvey, D., Priddle, J.D., et al.Effects of olsalazine in the jejunum of the ratGut28(3)346-352(1987) 4.Murthy, S., Murthy, N.S., Coppola, D., et al.The efficacy of BAY y 1015 in dextran sulfate model of mouse colitisInflamm. Res.46(6)224-233(1997) 5.Niu, Y., Li, H., Gao, L., et al.Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activityJ. Pharmacol. Sci.135(3)114-120(2017)