complete

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

NS11394 is a effective and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of α(5) > α(3) > α(2) > α(1) at GABA(A) alpha subunit-containing receptors.

Complete Freund's adjuvant (CFA) is an emulsified immunostimulant containing mineral oil and heat-killed mycobacteria, capable of inducing Th1 responses and enhancing immune reactions. It is frequently employed in establishing rat models of rheumatoid arthritis and persistent inflammatory pain.

Incomplete Freund's adjuvant (IFA) is an emulsified mineral oil-based immunostimulant that induces Th2 responses and enhances immune reactions, promoting storage effects at vaccination sites.

Dazostinag disodium (TAK-676) is a synthetic novel interferon gene (STING) agonist that triggers STING signaling pathway activation and type I interferon activation. Dazostinag disodium (TAK-676) is also a highly effective immune system modulator with complete resolution and lasting memory of T cell immunity and the ability to promote lasting interferon-dependent anti-tumor immune responses.

AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM).

FC 11 is a highly potent focal adhesion Ki nase (FAK) PROTAC®Degrader (DC50 values are 40 to 370 pM depending on cell line), which is composed of the FAK inhibitor PF 562217 joined by a linker to the cereblon-binding ligand Pomalidomide. The effects of FC 11 are reversible upon compound wash out. FC 11 also degrades autophosphorylated FAK (pFAKtyr397), displaying near complete degradation after 3 hours at 100 nM in TM3 cells.

(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg/kg, i.v., 50-200 J/cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg/m2, IV, 100 J/cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.

Tetradecylthioacetic acid is a synthetic fatty acid with a sulfur substitution in the β-position. This modification renders TTA unable to undergo complete β-oxidation and increases its biological activity, including activation of peroxisome proliferator activated receptors (PPARs) with preference for PPARα.

LY2457546 is a highly potent, orally bioavailable multi-target anti-angiogenic tyrosine kinase inhibitor. It shows strong inhibitory activity against multiple targets including VEGFR2, PDGFRβ, FLT-3, Tie-2, and Eph family receptors, and is applied in cancer research such as leukemia.

Flibanserin (T4297), a compound identified as BIMT-17, acts as a complete agonist at the serotonin 5-HT1A receptor, with a binding affinity (Ki) of 1 nM, while functioning as an antagonist at the 5-HT2A receptor with a 49 nM affinity. Flibanserin-D4 represents a deuterium-labeled version of Flibanserin.

Fosmanogepix (APX001) is a first-in-class, orally available broad-spectrum antifungal agent. It acts as an N-phosphonooxymethyl prodrug that undergoes rapid and complete metabolism by systemic alkaline phosphatases. This metabolism leads to the formation of the active moiety, APX001A. Fosmanogepix (APX001), with its ability to target the highly conserved Gwt1 fungal enzyme, holds great potential for the development of treatments against invasive fungal infections.

Draflazine is an ENT1 inhibitor. It completely reverses the hypersensitivity in the complete Freund's adjuvant (CFA) model of mechanical hyperalgesia. Draflazine also completely reverses the hypersensitivity of the carrageenan inflammation model of therma

A-889425 is a selectively active oral TRPV1 receptor antagonist with IC50 values of 335 nM (rat) and 34 nM (human). This compound effectively penetrates the central nervous system, reducing mechanical allodynia and the response of spinal neurons to mechanical stimuli in rat paws following inflammation induced by Complete Freund's Adjuvant.

E3 Ligase Ligand-linker Conjugate 133 is a critical intermediate in the synthesis of the complete PROTAC molecule CPD-39, comprising a conjugate (conjugate of E3 ligase Ligand and linker) that connects the E3 ligase ligand with a linker.

E3 Ligase Ligand-linker Conjugate 131 serves as a crucial intermediate in the synthesis of the complete PROTAC molecule CPD-39; it represents a (conjugate of E3 ligase Ligand and linker). This compound is vital for bridging the components necessary for forming the active PROTAC structure.

E3 Ligase Ligand-linker Conjugate 134 is a crucial intermediary in synthesizing the complete PROTAC molecule STING-IN-10. It consists of a conjugate of an E3 Ligase Ligand and a linker, which facilitates the assembly of the target molecule.

E3 Ligase Ligand-Linker Conjugate 135 is a critical intermediate in the synthesis of the complete PROTAC molecule pan-KRAS degrader 5, comprising a conjugate of E3 ligase ligand and linker.

Dihydrotestosterone-KLH is a hapten-carrier protein conjugate formed by coupling Dihydrotestosterone (DHT) to keyhole limpet hemocyanin (KLH). As a hapten, Diethylstilbestrol alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. Dihydrotestosterone-KLH may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M TBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

SR-12062 functions as a full agonist at neurotensin receptor 1 (NTSR1), demonstrating notable efficacy and increased potency. Its EC50 value on NTSR1 is 2 μM, with complete receptor activation (Emax=100%). Compared to the parent compound 1 (EC50=178 μM; Emax=17%), SR-12062 shows approximately 90-fold greater potency.

MD-265 is a PROTAC degrader that targets and degrades MDM2, leading to the activation of p53 in cancer cells with wild-type p53. MD-265 achieves complete tumor regression and enhances long-term survival in leukemic mice.

BI-113823 is an orally active and selective bradykinin B1 receptor antagonist. It alleviates mechanical hyperalgesia induced by complete Freund's adjuvant in rats. BI-113823 is applicable for research on chronic inflammatory pain.