Inflammation/Immunology

Timolol is a β-blocker available for both topical and systemic administration. Topical Timolol is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension. Timolol can also be used for the research of infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation.Timolol also has cardioprotective effect.

HY-P990999 is an FCGRT-targeting IgG1λ2 type human antibody, the recommed isotype control is Human IgG1 lambda2, Isotype Control (HY-P990096).

Racotumomab (Anti-Human NGcGM3 Recombinant Antibody) is an anti-idiotype monoclonal antibody (MAb). Racotumomab reacts to Neu-glycolyl (NeuGc)-containing gangliosides, sulfatides, and other antigens expressed in tumors. Racotumomab is an active anticancer agent for lung cancer.

PSB 0777 ammonium hydrate is a potent and selective adenosine A_2A receptor full agonist with K_i values of 44.4 nM, 360 nM for rat and human A_2A receptors, respectively. PSB 0777 ammonium hydrate has K_i values of ≥10000 nM, 541 nM for rat and human A₁ receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research.

PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC₅₀ of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.

CL-197 is an orally active and long-acting purine anti-HIV nucleoside reverse transcriptase inhibitor (NRTI). CL-197 has potential effect on the research of viral, oncological and cerebrovascular diseases. CL-197 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

9-cis-Retinoic acid-d₅ is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.

GPR4 antagonist 1 is a GPR4 antagonist, with an IC₅₀ of 189 nM.

Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC₅₀=1.3 μM in human liver microsomes) and CYP2D6 (K_i=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.

Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody to the human ICAM-1, inhibits leukocyte adhesion to the vascular endothelium, thereby decreasing leukocyte extravasation and inflammatory tissue injury. Enlimomab has anti-inflammatory effects, and can be used for stroke research .

HY-P990926 is an SIRPA-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

SGK1-IN-2 (Compound 14h) is a selective, ATP-competitive SGK1 inhibitor, with an IC₅₀ of 0.005 μM at 10 μM ATP and an IC₅₀ of 0.025 μM at 500 μM ATP. SGK1-IN-2 can be used in studies of cancer, hypertension and diabetes.

Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia.

SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .

Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP₂, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [³H] PGD2 from human recombinant DP₂ (K_i=13 nM), rat recombinant DP₂ (K_i=3 nM), and human native DP₂ (K_i=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils.

CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC₅₀=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC₅₀ of 0.04 μM.

PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER⁺ breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer.

Flobufen (VUFB 16066) is a non-steroidal anti-inflammatory agent and cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor agent. Flobufen inhibits alloantigen-driven cellular immune responses and stimulates phagocytosis of peritoneal cells. Flobufen can improve immunopathological disorders and has an inhibitory effect on rheumatoid arthritis.

AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth.

Ufenamate (Flufenamic acid butyl ester) is an anthranilic acid-based anti-inflammatory drug that can be used in the study of skin diseases such as acute and chronic eczema, contact dermatitis, diaper dermatitis, miliary rashes and atopic dermatitis. Ufenamate has a certain photoprotective effect, reduces the degree of skin erythema and swelling in the photoaging model, downregulates the expression level of COX-2 and can promote the healing of mouse skull defects by secreting BMP2.