Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: 0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection[1].
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
Sinigrin (hydrate) is a natural aliphatic glucosinolate present in plants of the Brassicaceae family. Sinigrin (hydrate) exhibits anti-cancer, antibacterial, antifungal, antioxidant and anti-inflammatory activities[1].
Ifinatamab is monoclonal immunoglobulin G1-kappa with anti-human B7 homolog 3 protein (Human B7-H3). Ifinatamab is a glycoforme α immunomodulateur[1].
Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis[1].
1-Eicosanol-d41 is the deuterium labeled 1-Eicosanol[1]. 1-Eicosanol is a natural compound with antioxidant activity isolated from Hypericum carinatum[2].
Hyptadienic acid is a triterpene acid that can be isolated from the leaves of Perilla frutescens. Hyptadienic acid inhibits 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice with an ID50 value of 0.13 mg/ear. Hyptadienic acid can be used for the research of inflammation[1].
SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research[1][2].
SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research[1].
Methyllucidone is a neuroprotective agent and an antioxidant that can be isolated from Lindera erythrocarpa Makino. Methyllucidone inhibits the ROS production, and activates antioxidant signaling pathways that include Nrf-2 and PI3K[1].
Isopicropodophyllone, a natural compound that can be isolated from leaves of Podophyllum hexandrum, possesses antifungal activity[1].
Verbascose, an alacto-oligosac-charides (GOS), has potent immunostimulatory activity. Verbascose acts as a potential natural immunomodulatory agent[1].
Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.Target: PDE4; mACHRIrsogladine treatment (300 and 500 mg/kg/day) resulted in a dose-dependent reduction of angiogenesis in wild-type mice by 21 and 45.3% (P < 0.02, P < 0.001), in tPA-deficient mice by 42.6 and 46% (P < 0.001, P < 0.001), and in uPA-deficient mice by 27.2 and 46% (P < 0.05, p < 0.001), respectively. Irsogladine inhibits bFGF-induced angiogenesis in wild-type, tPA-knockout, and uPA-knockout mice [1]. Irsogladine up-regulates GJIC between PC cells via regulation of the PKA pathway. It also suggests a useful adjuvant of Irsogladine to pancreatic cancer therapy [2]. irsogladine produces the increase of intracellular cAMP content via non-selective inhibition of PDE isozymes, which may be a key mechanism involved in its gastroprotective actions [3].
(S)-Lansoprazole (Levolansoprazole) is an isoform of Lansoprazole (HY-13662), which is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1][2].
BMS-561392 is a TNF alpha-converting enzyme (TACE) inhibitor. BMS-561392 is also an ADAM17 blocker. BMS-561392 can be used for research of inflammatory bowel disease[1][2].
12-Dehydrogingerdione is an inhibitor of NO Synthase. 12-Dehydrogingerdione signi?cantly inhibits LPS-stimulated production of NO, IL-6 and PGE2 in Raw 264.7 cells[1].
AK-IN-1 (compound 4072-2732) is an adenosine kinase (AK) inhibitor that is competitive for adenosine (Ado) but not for ATP. AK-IN-1 inhibits 86%, 87% and 89% of AK activity at concentrations of 2, 4 and 10 µM, respectively. AK-IN-1 has good potential for research in many disease areas, including ischaemia, inflammation and seizures[1].
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects[1].
L-Hisidine is an essential amino acid for infants. L-Hisidine is an inhibitor of mitochondrial glutamine transport.
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells[1].
Ergosterol is the primary sterol found in fungi, with antioxidative, anti-proliferative, and anti-inflammatory effects.
Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM[1].
Alcaftadine(R89674) is a H1 histamine receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis.Target: H1 Histamine ReceptorAlcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. alcaftadine was more effective than placebo and at least as effective as olopatadine 0.01% in preventing ocular itching at 15 minutes and at 16 hours after administration. Alcaftadine 0.025% ophthalmic solution has been approved by the U.S. Food and Drug Administration for prevention of itching associated with allergic conjunctivitis in patients over 2 years of age [1]. Alcaftadine is a safe and effective option for the prevention of ocular itching associated with allergic conjunctivitis, is dosed once daily, and is competitively priced among prescription medications for allergic conjunctivitis [2].
SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
p2Ca, an 8-mer peptide, is a ligand that is naturally processed and presented to the Ld-alloreactive T cell clone, 2C.
Bapotulimab (BAY-1905254) is a fully human IgG2 antibody targeting immunoglobulin-like domain containing receptor 2 (ILDR2). Bapotulimab has antitumor and immunosuppressive effects[1].
Betamethasone is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties.Target: Glucocorticoid ReceptorBetamethasone is a potent glucocorticoid steroid with anti-inflammatory and immunosuppressive properties. Unlike other drugs with these effects, betamethasone does not cause water retention. The median (range) IC50 value for betamethasone butyrate propionate evaluated in the streptococcal pyrogenic enterotoxin A-stimulated peripheral-blood mononuclear cells was 291.6 (0.001-1171.5) ng/ml, which was significantly higher than the value 0.072 (0.01-222.5) ng/ml found in concanavalin A-stimulated peripheral-blood mononuclear cells (P=0.0245) [1]. Children exposed prenatally to betamethasone (n = 121) did not differ in systolic or diastolic blood pressure from children exposed to placebo (n = 102) (mean difference: systolic: -1.6 mm Hg; 95% confidence interval: -4.1 to 0.8 mm Hg; diastolic: -0.3 mm Hg; 95% confidence interval: -2.5 to 1.8 mm Hg) [2]. Intra-articular corticosteroid injection of 6 mg of betamethasone acetate/betamethasone sodium phosphate at the knee joint was not significantly associated with SAI at the time points tested [3].Clinical indications: Dermatitis; Discoid lupus erythematosus; Eczema; Lichen; Prurigo; PsoriasisToxicity: Symptoms of overdose include burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria.
Tozorakimab (MEDI-3506) is a human immunoglobulin G1 monoclonal antibody targeting interleukin-33. Tozorakimab can be used to research chronic obstructive pulmonary disease[1].